Geoffrey Shapiro, MD, PhD
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Biography
Geoffrey Shapiro, MD, PhD
Dr. Shapiro received his PhD in 1987 and his MD in 1988 from Cornell University, followed by postgraduate training in internal medicine at Beth Israel Hospital, Boston, where he served as chief medical resident. He completed a fellowship in medical oncology at Dana-Farber Cancer Institute, during which he investigated the role of cell-cycle-related proteins in lung cancer. He joined the Dana-Farber faculty in 1994.
Dr. Shapiro's practice is based in the Center for Cancer Therapeutic Innovation, where he develops and leads early phase clinical trials primarily focused on cell cycle and DNA repair inhibitor therapeutics and provides mentoring to early career investigators. As Senior Vice President, Developmental Therapeutics, he leads DFCI efforts for National Cancer Institute (NCI)-sponsored clinical trials developed through the Experimental Therapeutics Clinical Trials Network (ETCTN) and works integrally with multiple disease groups within the Institute.
Researcher
Physician
Centers/Programs
Clinical Interests
Developmental therapeutics, Phase 1 clinical trials, Solid tumors
Board Certification
- Medical Oncology
Fellowship
- Dana-Farber Cancer Institute, Medical Oncology
Residency
- Beth Israel Hospital, Chief Medical Resident
- Beth Israel Hospital, Internal Medicine
Medical School
- Weill Medical College of Cornell University
Research
Cell-Cycle-Related Targets for Antitumor Drug Development
Cyclin-dependent kinases (cdks) are critical regulators of cell cycle progression and RNA transcription. A variety of genetic and epigenetic events cause universal overactivity of the cdks in human cancer, and their inhibition frequently leads to cell cycle arrest, depletion of transcripts with short half-lives, and apoptosis. Using siRNA technology, we have recently shown that depletion of both cell cycle and transcriptional cdk activities induces apoptosis in transformed cells. A primary focus of our laboratory is the characterization of cdk inhibitor drugs that mimic these effects. We are investigating both pan-cdk inhibitors, including flavopiridol, as well as inhibitors more selective for cdks 1 and 2. These compounds induce p53-independent apoptosis in transformed cells and modulate phosphorylation of Rb, p27(Kip1) and E2F-1. We are designing pharmacodynamic assays to assess their biologic effects in tumors as early-phase trials begin. In addition, we have found that cdk inhibition is synergistic with DNA damage in inducing cancer cell death. Cdk inhibition following cell-cycle disruption by chemotherapy drugs may alter the activity of the transcription factor E2F-1, thereby activating apoptosis pathways. Clinical trials exploiting this biology are under way, including a combination of gemcitabine and flavopiridol. We have also investigated the geldanamaycins, small-molecule inhibitors of hsp90, a cellular chaperone required for the proper folding of multiple kinases, including cdk4. We have demonstrated the depletion of cdk4 in lung cancer cell lines treated with geldanamycins, an effect that induces retinoblastoma-dependent G1 arrest. During the course of this work, we discovered that lung cancer cell lines harboring kinase domain mutations of epidermal growth factor receptor (EGFR) were the most sensitive to hsp90 inhibition, and we have defined mutant EGFR as a novel hsp90 client protein that is rapidly depleted following geldanamycin treatment. Hsp90 inhibition may represent a promising strategy for EGFR mutant lung cancers that have acquired resistance to standard tyrosine kinase inhibitors.Another active area of investigation is in regulation of Aurora kinases, mitotic kinases that are frequently dysregulated in cancer. We have shown that the Aurora kinase inhibitor VX-680 induces endoreduplication and eventual cell death in cancer cells. This effect is markedly enhanced in cells with a compromised p53-p21-dependent post-mitotic checkpoint. Transformed cells lacking the post-mitotic checkpoint are most likely to die in response to VX-680, while cells with intact checkpoint function are more likely to arrest. This work represents a first step toward defining tumors that are more likely to respond to Aurora kinase inhibition.
Research Departments
Support my researchPublications
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Single-stranded DNA Gap Accumulation is a Functional Biomarker for USP1 Inhibitor Sensitivity. Cancer Res. 2024 Jun 17. View in: Pubmed
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A phase 2 trial exploring the significance of homologous recombination status in patients with platinum sensitive or platinum resistant relapsed ovarian cancer receiving combination cediranib and olaparib. Gynecol Oncol. 2024 08; 187:105-112. View in: Pubmed
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Phase I/II Study of Combined BCL-xL and MEK Inhibition with Navitoclax and Trametinib in KRAS or NRAS Mutant Advanced Solid Tumors. Clin Cancer Res. 2024 May 01; 30(9):1739-1749. View in: Pubmed
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Selective CDK7 Inhibition Suppresses Cell Cycle Progression and MYC Signaling While Enhancing Apoptosis in Therapy-resistant Estrogen Receptor-positive Breast Cancer. Clin Cancer Res. 2024 May 01; 30(9):1889-1905. View in: Pubmed
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Randomized Phase II Study of Gemcitabine With or Without ATR Inhibitor Berzosertib in Platinum-Resistant Ovarian Cancer: Final Overall Survival and Biomarker Analyses. JCO Precis Oncol. 2024 Apr; 8:e2300635. View in: Pubmed
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Initial Chemotherapy for Locally Advanced and Metastatic NUT Carcinoma. J Thorac Oncol. 2024 May; 19(5):829-838. View in: Pubmed
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Novel BRD2::NUTM1 Fusion in NUT Carcinoma With Exceptional Response to Chemotherapy: A Case Report. JTO Clin Res Rep. 2024 Jan; 5(1):100625. View in: Pubmed
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A Phase I Expansion Cohort Study Evaluating the Safety and Efficacy of the CHK1 Inhibitor LY2880070 with Low-dose Gemcitabine in Patients with Metastatic Pancreatic Adenocarcinoma. Clin Cancer Res. 2023 12 15; 29(24):5047-5056. View in: Pubmed
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Retraction Note: Polymerase ? inhibition activates the cGAS-STING pathway and cooperates with immune checkpoint blockade in models of BRCA-deficient cancer. Nat Commun. 2023 Dec 11; 14(1):8193. View in: Pubmed
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The BRD4-NUT Fusion Alone Drives Malignant Transformation of NUT Carcinoma. Cancer Res. 2023 12 01; 83(23):3846-3860. View in: Pubmed
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EZH2 Cooperates with BRD4-NUT to Drive NUT Carcinoma Growth by Silencing Key Tumor Suppressor Genes. Cancer Res. 2023 12 01; 83(23):3956-3973. View in: Pubmed
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Oncogenic Drivers and Therapeutic Vulnerabilities in KRAS Wild-Type Pancreatic Cancer. Clin Cancer Res. 2023 11 14; 29(22):4627-4643. View in: Pubmed
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EZH2 synergizes with BRD4-NUT to drive NUT carcinoma growth through silencing of key tumor suppressor genes. bioRxiv. 2023 Aug 16. View in: Pubmed
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Clinicopathologic, Genomic, and Immunophenotypic Landscape of ATM Mutations in Non-Small Cell Lung Cancer. Clin Cancer Res. 2023 07 05; 29(13):2540-2550. View in: Pubmed
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Exceptional Response to Bromodomain and Extraterminal Domain Inhibitor Therapy With BMS-986158 in BRD4-NUTM1 NUT Carcinoma Harboring a BRD4 Splice Site Mutation. JCO Precis Oncol. 2023 06; 7:e2200633. View in: Pubmed
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Dose-escalation trial of combination dabrafenib, trametinib, and AT13387 in patients with BRAF-mutant solid tumors. Cancer. 2023 06 15; 129(12):1904-1918. View in: Pubmed
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Polymerase ? inhibition activates the cGAS-STING pathway and cooperates with immune checkpoint blockade in models of BRCA-deficient cancer. Nat Commun. 2023 03 13; 14(1):1390. View in: Pubmed
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MUC1-C Dictates PBRM1-Mediated Chronic Induction of Interferon Signaling, DNA Damage Resistance, and Immunosuppression in Triple-Negative Breast Cancer. Mol Cancer Res. 2023 03 01; 21(3):274-289. View in: Pubmed
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PD-1 blockade and CDK4/6 inhibition augment nonoverlapping features of T cell activation in cancer. J Exp Med. 2023 04 03; 220(4). View in: Pubmed
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Combining PARP Inhibition and Immunotherapy in BRCA-Associated Cancers. Cancer Treat Res. 2023; 186:207-221. View in: Pubmed
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Programmatic Precision Oncology Decision Support for Patients With Gastrointestinal Cancer. JCO Precis Oncol. 2023 01; 7:e2200342. View in: Pubmed
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Targeting DNA Repair with Combined Inhibition of NHEJ and MMEJ Induces Synthetic Lethality in TP53-Mutant Cancers. Cancer Res. 2022 10 17; 82(20):3815-3829. View in: Pubmed
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MatchMiner: an open-source platform for cancer precision medicine. NPJ Precis Oncol. 2022 Oct 06; 6(1):69. View in: Pubmed
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Targeting replication stress in cancer therapy. Nat Rev Drug Discov. 2023 01; 22(1):38-58. View in: Pubmed
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STING agonism enhances anti-tumor immune responses and therapeutic efficacy of PARP inhibition in BRCA-associated breast cancer. NPJ Breast Cancer. 2022 Sep 06; 8(1):102. View in: Pubmed
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Report of the First International Symposium on NUT Carcinoma. Clin Cancer Res. 2022 06 13; 28(12):2493-2505. View in: Pubmed
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A Phase I Study Investigating AZD8186, a Potent and Selective Inhibitor of PI3Kß/d, in Patients with Advanced Solid Tumors. Clin Cancer Res. 2022 06 01; 28(11):2257-2269. View in: Pubmed
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Targeting MUC1-C Suppresses Chronic Activation of Cytosolic Nucleotide Receptors and STING in Triple-Negative Breast Cancer. Cancers (Basel). 2022 May 24; 14(11). View in: Pubmed
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Phase 1b Clinical Trial with Alpelisib plus Olaparib for Patients with Advanced Triple-Negative Breast Cancer. Clin Cancer Res. 2022 04 14; 28(8):1493-1499. View in: Pubmed
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Microenvironment drives cell state, plasticity, and drug response in pancreatic cancer. Cell. 2021 12 09; 184(25):6119-6137.e26. View in: Pubmed
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Combined PARP and HSP90 inhibition: preclinical and Phase 1 evaluation in patients with advanced solid tumours. Br J Cancer. 2022 04; 126(7):1027-1036. View in: Pubmed
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Durable clinical benefit from PARP inhibition in a platinum-sensitive, BRCA2-mutated pancreatic cancer patient after earlier progression on placebo treatment on the POLO trial: a case report. J Gastrointest Oncol. 2021 Dec; 12(6):3133-3140. View in: Pubmed
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A Replication stress biomarker is associated with response to gemcitabine versus combined gemcitabine and ATR inhibitor therapy in ovarian cancer. Nat Commun. 2021 09 22; 12(1):5574. View in: Pubmed
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Opportunities for Utilization of DNA Repair Inhibitors in Homologous Recombination Repair-Deficient and Proficient Pancreatic Adenocarcinoma. Clin Cancer Res. 2021 12 15; 27(24):6622-6637. View in: Pubmed
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A first-in-class Polymerase Theta Inhibitor selectively targets Homologous-Recombination-Deficient Tumors. Nat Cancer. 2021 06; 2(6):598-610. View in: Pubmed
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Phase 1 Combination Study of the CHK1 Inhibitor Prexasertib and the PARP Inhibitor Olaparib in High-grade Serous Ovarian Cancer and Other Solid Tumors. Clin Cancer Res. 2021 09 01; 27(17):4710-4716. View in: Pubmed
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Phase 1 study of the ATR inhibitor berzosertib in combination with cisplatin in patients with advanced solid tumours. Br J Cancer. 2021 08; 125(4):520-527. View in: Pubmed
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FGFR2 Extracellular Domain In-Frame Deletions Are Therapeutically Targetable Genomic Alterations That Function as Oncogenic Drivers in Cholangiocarcinoma. Cancer Discov. 2021 10; 11(10):2488-2505. View in: Pubmed
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EZH2 inhibition activates a dsRNA-STING-interferon stress axis that potentiates response to PD-1 checkpoint blockade in prostate cancer. Nat Cancer. 2021 04; 2(4):444-456. View in: Pubmed
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Immune modulating activity of the CHK1 inhibitor prexasertib and anti-PD-L1 antibody LY3300054 in patients with high-grade serous ovarian cancer and other solid tumors. Cancer Immunol Immunother. 2021 Oct; 70(10):2991-3000. View in: Pubmed
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Phase II Clinical Trial of Everolimus in a Pan-Cancer Cohort of Patients with mTOR Pathway Alterations. Clin Cancer Res. 2021 07 15; 27(14):3845-3853. View in: Pubmed
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MMB-FOXM1-driven premature mitosis is required for CHK1 inhibitor sensitivity. Cell Rep. 2021 03 02; 34(9):108808. View in: Pubmed
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Pharmacokinetics and Safety of PTC596, a Novel Tubulin-Binding Agent, in Subjects With Advanced Solid Tumors. Clin Pharmacol Drug Dev. 2021 08; 10(8):940-949. View in: Pubmed
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Molecular Characterization and Therapeutic Targeting of Colorectal Cancers Harboring Receptor Tyrosine Kinase Fusions. Clin Cancer Res. 2021 03 15; 27(6):1695-1705. View in: Pubmed
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Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer. Nat Cancer. 2021 01; 2(1):66-82. View in: Pubmed
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A Phase 1 study of RO6870810, a novel bromodomain and extra-terminal protein inhibitor, in patients with NUT carcinoma, other solid tumours, or diffuse large B-cell lymphoma. Br J Cancer. 2021 02; 124(4):744-753. View in: Pubmed
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Clinical Efficacy and Molecular Response Correlates of the WEE1 Inhibitor Adavosertib Combined with Cisplatin in Patients with Metastatic Triple-Negative Breast Cancer. Clin Cancer Res. 2021 02 15; 27(4):983-991. View in: Pubmed
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CHK1 Inhibitor Blocks Phosphorylation of FAM122A and Promotes Replication Stress. Mol Cell. 2020 11 05; 80(3):410-422.e6. View in: Pubmed
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Phase 1 study of the HSP90 inhibitor onalespib in combination with AT7519, a pan-CDK inhibitor, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2020 12; 86(6):815-827. View in: Pubmed
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KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors. N Engl J Med. 2020 09 24; 383(13):1207-1217. View in: Pubmed
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A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors. Invest New Drugs. 2021 02; 39(1):163-174. View in: Pubmed
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A Phase I Study of DLYE5953A, an Anti-LY6E Antibody Covalently Linked to Monomethyl Auristatin E, in Patients with Refractory Solid Tumors. Clin Cancer Res. 2020 11 01; 26(21):5588-5597. View in: Pubmed
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Berzosertib plus gemcitabine versus gemcitabine alone in platinum-resistant high-grade serous ovarian cancer: a multicentre, open-label, randomised, phase 2 trial. Lancet Oncol. 2020 07; 21(7):957-968. View in: Pubmed
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A Phase Ib Study to Evaluate the MEK Inhibitor Cobimetinib in Combination with the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors. Oncologist. 2020 10; 25(10):833-e1438. View in: Pubmed
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Biomarker-Guided Development of DNA Repair Inhibitors. Mol Cell. 2020 06 18; 78(6):1070-1085. View in: Pubmed
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Author Correction: Immunogenomic profiling determines responses to combined PARP and PD-1 inhibition in ovarian cancer. Nat Commun. 2020 05 18; 11(1):2543. View in: Pubmed
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Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734. Mol Cancer Ther. 2020 07; 19(7):1406-1414. View in: Pubmed
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Impact of DNA Damage Response and Repair (DDR) Gene Mutations on Efficacy of PD-(L)1 Immune Checkpoint Inhibition in Non-Small Cell Lung Cancer. Clin Cancer Res. 2020 08 01; 26(15):4135-4142. View in: Pubmed
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Immunogenomic profiling determines responses to combined PARP and PD-1 inhibition in ovarian cancer. Nat Commun. 2020 03 19; 11(1):1459. View in: Pubmed
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A phase 1 study evaluating safety and pharmacokinetics of losatuxizumab vedotin (ABBV-221), an anti-EGFR antibody-drug conjugate carrying monomethyl auristatin E, in patients with solid tumors likely to overexpress EGFR. Invest New Drugs. 2020 10; 38(5):1483-1494. View in: Pubmed
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Reversion and non-reversion mechanisms of resistance to PARP inhibitor or platinum chemotherapy in BRCA1/2-mutant metastatic breast cancer. Ann Oncol. 2020 05; 31(5):590-598. View in: Pubmed
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Cooperation of the ATM and Fanconi Anemia/BRCA Pathways in Double-Strand Break End Resection. Cell Rep. 2020 02 18; 30(7):2402-2415.e5. View in: Pubmed
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Crizotinib in ROS1-rearranged advanced non-small-cell lung cancer (NSCLC): updated results, including overall survival, from PROFILE 1001. Ann Oncol. 2019 Jul; 30(7):1121-1126. View in: Pubmed
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Dose-escalation trial of the ALK, MET & ROS1 inhibitor, crizotinib, in patients with advanced cancer. Future Oncol. 2020 Jan; 16(1):4289-4301. View in: Pubmed
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An Anatomical Site and Genetic-Based Prognostic Model for Patients With Nuclear Protein in Testis (NUT) Midline Carcinoma: Analysis of 124 Patients. JNCI Cancer Spectr. 2020 Apr; 4(2):pkz094. View in: Pubmed
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A Phase I Study of LY3009120, a Pan-RAF Inhibitor, in Patients with Advanced or Metastatic Cancer. Mol Cancer Ther. 2020 02; 19(2):460-467. View in: Pubmed
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Functional profiling of nucleotide Excision repair in breast cancer. DNA Repair (Amst). 2019 10; 82:102697. View in: Pubmed
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The CHK1 Inhibitor Prexasertib Exhibits Monotherapy Activity in High-Grade Serous Ovarian Cancer Models and Sensitizes to PARP Inhibition. Clin Cancer Res. 2019 10 15; 25(20):6127-6140. View in: Pubmed
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Crizotinib in ROS1-rearranged advanced non-small-cell lung cancer (NSCLC): updated results, including overall survival, from PROFILE 1001. Ann Oncol. 2019 07 01; 30(7):1121-1126. View in: Pubmed
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Phase Ib study of the MEK inhibitor cobimetinib (GDC-0973) in combination with the PI3K inhibitor pictilisib (GDC-0941) in patients with advanced solid tumors. Invest New Drugs. 2020 04; 38(2):419-432. View in: Pubmed
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PARP Inhibitor Efficacy Depends on CD8+ T-cell Recruitment via Intratumoral STING Pathway Activation in BRCA-Deficient Models of Triple-Negative Breast Cancer. Cancer Discov. 2019 06; 9(6):722-737. View in: Pubmed
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Crizotinib in advanced ROS1-rearranged non-small cell lung cancer (NSCLC): Overall survival (OS) and updated safety from PROFILE 1001. Ann Oncol. 2019 Apr; 30 Suppl 2:ii48-ii49. View in: Pubmed
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Olaparib and a-specific PI3K inhibitor alpelisib for patients with epithelial ovarian cancer: a dose-escalation and dose-expansion phase 1b trial. Lancet Oncol. 2019 04; 20(4):570-580. View in: Pubmed
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MicroRNA-Mediated Suppression of the TGF-ß Pathway Confers Transmissible and Reversible CDK4/6 Inhibitor Resistance. Cell Rep. 2019 03 05; 26(10):2667-2680.e7. View in: Pubmed
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Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13. Elife. 2018 11 13; 7. View in: Pubmed
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Prediction of DNA Repair Inhibitor Response in Short-Term Patient-Derived Ovarian Cancer Organoids. Cancer Discov. 2018 11; 8(11):1404-1421. View in: Pubmed
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Palbociclib resistance confers dependence on an FGFR-MAP kinase-mTOR-driven pathway in KRAS-mutant non-small cell lung cancer. Oncotarget. 2018 Aug 03; 9(60):31572-31589. View in: Pubmed
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Real-time Genomic Characterization of Advanced Pancreatic Cancer to Enable Precision Medicine. Cancer Discov. 2018 09; 8(9):1096-1111. View in: Pubmed
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Pharmacokinetic Study of Rucaparib in Patients With Advanced Solid Tumors. Clin Pharmacol Drug Dev. 2019 01; 8(1):107-118. View in: Pubmed
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RAS-MAPK Reactivation Facilitates Acquired Resistance in FGFR1-Amplified Lung Cancer and Underlies a Rationale for Upfront FGFR-MEK Blockade. Mol Cancer Ther. 2018 07; 17(7):1526-1539. View in: Pubmed
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Cabozantinib in Patients with Advanced Merkel Cell Carcinoma. Oncologist. 2018 07; 23(7):814-821. View in: Pubmed
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First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study. Cancer Discov. 2018 02; 8(2):184-195. View in: Pubmed
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Genomic Biomarkers Predicting Response to Selective CDK4/6 Inhibition: Progress in an Elusive Search. Cancer Cell. 2017 12 11; 32(6):721-723. View in: Pubmed
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CDK4/6 Inhibition Augments Antitumor Immunity by Enhancing T-cell Activation. Cancer Discov. 2018 02; 8(2):216-233. View in: Pubmed
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Synergy of WEE1 and mTOR Inhibition in Mutant KRAS-Driven Lung Cancers. Clin Cancer Res. 2017 Nov 15; 23(22):6993-7005. View in: Pubmed
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Immunotherapy with single agent nivolumab for advanced leiomyosarcoma of the uterus: Results of a phase 2 study. Cancer. 2017 Sep 01; 123(17):3285-3290. View in: Pubmed
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The evolving role of cyclin-dependent kinase inhibitors in cancer management. Clin Adv Hematol Oncol. 2017 Mar; 15(3):174-177. View in: Pubmed
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A phase 1 study of the pharmacokinetics of nucleoside analog trifluridine and thymidine phosphorylase inhibitor tipiracil (components of TAS-102) vs trifluridine alone. Invest New Drugs. 2017 04; 35(2):189-197. View in: Pubmed
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First-in-human trial of an anti-5T4 antibody-monomethylauristatin conjugate, PF-06263507, in patients with advanced solid tumors. Invest New Drugs. 2017 06; 35(3):315-323. View in: Pubmed
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CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer. Cell Rep. 2016 11 22; 17(9):2367-2381. View in: Pubmed
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Evaluation of BGJ398, a Fibroblast Growth Factor Receptor 1-3 Kinase Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in Fibroblast Growth Factor Receptors: Results of a Global Phase I, Dose-Escalation and Dose-Expansion Study. J Clin Oncol. 2017 Jan 10; 35(2):157-165. View in: Pubmed
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Institutional implementation of clinical tumor profiling on an unselected cancer population. JCI Insight. 2016 11 17; 1(19):e87062. View in: Pubmed
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A phase 1 study combining the HER3 antibody seribantumab (MM-121) and cetuximab with and without irinotecan. Invest New Drugs. 2017 02; 35(1):68-78. View in: Pubmed
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Phase I Study Evaluating WEE1 Inhibitor AZD1775 As Monotherapy and in Combination With Gemcitabine, Cisplatin, or Carboplatin in Patients With Advanced Solid Tumors. J Clin Oncol. 2016 12 20; 34(36):4371-4380. View in: Pubmed
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Cabozantinib for metastatic breast carcinoma: results of a phase II placebo-controlled randomized discontinuation study. Breast Cancer Res Treat. 2016 11; 160(2):305-312. View in: Pubmed
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Clinical Development of the CDK4/6 Inhibitors Ribociclib and Abemaciclib in Breast Cancer. Breast Care (Basel). 2016 Jun; 11(3):167-73. View in: Pubmed
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Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-Small Cell Lung Cancer, and Other Solid Tumors. Cancer Discov. 2016 07; 6(7):740-53. View in: Pubmed
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The BRCA1-?11q Alternative Splice Isoform Bypasses Germline Mutations and Promotes Therapeutic Resistance to PARP Inhibition and Cisplatin. Cancer Res. 2016 05 01; 76(9):2778-90. View in: Pubmed
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Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor Veliparib (ABT-888) in Combination with Irinotecan in Patients with Advanced Solid Tumors. Clin Cancer Res. 2016 07 01; 22(13):3227-37. View in: Pubmed
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ASP9853, an inhibitor of inducible nitric oxide synthase dimerization, in combination with docetaxel: preclinical investigation and a Phase I study in advanced solid tumors. Cancer Chemother Pharmacol. 2016 Mar; 77(3):549-58. View in: Pubmed
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Incorporation of Next-Generation Sequencing into Routine Clinical Care to Direct Treatment of Head and Neck Squamous Cell Carcinoma. Clin Cancer Res. 2016 06 15; 22(12):2939-49. View in: Pubmed
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Targeting CDK4 and CDK6: From Discovery to Therapy. Cancer Discov. 2016 Apr; 6(4):353-67. View in: Pubmed
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Erratum to: A Phase 1 dose-escalation study of the safety and pharmacokinetics of once-daily oral foretinib, a multi-kinase inhibitor, in patients with solid tumors. Invest New Drugs. 2015 Dec; 33(6):1292. View in: Pubmed
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Homologous Recombination Deficiency: Exploiting the Fundamental Vulnerability of Ovarian Cancer. Cancer Discov. 2015 Nov; 5(11):1137-54. View in: Pubmed
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Phase I Study of the Investigational NEDD8-Activating Enzyme Inhibitor Pevonedistat (TAK-924/MLN4924) in Patients with Advanced Solid Tumors. Clin Cancer Res. 2016 Feb 15; 22(4):847-57. View in: Pubmed
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A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors. Invest New Drugs. 2015 10; 33(5):1100-7. View in: Pubmed
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Intratumoral Heterogeneity in EGFR-Mutant NSCLC Results in Divergent Resistance Mechanisms in Response to EGFR Tyrosine Kinase Inhibition. Cancer Res. 2015 Oct 15; 75(20):4372-83. View in: Pubmed
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Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor. N Engl J Med. 2015 Jul 30; 373(5):428-37. View in: Pubmed
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Phase II study of tivantinib (ARQ 197) in patients with metastatic triple-negative breast cancer. Invest New Drugs. 2015 Oct; 33(5):1108-14. View in: Pubmed
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A phase 1 study of ABT-806 in subjects with advanced solid tumors. Invest New Drugs. 2015 Jun; 33(3):671-8. View in: Pubmed
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First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 04 15; 21(8):1888-95. View in: Pubmed
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Cutaneous keratoacanthomas/squamous cell carcinomas associated with neutralization of transforming growth factor ß by the monoclonal antibody fresolimumab (GC1008). Cancer Immunol Immunother. 2015 Apr; 64(4):437-46. View in: Pubmed
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DNA-PK-A candidate driver of hepatocarcinogenesis and tissue biomarker that predicts response to treatment and survival. Clin Cancer Res. 2015 Feb 15; 21(4):925-33. View in: Pubmed
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The biology and clinical development of MEK inhibitors for cancer. Drugs. 2014 Dec; 74(18):2111-28. View in: Pubmed
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First-in-human phase I dose escalation study of a second-generation non-ansamycin HSP90 inhibitor, AT13387, in patients with advanced solid tumors. Clin Cancer Res. 2015 Jan 01; 21(1):87-97. View in: Pubmed
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Crizotinib in ROS1-rearranged non-small-cell lung cancer. N Engl J Med. 2014 Nov 20; 371(21):1963-71. View in: Pubmed
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A Phase I, dose-finding study in patients with advanced solid malignancies of the oral ?-secretase inhibitor PF-03084014. Clin Cancer Res. 2015 Jan 01; 21(1):60-7. View in: Pubmed
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Evaluation of statistical designs in phase I expansion cohorts: the Dana-Farber/Harvard Cancer Center experience. J Natl Cancer Inst. 2014 Jul; 106(7). View in: Pubmed
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A phase I clinical trial of navitoclax, a targeted high-affinity Bcl-2 family inhibitor, in combination with gemcitabine in patients with solid tumors. Invest New Drugs. 2014 Oct; 32(5):937-45. View in: Pubmed
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Activating mTOR mutations in a patient with an extraordinary response on a phase I trial of everolimus and pazopanib. Cancer Discov. 2014 May; 4(5):546-53. View in: Pubmed
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Phase I study of GC1008 (fresolimumab): a human anti-transforming growth factor-beta (TGFß) monoclonal antibody in patients with advanced malignant melanoma or renal cell carcinoma. PLoS One. 2014; 9(3):e90353. View in: Pubmed
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Crizotinib as salvage and maintenance with allogeneic stem cell transplantation for refractory anaplastic large cell lymphoma. J Natl Compr Canc Netw. 2014 Mar 01; 12(3):323-6; quiz 326. View in: Pubmed
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Phase I safety and pharmacokinetic study of the PI3K/mTOR inhibitor SAR245409 (XL765) in combination with erlotinib in patients with advanced solid tumors. J Thorac Oncol. 2014 Mar; 9(3):316-23. View in: Pubmed
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Co-clinical trials demonstrate superiority of crizotinib to chemotherapy in ALK-rearranged non-small cell lung cancer and predict strategies to overcome resistance. Clin Cancer Res. 2014 Mar 01; 20(5):1204-1211. View in: Pubmed
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Phase I study of neratinib in combination with temsirolimus in patients with human epidermal growth factor receptor 2-dependent and other solid tumors. J Clin Oncol. 2014 Jan 10; 32(2):68-75. View in: Pubmed
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A phase 1 open-label, sequential dose-escalation study investigating the safety, tolerability, and pharmacokinetics of intravenous TLC388 administered to patients with advanced solid tumors. Invest New Drugs. 2014 Jun; 32(3):445-51. View in: Pubmed
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Preclinical activity profile and therapeutic efficacy of the HSP90 inhibitor ganetespib in triple-negative breast cancer. Clin Cancer Res. 2014 Jan 15; 20(2):413-24. View in: Pubmed
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Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2014 Jan 01; 20(1):233-45. View in: Pubmed
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NUT midline carcinoma: an aggressive intrathoracic neoplasm. J Thorac Oncol. 2013 Oct; 8(10):1335-8. View in: Pubmed
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Stabilization of mutant BRCA1 protein confers PARP inhibitor and platinum resistance. Proc Natl Acad Sci U S A. 2013 Oct 15; 110(42):17041-6. View in: Pubmed
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Activation of the PD-1 pathway contributes to immune escape in EGFR-driven lung tumors. Cancer Discov. 2013 Dec; 3(12):1355-63. View in: Pubmed
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Aurora kinase inhibition as an anticancer strategy. J Clin Oncol. 2014 Jan 01; 32(1):57-9. View in: Pubmed
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Phase 2 trial of afatinib, an ErbB family blocker, in solid tumors genetically screened for target activation. Cancer. 2013 Aug 15; 119(16):3043-51. View in: Pubmed
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First-in-human phase I dose-escalation study of the HSP90 inhibitor AUY922 in patients with advanced solid tumors. Clin Cancer Res. 2013 Jul 01; 19(13):3671-80. View in: Pubmed
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Poly(ADP-ribose) polymerase inhibitors as cancer therapy. Front Biosci (Landmark Ed). 2013 06 01; 18(4):1392-406. View in: Pubmed
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A multicenter phase II study of ganetespib monotherapy in patients with genotypically defined advanced non-small cell lung cancer. Clin Cancer Res. 2013 Jun 01; 19(11):3068-77. View in: Pubmed
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A phase I trial of vorinostat and alvocidib in patients with relapsed, refractory, or poor prognosis acute leukemia, or refractory anemia with excess blasts-2. Clin Cancer Res. 2013 Apr 01; 19(7):1873-83. View in: Pubmed
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Sunitinib in combination with gemcitabine for advanced solid tumours: a phase I dose-finding study. Br J Cancer. 2013 Apr 16; 108(7):1393-401. View in: Pubmed
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Phase I dose-escalation study of afatinib, an ErbB family blocker, plus docetaxel in patients with advanced cancer. Future Oncol. 2013 Feb; 9(2):271-81. View in: Pubmed
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First-in-humans trial of an RNA interference therapeutic targeting VEGF and KSP in cancer patients with liver involvement. Cancer Discov. 2013 Apr; 3(4):406-17. View in: Pubmed
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Effect of aprepitant on the pharmacokinetics of the cyclin-dependent kinase inhibitor dinaciclib in patients with advanced malignancies. Cancer Chemother Pharmacol. 2012 Dec; 70(6):891-8. View in: Pubmed
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A Phase 1 dose-escalation study of the safety and pharmacokinetics of once-daily oral foretinib, a multi-kinase inhibitor, in patients with solid tumors. Invest New Drugs. 2013 Jun; 31(3):742-50. View in: Pubmed
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Cyclin-dependent kinase 4/6 inhibition in cancer therapy. Cell Cycle. 2012 Nov 01; 11(21):3913. View in: Pubmed
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Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study. Lancet Oncol. 2012 Oct; 13(10):1011-9. View in: Pubmed
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Ganetespib (STA-9090), a nongeldanamycin HSP90 inhibitor, has potent antitumor activity in in vitro and in vivo models of non-small cell lung cancer. Clin Cancer Res. 2012 Sep 15; 18(18):4973-85. View in: Pubmed
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Phase II trial of the histone deacetylase inhibitor romidepsin in patients with recurrent/metastatic head and neck cancer. Oral Oncol. 2012 Dec; 48(12):1281-8. View in: Pubmed
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BCL2 suppresses PARP1 function and nonapoptotic cell death. Cancer Res. 2012 Aug 15; 72(16):4193-203. View in: Pubmed
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Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients with advanced solid tumors. Invest New Drugs. 2013 Apr; 31(2):370-80. View in: Pubmed
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A phase I first-in-human trial of bardoxolone methyl in patients with advanced solid tumors and lymphomas. Clin Cancer Res. 2012 Jun 15; 18(12):3396-406. View in: Pubmed
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Suppression of heat shock protein 27 induces long-term dormancy in human breast cancer. Proc Natl Acad Sci U S A. 2012 May 29; 109(22):8699-704. View in: Pubmed
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Combined EGFR/MET or EGFR/HSP90 inhibition is effective in the treatment of lung cancers codriven by mutant EGFR containing T790M and MET. Cancer Res. 2012 Jul 01; 72(13):3302-11. View in: Pubmed
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Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors. J Clin Oncol. 2012 Jul 01; 30(19):2348-53. View in: Pubmed
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Phase II study of single-agent navitoclax (ABT-263) and biomarker correlates in patients with relapsed small cell lung cancer. Clin Cancer Res. 2012 Jun 01; 18(11):3163-9. View in: Pubmed
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Personalized tumor response assessment in the era of molecular medicine: cancer-specific and therapy-specific response criteria to complement pitfalls of RECIST. AJR Am J Roentgenol. 2012 Apr; 198(4):737-45. View in: Pubmed
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Selective CDK4/6 inhibition with tumor responses by PD0332991 in patients with mantle cell lymphoma. Blood. 2012 May 17; 119(20):4597-607. View in: Pubmed
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Chemotherapy-induced p53-dependent and -independent DNA damage responses are enhanced by poly(ADP-ribose) polymerase (PARP) inhibition in BRCA-proficient cancer cells. Cell Cycle. 2012 Feb 01; 11(3):432-3. View in: Pubmed
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The effect of food on the bioavailability of panobinostat, an orally active pan-histone deacetylase inhibitor, in patients with advanced cancer. Cancer Chemother Pharmacol. 2012 Feb; 69(2):555-62. View in: Pubmed
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Effect of crizotinib on overall survival in patients with advanced non-small-cell lung cancer harbouring ALK gene rearrangement: a retrospective analysis. Lancet Oncol. 2011 Oct; 12(11):1004-12. View in: Pubmed
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Compromised CDK1 activity sensitizes BRCA-proficient cancers to PARP inhibition. Nat Med. 2011 Jun 26; 17(7):875-82. View in: Pubmed
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Lack of food effect on single-dose pharmacokinetics of brivanib, and safety and efficacy following multiple doses in subjects with advanced or metastatic solid tumors. Cancer Chemother Pharmacol. 2011 Dec; 68(6):1377-85. View in: Pubmed
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Dependence on the MUC1-C oncoprotein in non-small cell lung cancer cells. Mol Cancer Ther. 2011 May; 10(5):806-16. View in: Pubmed
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Phase II multicenter trial of voreloxin as second-line therapy in chemotherapy-sensitive or refractory small cell lung cancer. J Thorac Oncol. 2011 Feb; 6(2):384-6. View in: Pubmed
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Phase I study of Navitoclax (ABT-263), a novel Bcl-2 family inhibitor, in patients with small-cell lung cancer and other solid tumors. J Clin Oncol. 2011 Mar 01; 29(7):909-16. View in: Pubmed
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Phase I studies of CBP501, a G2 checkpoint abrogator, as monotherapy and in combination with cisplatin in patients with advanced solid tumors. Clin Cancer Res. 2011 May 15; 17(10):3431-42. View in: Pubmed
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Combination mTOR and IGF-1R inhibition: phase I trial of everolimus and figitumumab in patients with advanced sarcomas and other solid tumors. Clin Cancer Res. 2011 Feb 15; 17(4):871-9. View in: Pubmed
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Phase I safety, pharmacokinetic, and pharmacodynamic study of ENMD-2076, a novel angiogenic and Aurora kinase inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2011 Feb 15; 17(4):849-60. View in: Pubmed
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Crizotinib, a small-molecule dual inhibitor of the c-Met and ALK receptor tyrosine kinases. Curr Opin Investig Drugs. 2010 Dec; 11(12):1477-90. View in: Pubmed
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Cyclin-dependent kinases (cdks) and the DNA damage response: rationale for cdk inhibitor-chemotherapy combinations as an anticancer strategy for solid tumors. Expert Opin Ther Targets. 2010 Nov; 14(11):1199-212. View in: Pubmed
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The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Res. 2010 Dec 15; 70(24):10038-43. View in: Pubmed
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Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med. 2010 Oct 28; 363(18):1693-703. View in: Pubmed
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Crizotinib in ALK-rearranged inflammatory myofibroblastic tumor. N Engl J Med. 2010 Oct 28; 363(18):1727-33. View in: Pubmed
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Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Res. 2010 Dec 01; 70(23):9827-36. View in: Pubmed
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Integrative genomic and proteomic analyses identify targets for Lkb1-deficient metastatic lung tumors. Cancer Cell. 2010 Jun 15; 17(6):547-59. View in: Pubmed
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Pattern of retinoblastoma pathway inactivation dictates response to CDK4/6 inhibition in GBM. Proc Natl Acad Sci U S A. 2010 Jun 22; 107(25):11501-6. View in: Pubmed
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A phase I open-label study evaluating the cardiovascular safety of sorafenib in patients with advanced cancer. Cancer Chemother Pharmacol. 2011 Apr; 67(4):751-64. View in: Pubmed
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A phase I study of foretinib, a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2. Clin Cancer Res. 2010 Jul 01; 16(13):3507-16. View in: Pubmed
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Development of phosphoinositide-3 kinase pathway inhibitors for advanced cancer. Curr Oncol Rep. 2010 Mar; 12(2):87-94. View in: Pubmed
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Phase I study of the c-raf-1 antisense oligonucleotide ISIS 5132 in combination with carboplatin and paclitaxel in patients with previously untreated, advanced non-small cell lung cancer. J Thorac Oncol. 2009 Sep; 4(9):1156-62. View in: Pubmed
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Cdk1 participates in BRCA1-dependent S phase checkpoint control in response to DNA damage. Mol Cell. 2009 Aug 14; 35(3):327-39. View in: Pubmed
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A phase I dose escalation study of AUY922, a novel HSP90 inhibitor, in patients with advanced solid malignancies. J Clin Oncol. 2009 May 20; 27(15_suppl):3532. View in: Pubmed
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Clinical activity observed in a phase I dose escalation trial of an oral c-met and ALK inhibitor, PF-02341066. J Clin Oncol. 2009 May 20; 27(15_suppl):3509. View in: Pubmed
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A phase I and pharmacological study of MK-1775, a Wee1 tyrosine kinase inhibitor, in both monotherapy and in combination with gemcitabine, cisplatin, or carboplatin in patients with advanced solid tumors. J Clin Oncol. 2009 May 20; 27(15_suppl):3510. View in: Pubmed
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Influence of food on the pharmacokinetics (PK) of panobinostat (LBH589), an orally active histone deacetylase inhibitor, in patients with advanced cancer. J Clin Oncol. 2009 May 20; 27(15_suppl):2550. View in: Pubmed
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Predicting drug susceptibility of non-small cell lung cancers based on genetic lesions. J Clin Invest. 2009 Jun; 119(6):1727-40. View in: Pubmed
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A phase I study with neratinib (HKI-272), an irreversible pan ErbB receptor tyrosine kinase inhibitor, in patients with solid tumors. Clin Cancer Res. 2009 Apr 01; 15(7):2552-8. View in: Pubmed
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HER2YVMA drives rapid development of adenosquamous lung tumors in mice that are sensitive to BIBW2992 and rapamycin combination therapy. Proc Natl Acad Sci U S A. 2009 Jan 13; 106(2):474-9. View in: Pubmed
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Early detection of erlotinib treatment response in NSCLC by 3'-deoxy-3'-[F]-fluoro-L-thymidine ([F]FLT) positron emission tomography (PET). PLoS One. 2008; 3(12):e3908. View in: Pubmed
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Hsp90 inhibition suppresses mutant EGFR-T790M signaling and overcomes kinase inhibitor resistance. Cancer Res. 2008 Jul 15; 68(14):5827-38. View in: Pubmed
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Heat shock protein 90 inhibition in lung cancer. J Thorac Oncol. 2008 Jun; 3(6 Suppl 2):S152-9. View in: Pubmed
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Summary statement novel agents in the treatment of lung cancer: Fifth Cambridge Conference assessing opportunities for combination therapy. J Thorac Oncol. 2008 Jun; 3(6 Suppl 2):S107-12. View in: Pubmed
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A phase I dose-escalation study of the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of the novel cyclin-dependent kinase inhibitor SCH 727965 administered every 3 weeks in subjects with advanced malignancies. J Clin Oncol. 2008 May 20; 26(15_suppl):3532. View in: Pubmed
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Phase I studies of CBP501, a novel G2 checkpoint abrogator, alone and combined with cisplatin (CDDP) in advanced solid tumor patients (pts). J Clin Oncol. 2008 May 20; 26(15_suppl):2528. View in: Pubmed
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A phase I dose-finding study of sunitinib (SU) in combination with gemcitabine (G) in patients (pts) with advanced solid tumors. J Clin Oncol. 2008 May 20; 26(15_suppl):14522. View in: Pubmed
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Phase I trial with a novel oral NF-?B/STAT3 inhibitor RTA 402 in patients with solid tumors and lymphoid malignancies. J Clin Oncol. 2008 May 20; 26(15_suppl):3517. View in: Pubmed
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Phase I/II study of GC1008: A human anti-transforming growth factor-beta (TGFß) monoclonal antibody (MAb) in patients with advanced malignant melanoma (MM) or renal cell carcinoma (RCC). J Clin Oncol. 2008 May 20; 26(15_suppl):9028. View in: Pubmed
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Phase I study of flavopiridol in combination with Paclitaxel and Carboplatin in patients with non-small-cell lung cancer. Clin Lung Cancer. 2008 May; 9(3):160-5. View in: Pubmed
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BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 07; 27(34):4702-11. View in: Pubmed
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PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res. 2007 Dec 15; 67(24):11924-32. View in: Pubmed
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Proapoptotic BH3-only BCL-2 family protein BIM connects death signaling from epidermal growth factor receptor inhibition to the mitochondrion. Cancer Res. 2007 Dec 15; 67(24):11867-75. View in: Pubmed
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Targeting aberrant PI3K pathway signaling with XL147, a potent, selective and orally bioavailable PI3K inhibitor [abstract]. Proc AACR-NCI-EORTC International Meeting on Molecular Targets and Cancer Therapeutics. 2007; A-C205. View in: Pubmed
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Phase I dose-escalation study of the safety, pharmacokinetics (PK) and pharmacodynamics of XL880,a VEGFRR and MET kinase inhibitor, administered daily to patients with advanced malignancies [abstract]. Proc AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics. 2007; A-B248. View in: Pubmed
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Phase I trial with a novel orally administered synthetic triperpenoid RTA 402 (CDDO-Me) in patients with solid tumors and lymphoid malignancies [abstract]. Proc AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics. 2007; A-B82. View in: Pubmed
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LKB1 modulates lung cancer differentiation and metastasis. Nature. 2007 Aug 16; 448(7155):807-10. View in: Pubmed
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Bronchial and peripheral murine lung carcinomas induced by T790M-L858R mutant EGFR respond to HKI-272 and rapamycin combination therapy. Cancer Cell. 2007 Jul; 12(1):81-93. View in: Pubmed
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The major lung cancer-derived mutants of ERBB2 are oncogenic and are associated with sensitivity to the irreversible EGFR/ERBB2 inhibitor HKI-272. Oncogene. 2007 Jul 26; 26(34):5023-7. View in: Pubmed
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Allele-dependent variation in the relative cellular potency of distinct EGFR inhibitors. Cancer Biol Ther. 2007 May; 6(5):661-7. View in: Pubmed
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Clinical and translational studies of depsipeptide, a histone deacetylase inhibitor, in patients with squamous cell carcinoma of the head and neck: New York Cancer Consortium Trial P6335 [abstract]. Proc Am Soc Clin Oncol. 2007; 25:A6065. View in: Pubmed
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Concomitant cdk1 and cdk2 depletion induces irreparable DNA damage, G2/M arrest and cell death [abstract]. Proc Am Assoc Cancer Res. 2007; 48:A4346. View in: Pubmed
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Direct and indirect modulation of EGFR-mediated growth signaling by Hsp90 inhibition in NSCLCs resistant to EGFR tyrosine kinase inhibitors in vitro and in vivo [abstract]. Proc Am Assoc Cancer Res. 2007; 48:A5237. View in: Pubmed
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Translational studies of depsipeptide, a histone deacetylase (HDAC) inhibitor in patients with head and neck cancer [abstract]. Proc Am Assoc Cancer Res. 2007; 48:A3524. View in: Pubmed
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Phase I experience with c-met inhibitor XL880 administered orally to patients with solid tumors [abstract]. Proc Am Soc Clin Oncol. 2007; 25:A3526. View in: Pubmed
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Entering a clinical trial: is it right for you?-a randomized study of the clinical trials video and its impact on the informed consent process [abstract]. Proc Am Soc Clin Oncol. 2007; 25:A9072. View in: Pubmed
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Retinoblastoma family member deficiency increases endoreduplication and apoptosis in response to the pan-Aurora kinase inhibitor VE-465 [abstract]. Proc Am Assoc Cancer Res. 2007; 48:A5394. View in: Pubmed
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Transcriptional profiling identifies cyclin D1 as a critical downstream effector of mutant epidermal growth factor receptor signaling. Cancer Res. 2006 Dec 01; 66(23):11389-98. View in: Pubmed
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Combined depletion of cell cycle and transcriptional cyclin-dependent kinase activities induces apoptosis in cancer cells. Cancer Res. 2006 Sep 15; 66(18):9270-80. View in: Pubmed
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The Aurora kinase inhibitor VX-680 induces endoreduplication and apoptosis preferentially in cells with compromised p53-dependent postmitotic checkpoint function. Cancer Res. 2006 Aug 01; 66(15):7668-77. View in: Pubmed
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Non-small-cell lung cancer and Ba/F3 transformed cells harboring the ERBB2 G776insV_G/C mutation are sensitive to the dual-specific epidermal growth factor receptor and ERBB2 inhibitor HKI-272. Cancer Res. 2006 Jul 01; 66(13):6487-91. View in: Pubmed
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A phase I clinical and pharmacokinetic (PK) trial of the aurora kinase (AK) inhibitor MK-0457 in cancer patients. J Clin Oncol. 2006 Jun 20; 24(18_suppl):3009. View in: Pubmed
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Pharmacokinetics of PT523, a novel aminopterin analogue, in patients with solid tumors. J Clin Oncol. 2006 Jun 20; 24(18_suppl):2052. View in: Pubmed
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The impact of human EGFR kinase domain mutations on lung tumorigenesis and in vivo sensitivity to EGFR-targeted therapies. Cancer Cell. 2006 Jun; 9(6):485-95. View in: Pubmed
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Epidermal growth factor receptor variant III mutations in lung tumorigenesis and sensitivity to tyrosine kinase inhibitors. Proc Natl Acad Sci U S A. 2006 May 16; 103(20):7817-22. View in: Pubmed
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Cyclin-dependent kinase pathways as targets for cancer treatment. J Clin Oncol. 2006 Apr 10; 24(11):1770-83. View in: Pubmed
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AZ703, an imidazo[1,2-a]pyridine inhibitor of cyclin-dependent kinases 1 and 2, induces E2F-1-dependent apoptosis enhanced by depletion of cyclin-dependent kinase 9. Cancer Res. 2006 Jan 01; 66(1):435-44. View in: Pubmed
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Multiple mechanisms of Mcl-1 depletion by the cyclin-dependent kinase inhibitor flavopiridol in mantle cell lymphoma cell lines [abstract]. Proc Am Assoc Cancer Res. 2006; 47:A2805. View in: Pubmed
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Phase 1 trial of ARQ501, a novel checkpoint pathway activator, in patients with advanced solid tumors [abstract]. Proc Am Assoc Cancer Res. 2006; 47:LB-12. View in: Pubmed
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CBP501, a novel cell cycle G2 checkpoint abrogator: preliminary results of the initial phase 1 and pharmacokinetic/pharmacodynamic study in patients with advanced solid tumors [abstract]. Eur J Cancer. 2006; 4:A346. View in: Pubmed
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A phase 1 clinical and pharmacokinetic trial of the aurora kinase (AK) inhibitor MK-0457 in cancer patients [abstract]. Proc Am Soc Clin Oncol. 2006; 24:A3009. View in: Pubmed
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A phase 1 dose escalation trial of ispinesib (SB-715992) administered days 1-3 of a 21-day cycle in patients with advanced solid tumors [abstract]. Proc Am Soc Clin Oncol. 2006; 24:A2026. View in: Pubmed
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A phase 1 study of a novel spectrum-selective kinase inhibitor (SSKI) XL880, administered orally in pajtients with advanced tumors [abstract]. Proc Am Soc Clin Oncol. 2006; 24:A3041. View in: Pubmed
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Pharmacokinetics of PT523, a novel aminopterin analogue in patients with solid tumors [abstract]. Proc Am Soc Clin Oncol. 2006; 24:A2052. View in: Pubmed
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Pharmacodynamics of XL880 a novel spectrum-selective kinase inhibitor (SSKI) administered orally to patients with advanced solid tumors [abstract]. Eur J Cancer. 2006; 4:A404. View in: Pubmed
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Epidermal growth factor receptors harboring kinase domain mutations associate with the heat shock protein 90 chaperone and are destabilized following exposure to geldanamycins. Cancer Res. 2005 Jul 15; 65(14):6401-8. View in: Pubmed
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Phase I trial of ARQ 501, an Activated Checkpoint Therapy (ACT) agent, in patients with advanced solid tumors. J Clin Oncol. 2005 Jun; 23(16_suppl):3042. View in: Pubmed
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Phase I trial of the matrix metalloproteinase inhibitor marimastat combined with carboplatin and paclitaxel in patients with advanced non-small cell lung cancer. Clin Cancer Res. 2005 May 01; 11(9):3417-24. View in: Pubmed
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Flavopiridol reduces malignant transformation of the esophageal mucosa in p27 knockout mice. Oncogene. 2005 Mar 03; 24(10):1683-8. View in: Pubmed
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Pharmacodynamic assessment of the cyclin-dependent kinase inhibitor flaopiridol: Modulation of cdk targets in clinical samples [abstract]. Lab Invest. 2005; 18(Supplement):1375. View in: Pubmed
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Phase 1 Trial of ARQ 501, an activated checkpoint therapy (trade mark ACT) agent, in patients with advanced solid tumors [abstract]. Proc Am Soc Clin Oncol. 2005; 23:A3042. View in: Pubmed
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A phase 1 study of E7070, a chloroindolyl-sulfonamide, in combination with irinotecan in gastrointestinal and thoracic carcinomas [abstract]. Am Soc Clin Oncol Gastrointestinal Cancers Symposium. 2005; A290. View in: Pubmed
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Pharmacodynamic assessment of the cyclin-dependent kinase inhibitor flavopiridol: Modualtion of cdk targets in clinical samples [abstract]. Modern Pathol. 2005; 18(Supplement):1375. View in: Pubmed
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A phase I study of E7070, a chloroindolyl-sulfonamide, in combination with irinotecan in gastrointestinal and thoracic carcinomas [abstract]. Proc Am Soc Clin Oncol. 2005; 23:A2031. View in: Pubmed
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A phase II clinical and pharmacodynamic study of E7070 in patients with metastatic, recurrent, or refractory squamous cell carcinoma of the head and neck: modulation of retinoblastoma protein phosphorylation by a novel chloroindolyl sulfonamide cell cycle inhibitor. Clin Cancer Res. 2004 Jul 15; 10(14):4680-7. View in: Pubmed
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Preclinical and clinical development of the cyclin-dependent kinase inhibitor flavopiridol. Clin Cancer Res. 2004 Jun 15; 10(12 Pt 2):4270s-4275s. View in: Pubmed
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Novel agents in the treatment of lung cancer: conference summary statement. Clin Cancer Res. 2004 Jun 15; 10(12 Pt 2):4199s-4204s. View in: Pubmed
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Bioluminescent imaging of Cdk2 inhibition in vivo. Nat Med. 2004 Jun; 10(6):643-8. View in: Pubmed
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The role of metastasis-associated protein 1 in prostate cancer progression. Cancer Res. 2004 Feb 01; 64(3):825-9. View in: Pubmed
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Selective sensitization of transformed cells to flavopiridol-induced apoptosis following recruitment to S-phase. Cancer Res. 2002 Mar 15; 62(6):1707-17. View in: Pubmed
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Modulation of the c-Met/hepatocyte growth factor pathway in small cell lung cancer. Clin Cancer Res. 2002 Feb; 8(2):620-7. View in: Pubmed
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A phase II study of weekly paclitaxel in elderly patients with advanced non-small cell lung cancer. Clin Cancer Res. 2001 Dec; 7(12):3942-9. View in: Pubmed
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A phase II trial of the cyclin-dependent kinase inhibitor flavopiridol in patients with previously untreated stage IV non-small cell lung cancer. Clin Cancer Res. 2001 Jun; 7(6):1590-9. View in: Pubmed
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The physiology of p16(INK4A)-mediated G1 proliferative arrest. Cell Biochem Biophys. 2000; 33(2):189-97. View in: Pubmed
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