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Publications
- A genome-wide RNAi screen identifies multiple synthetic lethal interactions with the Ras oncogene. Cell 2009, 137:835–848.
- Targeting the cyclin E-Cdk-2 complex represses lung cancer growth by triggering anaphase catastrophe. Clin. Cancer Res. 2010, 16:109-20.
- Discovery, biological characterization and oral antitumor activity of polo-like kinase 1 (Plk1) selective small molecule inhibitors. Proceedings of the 101st Annual Meeting AACR; 2010, Apr 17-21; Washington, DC, Abstract 4435.
- Cyclin E amplification/overexpression is a mechanism of trastuzumab resistance in HER2+ breast cancer patients. Proc Natl Acad Sci USA. 2011, 108:3761-3766.
- Potent and selective small molecule inhibitors of Polo-like kinase 1: Biological characterization. Proceedings of the 103rd Annual Meeting AACR; 2012, Mar 31-Apr 4; Chicago, Illinois. Philadelphia, PA: AACR; 2012. Abstract 2814.
- Parameters improving the therapeutic window of Compound 4, a potent and selective Polo-like kinase 1 inhibitor: in vitro studies. National Cancer Research Institute (NCRI) Cancer Conference 2012, Nov 4-7; Liverpool, UK. NCRI; Nov 2012. Abstract B15.
- CYC065, potential therapeutic agent for AML and MLL leukaemia. Proceedings of the Annual Meeting of the Society of Hematologic Oncology (SOHO), 2014, Huston, Texas (TX), Sept 17-20, Abstract 209.
- Cyclin E amplification predicts sensitivity of primary Uterine Serous Carcinoma (USC) cell lines to the cdk2 inhibitor CYC065. Proc. 106th Annual Meeting AACR, 2015, Apr 18-22; Philadelphia, PA, Abstract 3103.
- Molecular basis for clinical development in basal-like triple-negative breast cancer. Proceedings of the 38th Annual CTRC-AACR San Antonio Breast Cancer Symposium: 2015 Dec 8-12; San Antonio, TX. Philadelphia, PA: AACR; Cancer Res 2016;76 (4 Suppl): Abstract P5-03-10.
- CYC065, a novel CDK2/9 inhibitor, is an effective inducer of cell death and synergizes with BCL2 and BET inhibitors in B-cell lymphoma, including double-hit lymphomas. Proc. 107th Ann. Meeting AACR, 2016, Apr 16-20; New Orleans, LA, Abstract 1309.
- Dual CCNE1/PIK3CA targeting is synergistic in CCNE1-amplified/PIK3CA-mutated uterine serous carcinomas in vitro and in vivo. Br J Cancer 2016. 115:303-11.
- The small molecule CDK2 and CDK9 inhibitors CYC065 and CCT68127 are potent inhibitors of MYCN via transcriptional repression. Childhood Cancer Meeting 2016, Sept 5–7, London, UK, Abstract 1-19.
- Therapeutic potential of novel PLK1 inhibitor CYC140 in esophageal cancer and acute leukemia. 28th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics; 2016 Nov 29–Dec 2; Munich, Germany. Abstract 355.
- Next-Generation CDK2/9 Inhibitors and Anaphase Catastrophe in Lung Cancer. J Natl Cancer Inst. 2017, 109(6): djw297.
- Identification of pharmacodynamic markers, sensitive target indications and potential combinations. Proc. Ann. Meeting AACR, 2017, Apr 1-5; Washington, D.C., Abstract 4178.
- Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor
- Phase I safety, pharmacokinetic and pharmacodynamic study of CYC065, a cyclin-dependent kinase inhibitor, in patients with advanced cancers (NCT02552953). Proc. Ann. Meeting AACR, 2018, Apr 14-18; Chicago, IL, Abstract CT037.
- Strategic combination of the cyclin-dependent kinase inhibitor CYC065 with venetoclax to target anti-apoptotic proteins in chronic lymphocytic leukemia. Proc. Ann. Meeting AACR, 2018, Apr 14-18; Chicago, IL, Abstract 3905.
- Application of a MYC degradation screen identifies sensitivity to CDK9 inhibitors in KRAS-mutant pancreatic cancer. Science Signal. Jul 16, 2019, 12(590):eaav7259.
- Targeting the rheumatoid arthritis synovial fibroblast via cyclin dependent kinase inhibition: An early phase trial. Medicine 2020, 99:26.
- Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer. PLOS One, July 9, 2020; doi.org/10.1371/journal.pone.0234103.
- Cyclin E overexpression confers resistance to trastuzumab through noncanonical phosphorylation of SMAD3 in HER2+ breast cancer. Cancer Biol & Therapy 2020; https://doi.org/10.1080/15384047.2020.1818518.
- Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma. J Clin Invest 2020; https://doi.org/10.1172/JCI134132.
- Phase 1 safety, pharmacokinetic and pharmacodynamic study of fadraciclib (CYC065), a cyclin-dependent kinase inhibitor, in patients with advanced cancers (NCT02552953). An oral presentation delivered at the 32nd EORTC/AACR/NCI Virtual Symposium 24-25 Oct 2020.
- A Novel CDK2/9 Inhibitor CYC065 Causes Anaphase Catastrophe and Represses Proliferation, Tumorigenesis, and Metastasis in Aneuploid Cancers. Mol Cancer Ther. 2021, 20:477-489.
- Sensitivity of oncogenic KRAS-expressing cells to CDK9 inhibition. SLAS Discovery. April 24, 2021; doi.org/10.1177/24725552211008853.
- A precision medicine drug discovery pipeline identifies combined CDK2 and 9 inhibition as a novel therapeutic strategy in colorectal cancer. Mol Cancer Ther. 2020, 19: 2516-2527.
- A Phase 1/2, Open-label, Multi-center Study to Investigate the Safety, Pharmacokinetics, and Efficacy of Fadraciclib (CYC065), an Oral CDK2/9 Inhibitor, in Subjects with Advanced Solid Tumors and Lymphoma. A poster presentation at the 34th EORTC-NCI-AACR Symposium 26-28 Oct 2022, Abstract 50.