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Page 1
Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors.
Zhang T, Kwiatkowski N, Olson CM, Dixon-Clarke SE, Abraham BJ, Greifenberg AK, Ficarro SB, Elkins JM, Liang Y, Hannett NM, Manz T, Hao M, Bartkowiak B, Greenleaf AL, Marto JA, Geyer M, Bullock AN, Young RA, Gray NS. Zhang T, et al. Nat Chem Biol. 2016 Oct;12(10):876-84. doi: 10.1038/nchembio.2166. Epub 2016 Aug 29. Nat Chem Biol. 2016. PMID: 27571479 Free PMC article.
Targeting transcription regulation in cancer with a covalent CDK7 inhibitor.
Kwiatkowski N, Zhang T, Rahl PB, Abraham BJ, Reddy J, Ficarro SB, Dastur A, Amzallag A, Ramaswamy S, Tesar B, Jenkins CE, Hannett NM, McMillin D, Sanda T, Sim T, Kim ND, Look T, Mitsiades CS, Weng AP, Brown JR, Benes CH, Marto JA, Young RA, Gray NS. Kwiatkowski N, et al. Nature. 2014 Jul 31;511(7511):616-20. doi: 10.1038/nature13393. Epub 2014 Jun 22. Nature. 2014. PMID: 25043025 Free PMC article.
Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors.
Gao Y, Zhang T, Terai H, Ficarro SB, Kwiatkowski N, Hao MF, Sharma B, Christensen CL, Chipumuro E, Wong KK, Marto JA, Hammerman PS, Gray NS, George RE. Gao Y, et al. Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5. doi: 10.1016/j.chembiol.2017.11.007. Epub 2017 Dec 21. Cell Chem Biol. 2018. PMID: 29276047 Free PMC article.
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.
Jiang B, Jiang J, Kaltheuner IH, Iniguez AB, Anand K, Ferguson FM, Ficarro SB, Seong BKA, Greifenberg AK, Dust S, Kwiatkowski NP, Marto JA, Stegmaier K, Zhang T, Geyer M, Gray NS. Jiang B, et al. Eur J Med Chem. 2021 Oct 5;221:113481. doi: 10.1016/j.ejmech.2021.113481. Epub 2021 Apr 20. Eur J Med Chem. 2021. PMID: 33945934
12 results