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CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation.
Krajewska M, Dries R, Grassetti AV, Dust S, Gao Y, Huang H, Sharma B, Day DS, Kwiatkowski N, Pomaville M, Dodd O, Chipumuro E, Zhang T, Greenleaf AL, Yuan GC, Gray NS, Young RA, Geyer M, Gerber SA, George RE. Krajewska M, et al. Among authors: geyer m. Nat Commun. 2019 Apr 15;10(1):1757. doi: 10.1038/s41467-019-09703-y. Nat Commun. 2019. PMID: 30988284 Free PMC article.
The structure and substrate specificity of human Cdk12/Cyclin K.
Bösken CA, Farnung L, Hintermair C, Merzel Schachter M, Vogel-Bachmayr K, Blazek D, Anand K, Fisher RP, Eick D, Geyer M. Bösken CA, et al. Among authors: geyer m. Nat Commun. 2014 Mar 24;5:3505. doi: 10.1038/ncomms4505. Nat Commun. 2014. PMID: 24662513 Free PMC article.
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. Among authors: geyer m. 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.
CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer.
Johnson SF, Cruz C, Greifenberg AK, Dust S, Stover DG, Chi D, Primack B, Cao S, Bernhardy AJ, Coulson R, Lazaro JB, Kochupurakkal B, Sun H, Unitt C, Moreau LA, Sarosiek KA, Scaltriti M, Juric D, Baselga J, Richardson AL, Rodig SJ, D'Andrea AD, Balmaña J, Johnson N, Geyer M, Serra V, Lim E, Shapiro GI. Johnson SF, et al. Among authors: geyer m. Cell Rep. 2016 Nov 22;17(9):2367-2381. doi: 10.1016/j.celrep.2016.10.077. Cell Rep. 2016. PMID: 27880910 Free PMC article.
Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype.
Olson CM, Liang Y, Leggett A, Park WD, Li L, Mills CE, Elsarrag SZ, Ficarro SB, Zhang T, Düster R, Geyer M, Sim T, Marto JA, Sorger PK, Westover KD, Lin CY, Kwiatkowski N, Gray NS. Olson CM, et al. Among authors: geyer m. Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10. doi: 10.1016/j.chembiol.2019.02.012. Epub 2019 Mar 21. Cell Chem Biol. 2019. PMID: 30905681 Free PMC article.
CDK13 cooperates with CDK12 to control global RNA polymerase II processivity.
Fan Z, Devlin JR, Hogg SJ, Doyle MA, Harrison PF, Todorovski I, Cluse LA, Knight DA, Sandow JJ, Gregory G, Fox A, Beilharz TH, Kwiatkowski N, Scott NE, Vidakovic AT, Kelly GP, Svejstrup JQ, Geyer M, Gray NS, Vervoort SJ, Johnstone RW. Fan Z, et al. Among authors: geyer m. Sci Adv. 2020 Apr 29;6(18):eaaz5041. doi: 10.1126/sciadv.aaz5041. Print 2020 May. Sci Adv. 2020. PMID: 32917631 Free PMC article.
Discovery and resistance mechanism of a selective CDK12 degrader.
Jiang B, Gao Y, Che J, Lu W, Kaltheuner IH, Dries R, Kalocsay M, Berberich MJ, Jiang J, You I, Kwiatkowski N, Riching KM, Daniels DL, Sorger PK, Geyer M, Zhang T, Gray NS. Jiang B, et al. Among authors: geyer m. Nat Chem Biol. 2021 Jun;17(6):675-683. doi: 10.1038/s41589-021-00765-y. Epub 2021 Mar 22. Nat Chem Biol. 2021. PMID: 33753926 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. Among authors: geyer m. 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
1,083 results