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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: greifenberg ak. 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.
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: greifenberg ak. 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
Structural and Functional Analysis of the Cdk13/Cyclin K Complex.
Greifenberg AK, Hönig D, Pilarova K, Düster R, Bartholomeeusen K, Bösken CA, Anand K, Blazek D, Geyer M. Greifenberg AK, et al. Cell Rep. 2016 Jan 12;14(2):320-31. doi: 10.1016/j.celrep.2015.12.025. Epub 2015 Dec 31. Cell Rep. 2016. PMID: 26748711 Free 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: greifenberg ak. 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.
Brd4 activates P-TEFb for RNA polymerase II CTD phosphorylation.
Itzen F, Greifenberg AK, Bösken CA, Geyer M. Itzen F, et al. Among authors: greifenberg ak. Nucleic Acids Res. 2014 Jul;42(12):7577-90. doi: 10.1093/nar/gku449. Epub 2014 May 23. Nucleic Acids Res. 2014. PMID: 24860166 Free PMC article.
MIR sequences recruit zinc finger protein ZNF768 to expressed genes.
Rohrmoser M, Kluge M, Yahia Y, Gruber-Eber A, Maqbool MA, Forné I, Krebs S, Blum H, Greifenberg AK, Geyer M, Descostes N, Imhof A, Andrau JC, Friedel CC, Eick D. Rohrmoser M, et al. Among authors: greifenberg ak. Nucleic Acids Res. 2019 Jan 25;47(2):700-715. doi: 10.1093/nar/gky1148. Nucleic Acids Res. 2019. PMID: 30476274 Free PMC article.