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Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.
Freeman DB, Hopkins TD, Mikochik PJ, Vacca JP, Gao H, Naylor-Olsen A, Rudra S, Li H, Pop MS, Villagomez RA, Lee C, Li H, Zhou M, Saffran DC, Rioux N, Hood TR, Day MAL, McKeown MR, Lin CY, Bischofberger N, Trotter BW. Freeman DB, et al. Among authors: mikochik pj. J Med Chem. 2023 Dec 14;66(23):15629-15647. doi: 10.1021/acs.jmedchem.3c01233. Epub 2023 Nov 15. J Med Chem. 2023. PMID: 37967851 Free PMC article.
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.
Brodney MA, Beck EM, Butler CR, Barreiro G, Johnson EF, Riddell D, Parris K, Nolan CE, Fan Y, Atchison K, Gonzales C, Robshaw AE, Doran SD, Bundesmann MW, Buzon L, Dutra J, Henegar K, LaChapelle E, Hou X, Rogers BN, Pandit J, Lira R, Martinez-Alsina L, Mikochik P, Murray JC, Ogilvie K, Price L, Sakya SM, Yu A, Zhang Y, O'Neill BT. Brodney MA, et al. J Med Chem. 2015 Apr 9;58(7):3223-52. doi: 10.1021/acs.jmedchem.5b00191. Epub 2015 Apr 1. J Med Chem. 2015. PMID: 25781223 Free PMC article.
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors.
Richters A, Doyle SK, Freeman DB, Lee C, Leifer BS, Jagannathan S, Kabinger F, Koren JV, Struntz NB, Urgiles J, Stagg RA, Curtin BH, Chatterjee D, Mathea S, Mikochik PJ, Hopkins TD, Gao H, Branch JR, Xin H, Westover L, Bignan GC, Rupnow BA, Karlin KL, Olson CM, Westbrook TF, Vacca J, Wilfong CM, Trotter BW, Saffran DC, Bischofberger N, Knapp S, Russo JW, Hickson I, Bischoff JR, Gottardis MM, Balk SP, Lin CY, Pop MS, Koehler AN. Richters A, et al. Among authors: mikochik pj. Cell Chem Biol. 2021 Feb 18;28(2):134-147.e14. doi: 10.1016/j.chembiol.2020.10.001. Epub 2020 Oct 20. Cell Chem Biol. 2021. PMID: 33086052 Free article.