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From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors.
Koravovic M, Mayasundari A, Tasic G, Keramatnia F, Stachowski TR, Cui H, Chai SC, Jonchere B, Yang L, Li Y, Fu X, Hiltenbrand R, Paul L, Mishra V, Klco JM, Roussel MF, Pomerantz WC, Fischer M, Rankovic Z, Savic V. Koravovic M, et al. Among authors: chai sc. Eur J Med Chem. 2023 May 5;251:115246. doi: 10.1016/j.ejmech.2023.115246. Epub 2023 Mar 4. Eur J Med Chem. 2023. PMID: 36898329 Free PMC article.
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
Shadrick WR, Slavish PJ, Chai SC, Waddell B, Connelly M, Low JA, Tallant C, Young BM, Bharatham N, Knapp S, Boyd VA, Morfouace M, Roussel MF, Chen T, Lee RE, Kiplin Guy R, Shelat AA, Potter PM. Shadrick WR, et al. Among authors: chai sc. Bioorg Med Chem. 2018 Jan 1;26(1):25-36. doi: 10.1016/j.bmc.2017.10.042. Epub 2017 Nov 4. Bioorg Med Chem. 2018. PMID: 29170024 Free PMC article.
Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer.
Slavish PJ, Chi L, Yun MK, Tsurkan L, Martinez NE, Jonchere B, Chai SC, Connelly M, Waddell MB, Das S, Neale G, Li Z, Shadrick WR, Olsen RR, Freeman KW, Low JA, Price JE, Young BM, Bharatham N, Boyd VA, Yang J, Lee RE, Morfouace M, Roussel MF, Chen T, Savic D, Guy RK, White SW, Shelat AA, Potter PM. Slavish PJ, et al. Among authors: chai sc. Cancer Res. 2020 Sep 1;80(17):3507-3518. doi: 10.1158/0008-5472.CAN-19-3934. Epub 2020 Jul 10. Cancer Res. 2020. PMID: 32651255 Free PMC article.
Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs.
Min J, Mayasundari A, Keramatnia F, Jonchere B, Yang SW, Jarusiewicz J, Actis M, Das S, Young B, Slavish J, Yang L, Li Y, Fu X, Garrett SH, Yun MK, Li Z, Nithianantham S, Chai S, Chen T, Shelat A, Lee RE, Nishiguchi G, White SW, Roussel MF, Potts PR, Fischer M, Rankovic Z. Min J, et al. Angew Chem Int Ed Engl. 2021 Dec 13;60(51):26663-26670. doi: 10.1002/anie.202108848. Epub 2021 Nov 16. Angew Chem Int Ed Engl. 2021. PMID: 34614283 Free PMC article.
136 results