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Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors.
Teuscher KB, Mills JJ, Tian J, Han C, Meyers KM, Sai J, South TM, Crow MM, Van Meveren M, Sensintaffar JL, Zhao B, Amporndanai K, Moore WJ, Stott GM, Tansey WP, Lee T, Fesik SW. Teuscher KB, et al. Among authors: van meveren m. J Med Chem. 2023 Dec 28;66(24):16783-16806. doi: 10.1021/acs.jmedchem.3c01529. Epub 2023 Dec 12. J Med Chem. 2023. PMID: 38085679 Free PMC article.
Structure-based discovery of potent WD repeat domain 5 inhibitors that demonstrate efficacy and safety in preclinical animal models.
Teuscher KB, Chowdhury S, Meyers KM, Tian J, Sai J, Van Meveren M, South TM, Sensintaffar JL, Rietz TA, Goswami S, Wang J, Grieb BC, Lorey SL, Howard GC, Liu Q, Moore WJ, Stott GM, Tansey WP, Lee T, Fesik SW. Teuscher KB, et al. Among authors: van meveren m. Proc Natl Acad Sci U S A. 2023 Jan 3;120(1):e2211297120. doi: 10.1073/pnas.2211297120. Epub 2022 Dec 27. Proc Natl Acad Sci U S A. 2023. PMID: 36574664 Free PMC article.
Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization.
Teuscher KB, Meyers KM, Wei Q, Mills JJ, Tian J, Alvarado J, Sai J, Van Meveren M, South TM, Rietz TA, Zhao B, Moore WJ, Stott GM, Tansey WP, Lee T, Fesik SW. Teuscher KB, et al. Among authors: van meveren m. J Med Chem. 2022 Apr 28;65(8):6287-6312. doi: 10.1021/acs.jmedchem.2c00195. Epub 2022 Apr 18. J Med Chem. 2022. PMID: 35436124 Free PMC article.