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Rapid Affinity and Microsomal Stability Ranking of Crude Mixture Libraries of Histone Deacetylase Inhibitors.
Tyagarajan S, Andrews CL, Beshore DC, Buevich AV, Curran PJ, Dandliker P, Greshock TJ, Hoar J, Kim A, Karnachi P, Knemeyer I, Kozlowski J, Liu J, Maletic M, Myers R, Rada V, Sha D, Sauvagnat B, Vachal P, Wolkenberg S, Yu W, Yu Y, Krska SW. Tyagarajan S, et al. Among authors: wolkenberg s. ACS Med Chem Lett. 2024 Sep 12;15(10):1787-1794. doi: 10.1021/acsmedchemlett.4c00345. eCollection 2024 Oct 10. ACS Med Chem Lett. 2024. PMID: 39411537
Enabling Deoxygenative C(sp2)-C(sp3) Cross-Coupling for Parallel Medicinal Chemistry.
Liu W, Mulhearn J, Hao B, Cañellas S, Last S, Gómez JE, Jones A, De Vera A, Kumar K, Rodríguez R, Van Eynde L, Strambeanu II, Wolkenberg SE. Liu W, et al. Among authors: wolkenberg se. ACS Med Chem Lett. 2023 May 22;14(6):853-859. doi: 10.1021/acsmedchemlett.3c00118. eCollection 2023 Jun 8. ACS Med Chem Lett. 2023. PMID: 37312855 Free PMC article.
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
Beshore DC, Adam GC, Barnard RJO, Burlein C, Gallicchio SN, Holloway MK, Krosky D, Lemaire W, Myers RW, Patel S, Plotkin MA, Powell DA, Rada V, Cox CD, Coleman PJ, Klein DJ, Wolkenberg SE. Beshore DC, et al. Among authors: wolkenberg se. ACS Med Chem Lett. 2021 Mar 7;12(4):540-547. doi: 10.1021/acsmedchemlett.1c00074. eCollection 2021 Apr 8. ACS Med Chem Lett. 2021. PMID: 33854701 Free PMC article.
Trends in Hit-to-Lead Optimization Following DNA-Encoded Library Screens.
Reiher CA, Schuman DP, Simmons N, Wolkenberg SE. Reiher CA, et al. Among authors: wolkenberg se. ACS Med Chem Lett. 2021 Feb 11;12(3):343-350. doi: 10.1021/acsmedchemlett.0c00615. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738060 Free PMC article.
Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.
Bukhtiyarova M, Cook EM, Hancock PJ, Hruza AW, Shaw AW, Adam GC, Barnard RJO, McKenna PM, Holloway MK, Bell IM, Carroll S, Cornella-Taracido I, Cox CD, Kutchukian PS, Powell DA, Strickland C, Trotter BW, Tudor M, Wolkenberg S, Li J, Tellers DM. Bukhtiyarova M, et al. Among authors: wolkenberg s. ACS Med Chem Lett. 2020 Dec 23;12(1):99-106. doi: 10.1021/acsmedchemlett.0c00551. eCollection 2021 Jan 14. ACS Med Chem Lett. 2020. PMID: 33488970 Free PMC article.
Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group.
Liu J, Yu Y, Kelly J, Sha D, Alhassan AB, Yu W, Maletic MM, Duffy JL, Klein DJ, Holloway MK, Carroll S, Howell BJ, Barnard RJO, Wolkenberg S, Kozlowski JA. Liu J, et al. Among authors: wolkenberg s. ACS Med Chem Lett. 2020 Oct 13;11(12):2476-2483. doi: 10.1021/acsmedchemlett.0c00462. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335670 Free PMC article.
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Yu W, Liu J, Yu Y, Zhang V, Clausen D, Kelly J, Wolkenberg S, Beshore D, Duffy JL, Chung CC, Myers RW, Klein DJ, Fells J, Holloway K, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J. Yu W, et al. Among authors: wolkenberg s. Bioorg Med Chem Lett. 2020 Jul 1;30(13):127197. doi: 10.1016/j.bmcl.2020.127197. Epub 2020 Apr 15. Bioorg Med Chem Lett. 2020. PMID: 32331932
Benzoxazolinone aryl sulfonamides as potent, selective Nav1.7 inhibitors with in vivo efficacy in a preclinical pain model.
Pero JE, Rossi MA, Lehman HDGF, Kelly MJ 3rd, Mulhearn JJ, Wolkenberg SE, Cato MJ, Clements MK, Daley CJ, Filzen T, Finger EN, Gregan Y, Henze DA, Jovanovska A, Klein R, Kraus RL, Li Y, Liang A, Majercak JM, Panigel J, Urban MO, Wang J, Wang YH, Houghton AK, Layton ME. Pero JE, et al. Among authors: wolkenberg se. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2683-2688. doi: 10.1016/j.bmcl.2017.04.040. Epub 2017 Apr 22. Bioorg Med Chem Lett. 2017. PMID: 28465103
42 results