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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Hale JJ, Budhu RJ, Holson EB, Finke PE, Oates B, Mills SG, MacCoss M, Gould SL, DeMartino JA, Springer MS, Siciliano S, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini E. Hale JJ, et al. Among authors: holson eb. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2741-5. doi: 10.1016/s0960-894x(01)00545-5. Bioorg Med Chem Lett. 2001. PMID: 11591514
Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors.
Wagner FF, Weïwer M, Steinbacher S, Schomburg A, Reinemer P, Gale JP, Campbell AJ, Fisher SL, Zhao WN, Reis SA, Hennig KM, Thomas M, Müller P, Jefson MR, Fass DM, Haggarty SJ, Zhang YL, Holson EB. Wagner FF, et al. Among authors: holson eb. Bioorg Med Chem. 2016 Sep 15;24(18):4008-4015. doi: 10.1016/j.bmc.2016.06.040. Epub 2016 Jun 22. Bioorg Med Chem. 2016. PMID: 27377864
Discovery of the first histone deacetylase 6/8 dual inhibitors.
Olson DE, Wagner FF, Kaya T, Gale JP, Aidoud N, Davoine EL, Lazzaro F, Weïwer M, Zhang YL, Holson EB. Olson DE, et al. Among authors: holson eb. J Med Chem. 2013 Jun 13;56(11):4816-20. doi: 10.1021/jm400390r. Epub 2013 May 29. J Med Chem. 2013. PMID: 23672185
Small molecule inhibitors of zinc-dependent histone deacetylases.
Wagner FF, Weїwer M, Lewis MC, Holson EB. Wagner FF, et al. Among authors: holson eb. Neurotherapeutics. 2013 Oct;10(4):589-604. doi: 10.1007/s13311-013-0226-1. Neurotherapeutics. 2013. PMID: 24101253 Free PMC article. Review.
An unbiased approach to identify endogenous substrates of "histone" deacetylase 8.
Olson DE, Udeshi ND, Wolfson NA, Pitcairn CA, Sullivan ED, Jaffe JD, Svinkina T, Natoli T, Lu X, Paulk J, McCarren P, Wagner FF, Barker D, Howe E, Lazzaro F, Gale JP, Zhang YL, Subramanian A, Fierke CA, Carr SA, Holson EB. Olson DE, et al. Among authors: holson eb. ACS Chem Biol. 2014 Oct 17;9(10):2210-6. doi: 10.1021/cb500492r. Epub 2014 Aug 11. ACS Chem Biol. 2014. PMID: 25089360 Free PMC article.
54 results