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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: gale jp. J Med Chem. 2013 Jun 13;56(11):4816-20. doi: 10.1021/jm400390r. Epub 2013 May 29. J Med Chem. 2013. PMID: 23672185
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: gale jp. 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.
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection.
Wagner FF, Lundh M, Kaya T, McCarren P, Zhang YL, Chattopadhyay S, Gale JP, Galbo T, Fisher SL, Meier BC, Vetere A, Richardson S, Morgan NG, Christensen DP, Gilbert TJ, Hooker JM, Leroy M, Walpita D, Mandrup-Poulsen T, Wagner BK, Holson EB. Wagner FF, et al. Among authors: gale jp. ACS Chem Biol. 2016 Feb 19;11(2):363-74. doi: 10.1021/acschembio.5b00640. Epub 2015 Dec 7. ACS Chem Biol. 2016. PMID: 26640968
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: gale jp. 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
Kinetically Selective Inhibitors of Histone Deacetylase 2 (HDAC2) as Cognition Enhancers.
Wagner FF, Zhang YL, Fass DM, Joseph N, Gale JP, Weïwer M, McCarren P, Fisher SL, Kaya T, Zhao WN, Reis SA, Hennig KM, Thomas M, Lemercier BC, Lewis MC, Guan JS, Moyer MP, Scolnick E, Haggarty SJ, Tsai LH, Holson EB. Wagner FF, et al. Among authors: gale jp. Chem Sci. 2015 Jan 1;6(1):804-815. doi: 10.1039/C4SC02130D. Chem Sci. 2015. PMID: 25642316 Free PMC article.
PET imaging demonstrates histone deacetylase target engagement and clarifies brain penetrance of known and novel small molecule inhibitors in rat.
Schroeder FA, Wang C, Van de Bittner GC, Neelamegam R, Takakura WR, Karunakaran A, Wey HY, Reis SA, Gale J, Zhang YL, Holson EB, Haggarty SJ, Hooker JM. Schroeder FA, et al. ACS Chem Neurosci. 2014 Oct 15;5(10):1055-62. doi: 10.1021/cn500162j. Epub 2014 Sep 19. ACS Chem Neurosci. 2014. PMID: 25188794 Free PMC article.
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