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22 results

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Page 1
Functionally Biased D2R Antagonists: Targeting the β-Arrestin Pathway to Improve Antipsychotic Treatment.
Weïwer M, Xu Q, Gale JP, Lewis M, Campbell AJ, Schroeder FA, Van de Bittner GC, Walk M, Amaya A, Su P, D Ordevic L, Sacher JR, Skepner A, Fei D, Dennehy K, Nguyen S, Faloon PW, Perez J, Cottrell JR, Liu F, Palmer M, Pan JQ, Hooker JM, Zhang YL, Scolnick E, Wagner FF, Holson EB. Weïwer M, et al. Among authors: gale jp. ACS Chem Biol. 2018 Apr 20;13(4):1038-1047. doi: 10.1021/acschembio.8b00168. Epub 2018 Mar 14. ACS Chem Biol. 2018. PMID: 29485852
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.
Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects.
Wagner FF, Bishop JA, Gale JP, Shi X, Walk M, Ketterman J, Patnaik D, Barker D, Walpita D, Campbell AJ, Nguyen S, Lewis M, Ross L, Weïwer M, An WF, Germain AR, Nag PP, Metkar S, Kaya T, Dandapani S, Olson DE, Barbe AL, Lazzaro F, Sacher JR, Cheah JH, Fei D, Perez J, Munoz B, Palmer M, Stegmaier K, Schreiber SL, Scolnick E, Zhang YL, Haggarty SJ, Holson EB, Pan JQ. Wagner FF, et al. Among authors: gale jp. ACS Chem Biol. 2016 Jul 15;11(7):1952-63. doi: 10.1021/acschembio.6b00306. Epub 2016 May 13. ACS Chem Biol. 2016. PMID: 27128528
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
Novel Fluorescence-Based High-Throughput FLIPR Assay Utilizing Membrane-Tethered Genetic Calcium Sensors to Identify T-Type Calcium Channel Modulators.
Zhang YL, Moran SP, Allen A, Baez-Nieto D, Xu Q, Wang LA, Martenis WE, Sacher JR, Gale JP, Weïwer M, Wagner FF, Pan JQ. Zhang YL, et al. Among authors: gale jp. ACS Pharmacol Transl Sci. 2022 Feb 25;5(3):156-168. doi: 10.1021/acsptsci.1c00233. eCollection 2022 Mar 11. ACS Pharmacol Transl Sci. 2022. PMID: 35311021 Free PMC article.
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.
Selective HDAC inhibition for the disruption of latent HIV-1 infection.
Barton KM, Archin NM, Keedy KS, Espeseth AS, Zhang YL, Gale J, Wagner FF, Holson EB, Margolis DM. Barton KM, et al. PLoS One. 2014 Aug 19;9(8):e102684. doi: 10.1371/journal.pone.0102684. eCollection 2014. PLoS One. 2014. PMID: 25136952 Free PMC article.
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
22 results