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Items: 14

1.

High throughput screen identifies IFN-γ-dependent inhibitors of Toxoplasma gondii growth.

Radke JB, Carey KL, Shaw S, Metkar S, Mulrooney C, Gale JP, Bittker JA, Hilgraf R, Comer E, Schreiber SL, Virgin HW, Perez JR, Sibley LD.

ACS Infect Dis. 2018 Jul 30. doi: 10.1021/acsinfecdis.8b00135. [Epub ahead of print]

PMID:
30058798
2.

Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia.

Wagner FF, Benajiba L, Campbell AJ, Weïwer M, Sacher JR, Gale JP, Ross L, Puissant A, Alexe G, Conway A, Back M, Pikman Y, Galinsky I, DeAngelo DJ, Stone RM, Kaya T, Shi X, Robers MB, Machleidt T, Wilkinson J, Hermine O, Kung A, Stein AJ, Lakshminarasimhan D, Hemann MT, Scolnick E, Zhang YL, Pan JQ, Stegmaier K, Holson EB.

Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. doi: 10.1126/scitranslmed.aam8460.

PMID:
29515000
3.

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.

ACS Chem Biol. 2018 Apr 20;13(4):1038-1047. doi: 10.1021/acschembio.8b00168. Epub 2018 Mar 14.

PMID:
29485852
4.

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.

Bioorg Med Chem. 2016 Sep 15;24(18):4008-4015. doi: 10.1016/j.bmc.2016.06.040. Epub 2016 Jun 22.

PMID:
27377864
5.

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.

ACS Chem Biol. 2016 Jul 15;11(7):1952-63. doi: 10.1021/acschembio.6b00306. Epub 2016 May 13.

PMID:
27128528
6.

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.

ACS Chem Biol. 2016 Feb 19;11(2):363-74. doi: 10.1021/acschembio.5b00640. Epub 2015 Dec 7.

PMID:
26640968
7.

Hydroxamate-based histone deacetylase inhibitors can protect neurons from oxidative stress via a histone deacetylase-independent catalase-like mechanism.

Olson DE, Sleiman SF, Bourassa MW, Wagner FF, Gale JP, Zhang YL, Ratan RR, Holson EB.

Chem Biol. 2015 Apr 23;22(4):439-445. doi: 10.1016/j.chembiol.2015.03.014. Epub 2015 Apr 16.

8.

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.

Chem Sci. 2015 Jan 1;6(1):804-815.

9.

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.

ACS Chem Biol. 2014 Oct 17;9(10):2210-6. doi: 10.1021/cb500492r. Epub 2014 Aug 11.

10.

Class I HDAC imaging using [ (3)H]CI-994 autoradiography.

Wang Y, Zhang YL, Hennig K, Gale JP, Hong Y, Cha A, Riley M, Wagner F, Haggarty SJ, Holson E, Hooker J.

Epigenetics. 2013 Jul;8(7):756-64. doi: 10.4161/epi.25202. Epub 2013 Jun 11.

11.

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.

J Med Chem. 2013 Jun 13;56(11):4816-20. doi: 10.1021/jm400390r. Epub 2013 May 29.

PMID:
23672185
12.

Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.

Wagner FF, Olson DE, Gale JP, Kaya T, Weïwer M, Aidoud N, Thomas M, Davoine EL, Lemercier BC, Zhang YL, Holson EB.

J Med Chem. 2013 Feb 28;56(4):1772-6. doi: 10.1021/jm301355j. Epub 2013 Feb 18.

PMID:
23368884
13.

A sensitive method for the determination of entecavir at picogram per milliliter level in human plasma by solid phase extraction and high-pH LC-MS/MS.

Zhang D, Fu Y, Gale JP, Aubry AF, Arnold ME.

J Pharm Biomed Anal. 2009 May 1;49(4):1027-33. doi: 10.1016/j.jpba.2009.02.003. Epub 2009 Feb 13.

PMID:
19285822
14.

Cloning and functional expression of the small subunit of acetolactate synthase from Nicotiana plumbaginifolia.

Hershey HP, Schwartz LJ, Gale JP, Abell LM.

Plant Mol Biol. 1999 Jul;40(5):795-806.

PMID:
10487214

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