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Items: 40

1.

2-Hydroxypropyl-β-cyclodextrin is the active component in a triple combination formulation for treatment of Niemann-Pick C1 disease.

Davidson J, Molitor E, Moores S, Gale SE, Subramanian K, Jiang X, Sidhu R, Kell P, Zhang J, Fujiwara H, Davidson C, Helquist P, Melancon BJ, Grigalunas M, Liu G, Salahi F, Wiest O, Xu X, Porter FD, Pipalia NH, Cruz DL, Holson EB, Schaffer JE, Walkley SU, Maxfield FR, Ory DS.

Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Oct;1864(10):1545-1561. doi: 10.1016/j.bbalip.2019.04.011. Epub 2019 Apr 30.

PMID:
31051283
2.

Lactate is an antidepressant that mediates resilience to stress by modulating the hippocampal levels and activity of histone deacetylases.

Karnib N, El-Ghandour R, El Hayek L, Nasrallah P, Khalifeh M, Barmo N, Jabre V, Ibrahim P, Bilen M, Stephan JS, Holson EB, Ratan RR, Sleiman SF.

Neuropsychopharmacology. 2019 May;44(6):1152-1162. doi: 10.1038/s41386-019-0313-z. Epub 2019 Jan 8.

PMID:
30647450
3.

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.

4.

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
5.

Isoform-selective inhibitor of histone deacetylase 3 (HDAC3) limits pancreatic islet infiltration and protects female nonobese diabetic mice from diabetes.

Dirice E, Ng RWS, Martinez R, Hu J, Wagner FF, Holson EB, Wagner BK, Kulkarni RN.

J Biol Chem. 2017 Oct 27;292(43):17598-17608. doi: 10.1074/jbc.M117.804328. Epub 2017 Aug 31.

6.

Overlapping and Divergent Actions of Structurally Distinct Histone Deacetylase Inhibitors in Cardiac Fibroblasts.

Schuetze KB, Stratton MS, Blakeslee WW, Wempe MF, Wagner FF, Holson EB, Kuo YM, Andrews AJ, Gilbert TM, Hooker JM, McKinsey TA.

J Pharmacol Exp Ther. 2017 Apr;361(1):140-150. doi: 10.1124/jpet.116.237701. Epub 2017 Feb 7.

7.

Activity of caffeic acid phenethyl ester in Caenorhabditis elegans.

Coleman JJ, Komura T, Munro J, Wu MP, Busanelli RR, Koehler AN, Thomas M, Wagner FF, Holson EB, Mylonakis E.

Future Med Chem. 2016 Nov;8(17):2033-2046. doi: 10.4155/fmc-2016-0085. Epub 2016 Oct 14.

8.

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
9.

Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.

Liang SH, Chen JM, Normandin MD, Chang JS, Chang GC, Taylor CK, Trapa P, Plummer MS, Para KS, Conn EL, Lopresti-Morrow L, Lanyon LF, Cook JM, Richter KE, Nolan CE, Schachter JB, Janat F, Che Y, Shanmugasundaram V, Lefker BA, Enerson BE, Livni E, Wang L, Guehl NJ, Patnaik D, Wagner FF, Perlis R, Holson EB, Haggarty SJ, El Fakhri G, Kurumbail RG, Vasdev N.

Angew Chem Int Ed Engl. 2016 Aug 8;55(33):9601-5. doi: 10.1002/anie.201603797. Epub 2016 Jun 29.

10.

Exercise promotes the expression of brain derived neurotrophic factor (BDNF) through the action of the ketone body β-hydroxybutyrate.

Sleiman SF, Henry J, Al-Haddad R, El Hayek L, Abou Haidar E, Stringer T, Ulja D, Karuppagounder SS, Holson EB, Ratan RR, Ninan I, Chao MV.

Elife. 2016 Jun 2;5. pii: e15092. doi: 10.7554/eLife.15092.

11.

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
12.

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
13.

EHMT1 and EHMT2 inhibition induces fetal hemoglobin expression.

Renneville A, Van Galen P, Canver MC, McConkey M, Krill-Burger JM, Dorfman DM, Holson EB, Bernstein BE, Orkin SH, Bauer DE, Ebert BL.

Blood. 2015 Oct 15;126(16):1930-9. doi: 10.1182/blood-2015-06-649087. Epub 2015 Aug 28.

14.

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.

15.

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.

16.

Hydroxamic acid-based histone deacetylase (HDAC) inhibitors can mediate neuroprotection independent of HDAC inhibition.

Sleiman SF, Olson DE, Bourassa MW, Karuppagounder SS, Zhang YL, Gale J, Wagner FF, Basso M, Coppola G, Pinto JT, Holson EB, Ratan RR.

J Neurosci. 2014 Oct 22;34(43):14328-37. doi: 10.1523/JNEUROSCI.1010-14.2014. Erratum in: J Neurosci. 2015 Jan 7;35(1):438.

17.

In vivo imaging of histone deacetylases (HDACs) in the central nervous system and major peripheral organs.

Wang C, Schroeder FA, Wey HY, Borra R, Wagner FF, Reis S, Kim SW, Holson EB, Haggarty SJ, Hooker JM.

J Med Chem. 2014 Oct 9;57(19):7999-8009. doi: 10.1021/jm500872p. Epub 2014 Sep 18.

18.

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.

ACS Chem Neurosci. 2014 Oct 15;5(10):1055-62. doi: 10.1021/cn500162j. Epub 2014 Sep 19.

19.

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.

PLoS One. 2014 Aug 19;9(8):e102684. doi: 10.1371/journal.pone.0102684. eCollection 2014.

20.

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.

21.

Discovery of Potent and Highly Selective Inhibitors of GSK3b.

An WF, Germain AR, Bishop JA, Nag PP, Metkar S, Ketterman J, Walk M, Weiwer M, Liu X, Patnaik D, Zhang YL, Gale J, Zhao W, Kaya T, Barker D, Wagner FF, Holson EB, Dandapani S, Perez J, Munoz B, Palmer M, Pan JQ, Haggarty SJ, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 16 [updated 2014 May 13].

22.

Design, synthesis, and evaluation of hydroxamic acid-based molecular probes for in vivo imaging of histone deacetylase (HDAC) in brain.

Wang C, Eessalu TE, Barth VN, Mitch CH, Wagner FF, Hong Y, Neelamegam R, Schroeder FA, Holson EB, Haggarty SJ, Hooker JM.

Am J Nucl Med Mol Imaging. 2013 Dec 15;4(1):29-38. eCollection 2013.

23.

Small molecule inhibitors of zinc-dependent histone deacetylases.

Wagner FF, Weїwer M, Lewis MC, Holson EB.

Neurotherapeutics. 2013 Oct;10(4):589-604. doi: 10.1007/s13311-013-0226-1. Review.

24.

Therapeutic potential of isoform selective HDAC inhibitors for the treatment of schizophrenia.

Weïwer M, Lewis MC, Wagner FF, Holson EB.

Future Med Chem. 2013 Sep;5(13):1491-508. doi: 10.4155/fmc.13.141. Review.

PMID:
24024943
25.

A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and alters mouse behavior in two mood-related tests.

Schroeder FA, Lewis MC, Fass DM, Wagner FF, Zhang YL, Hennig KM, Gale J, Zhao WN, Reis S, Barker DD, Berry-Scott E, Kim SW, Clore EL, Hooker JM, Holson EB, Haggarty SJ, Petryshen TL.

PLoS One. 2013 Aug 14;8(8):e71323. doi: 10.1371/journal.pone.0071323. eCollection 2013.

26.

FDG-PET imaging reveals local brain glucose utilization is altered by class I histone deacetylase inhibitors.

Schroeder FA, Chonde DB, Riley MM, Moseley CK, Granda ML, Wilson CM, Wagner FF, Zhang YL, Gale J, Holson EB, Haggarty SJ, Hooker JM.

Neurosci Lett. 2013 Aug 29;550:119-24. doi: 10.1016/j.neulet.2013.06.016. Epub 2013 Jun 25.

27.

Signal-dependent repression of DUSP5 by class I HDACs controls nuclear ERK activity and cardiomyocyte hypertrophy.

Ferguson BS, Harrison BC, Jeong MY, Reid BG, Wempe MF, Wagner FF, Holson EB, McKinsey TA.

Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9806-11. doi: 10.1073/pnas.1301509110. Epub 2013 May 29.

28.

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
29.

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
30.

Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries.

Lowe JT, Lee MD 4th, Akella LB, Davoine E, Donckele EJ, Durak L, Duvall JR, Gerard B, Holson EB, Joliton A, Kesavan S, Lemercier BC, Liu H, Marié JC, Mulrooney CA, Muncipinto G, Welzel-O'Shea M, Panko LM, Rowley A, Suh BC, Thomas M, Wagner FF, Wei J, Foley MA, Marcaurelle LA.

J Org Chem. 2012 Sep 7;77(17):7187-211. doi: 10.1021/jo300974j. Epub 2012 Aug 10.

31.

Inhibition of histone deacetylase 3 protects beta cells from cytokine-induced apoptosis.

Chou DH, Holson EB, Wagner FF, Tang AJ, Maglathlin RL, Lewis TA, Schreiber SL, Wagner BK.

Chem Biol. 2012 Jun 22;19(6):669-73. doi: 10.1016/j.chembiol.2012.05.010.

32.

Chromatin-targeting small molecules cause class-specific transcriptional changes in pancreatic endocrine cells.

Kubicek S, Gilbert JC, Fomina-Yadlin D, Gitlin AD, Yuan Y, Wagner FF, Holson EB, Luo T, Lewis TA, Taylor B, Gupta S, Shamji AF, Wagner BK, Clemons PA, Schreiber SL.

Proc Natl Acad Sci U S A. 2012 Apr 3;109(14):5364-9. doi: 10.1073/pnas.1201079109. Epub 2012 Mar 20.

33.

Chemoproteomics quantifies complexity.

Holson EB, Schreiber SL.

Nat Biotechnol. 2011 Mar;29(3):235-6. doi: 10.1038/nbt.1804. No abstract available.

PMID:
21390028
34.

AKT kinase activity is required for lithium to modulate mood-related behaviors in mice.

Pan JQ, Lewis MC, Ketterman JK, Clore EL, Riley M, Richards KR, Berry-Scott E, Liu X, Wagner FF, Holson EB, Neve RL, Biechele TL, Moon RT, Scolnick EM, Petryshen TL, Haggarty SJ.

Neuropsychopharmacology. 2011 Jun;36(7):1397-411. doi: 10.1038/npp.2011.24. Epub 2011 Mar 9.

35.

Hdac3 is essential for the maintenance of chromatin structure and genome stability.

Bhaskara S, Knutson SK, Jiang G, Chandrasekharan MB, Wilson AJ, Zheng S, Yenamandra A, Locke K, Yuan JL, Bonine-Summers AR, Wells CE, Kaiser JF, Washington MK, Zhao Z, Wagner FF, Sun ZW, Xia F, Holson EB, Khabele D, Hiebert SW.

Cancer Cell. 2010 Nov 16;18(5):436-47. doi: 10.1016/j.ccr.2010.10.022.

36.

Characterization of plant-derived saponin natural products against Candida albicans.

Coleman JJ, Okoli I, Tegos GP, Holson EB, Wagner FF, Hamblin MR, Mylonakis E.

ACS Chem Biol. 2010 Mar 19;5(3):321-32. doi: 10.1021/cb900243b.

37.
40.

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.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2741-5.

PMID:
11591514

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