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Items: 9

1.

TRPA1 modulation by piperidine carboxamides suggests an evolutionarily conserved binding site and gating mechanism.

Chernov-Rogan T, Gianti E, Liu C, Villemure E, Cridland AP, Hu X, Ballini E, Lange W, Deisemann H, Li T, Ward SI, Hackos DH, Magnuson S, Safina B, Klein ML, Volgraf M, Carnevale V, Chen J.

Proc Natl Acad Sci U S A. 2019 Dec 17;116(51):26008-26019. doi: 10.1073/pnas.1913929116. Epub 2019 Dec 3. Erratum in: Proc Natl Acad Sci U S A. 2020 Jan 28;117(4):2226-2227.

2.

Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.

Chen H, Volgraf M, Do S, Kolesnikov A, Shore DG, Verma VA, Villemure E, Wang L, Chen Y, Hu B, Lu AJ, Wu G, Xu X, Yuen PW, Zhang Y, Erickson SD, Dahl M, Brotherton-Pleiss C, Tay S, Ly JQ, Murray LJ, Chen J, Amm D, Lange W, Hackos DH, Reese RM, Shields SD, Lyssikatos JP, Safina BS, Estrada AA.

J Med Chem. 2018 Apr 26;61(8):3641-3659. doi: 10.1021/acs.jmedchem.8b00117. Epub 2018 Apr 12.

PMID:
29590749
3.

GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile.

Villemure E, Volgraf M, Jiang Y, Wu G, Ly CQ, Yuen PW, Lu A, Luo X, Liu M, Zhang S, Lupardus PJ, Wallweber HJ, Liederer BM, Deshmukh G, Plise E, Tay S, Wang TM, Hanson JE, Hackos DH, Scearce-Levie K, Schwarz JB, Sellers BD.

ACS Med Chem Lett. 2016 Oct 31;8(1):84-89. doi: 10.1021/acsmedchemlett.6b00388. eCollection 2017 Jan 12.

4.

Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.

Volgraf M, Sellers BD, Jiang Y, Wu G, Ly CQ, Villemure E, Pastor RM, Yuen PW, Lu A, Luo X, Liu M, Zhang S, Sun L, Fu Y, Lupardus PJ, Wallweber HJ, Liederer BM, Deshmukh G, Plise E, Tay S, Reynen P, Herrington J, Gustafson A, Liu Y, Dirksen A, Dietz MG, Liu Y, Wang TM, Hanson JE, Hackos D, Scearce-Levie K, Schwarz JB.

J Med Chem. 2016 Mar 24;59(6):2760-79. doi: 10.1021/acs.jmedchem.5b02010. Epub 2016 Mar 8.

PMID:
26919761
5.

Discovery of hepatitis C virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution.

Moreau B, O'Meara JA, Bordeleau J, Garneau M, Godbout C, Gorys V, Leblanc M, Villemure E, White PW, LlinĂ s-Brunet M.

J Med Chem. 2014 Mar 13;57(5):1770-6. doi: 10.1021/jm400121t. Epub 2013 Mar 28.

PMID:
23506530
6.

Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.

Rew Y, McMinn DL, Wang Z, He X, Hungate RW, Jaen JC, Sudom A, Sun D, Tu H, Ursu S, Villemure E, Walker NP, Yan X, Ye Q, Powers JP.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1797-801. doi: 10.1016/j.bmcl.2009.01.058. Epub 2009 Jan 23.

PMID:
19217779
7.

Palladium-catalyzed direct arylation of azine and azole N-oxides: reaction development, scope and applications in synthesis.

Campeau LC, Stuart DR, Leclerc JP, Bertrand-Laperle M, Villemure E, Sun HY, Lasserre S, Guimond N, Lecavallier M, Fagnou K.

J Am Chem Soc. 2009 Mar 11;131(9):3291-306. doi: 10.1021/ja808332k.

PMID:
19215128
8.

C2, C5, and C4 azole N-oxide direct arylation including room-temperature reactions.

Campeau LC, Bertrand-Laperle M, Leclerc JP, Villemure E, Gorelsky S, Fagnou K.

J Am Chem Soc. 2008 Mar 19;130(11):3276-7. doi: 10.1021/ja7107068. Epub 2008 Feb 27. No abstract available.

PMID:
18302383
9.

Elements of regiocontrol in palladium-catalyzed oxidative arene cross-coupling.

Stuart DR, Villemure E, Fagnou K.

J Am Chem Soc. 2007 Oct 10;129(40):12072-3. Epub 2007 Sep 19. No abstract available.

PMID:
17880083

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