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Items: 34

1.

Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into Clinical Trials.

Gilmore JL, Xiao HY, Dhar TGM, Yang MG, Xiao Z, Xie J, Lehman-McKeeman LD, Gong L, Sun H, Lecureux L, Chen C, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Borowski V, Warrack BM, Li Y, Shi H, Levesque PC, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Rampulla R, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Salter-Cid LM, Carter PH, Dyckman AJ.

J Med Chem. 2019 Mar 14;62(5):2265-2285. doi: 10.1021/acs.jmedchem.8b01695. Epub 2019 Mar 6.

PMID:
30785748
2.

Development of a Chemiluminescent ELISA Method for the Detection of Total Anti-Adeno Associated Virus Serotype 9 (AAV9) Antibodies.

Kavita U, Dai Y, Salvador L, Miller W, Adam LP, Levesque PC, Zhang YJ, Ji QC, Pillutla RC.

Hum Gene Ther Methods. 2018 Nov 22. doi: 10.1089/hgtb.2018.131. [Epub ahead of print]

PMID:
30351228
3.

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA.

J Med Chem. 2017 Jun 22;60(12):5193-5208. doi: 10.1021/acs.jmedchem.7b00618. Epub 2017 Jun 5.

PMID:
28541707
4.

Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus.

Wang AX, Chen J, Zhao Q, Sun LQ, Friborg J, Yu F, Hernandez D, Good AC, Klei HE, Rajamani R, Mosure K, Knipe JO, Li D, Zhu J, Levesque PC, McPhee F, Meanwell NA, Scola PM.

Bioorg Med Chem Lett. 2017 Feb 1;27(3):590-596. doi: 10.1016/j.bmcl.2016.12.013. Epub 2016 Dec 9.

PMID:
28011221
5.

Identification of potent tricyclic prodrug S1P1 receptor modulators.

Marcoux D, Xiao HY, Murali Dhar TG, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Shi H, Levesque PC, Sun H, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Gupta A, Pragalathan B, Rampulla R, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Lombardo LJ, Carter PH, Dyckman AJ.

Medchemcomm. 2016 Nov 25;8(4):725-729. doi: 10.1039/c6md00539j. eCollection 2017 Apr 1.

6.

Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.

Sun LQ, Mull E, Zheng B, D'Andrea S, Zhao Q, Wang AX, Sin N, Venables BL, Sit SY, Chen Y, Chen J, Cocuzza A, Bilder DM, Mathur A, Rampulla R, Chen BC, Palani T, Ganesan S, Arunachalam PN, Falk P, Levine S, Chen C, Friborg J, Yu F, Hernandez D, Sheaffer AK, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Ng A, Mueller L, Grasela DM, Adams S, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Wang YK, Fang H, Cockett MI, Meanwell NA, McPhee F, Scola PM.

J Med Chem. 2016 Sep 8;59(17):8042-60. doi: 10.1021/acs.jmedchem.6b00821. Epub 2016 Aug 26.

PMID:
27564532
7.

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

Gilmore JL, Sheppeck JE 2nd, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ.

J Med Chem. 2016 Jul 14;59(13):6248-64. doi: 10.1021/acs.jmedchem.6b00373. Epub 2016 Jul 1.

PMID:
27309907
8.

Evaluation of cardiac function in unrestrained dogs and monkeys using left ventricular dP/dt.

Buchanan LV, Warner WA, Arthur SR, Gleason CR, Lewen G, Levesque PC, Gill MW.

J Pharmacol Toxicol Methods. 2016 Jul-Aug;80:51-8. doi: 10.1016/j.vascn.2016.03.006. Epub 2016 Apr 8.

PMID:
27063376
9.

Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.

Dhar TG, Xiao HY, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Warrack B, Shi H, Levesque PC, Zhu JL, Hennan J, Balimane P, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.

ACS Med Chem Lett. 2016 Jan 19;7(3):283-8. doi: 10.1021/acsmedchemlett.5b00448. eCollection 2016 Mar 10.

10.

The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.

Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F.

J Med Chem. 2014 Mar 13;57(5):1730-52. doi: 10.1021/jm500297k. Epub 2014 Mar 5.

PMID:
24564672
11.

Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.

Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F.

J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20.

PMID:
24555570
12.

Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.

Jeon YT, Yang W, Qiao JX, Li L, Ruel R, Thibeault C, Hiebert S, Wang TC, Wang Y, Liu Y, Clark CG, Wong HS, Zhu J, Wu DR, Sun D, Chen BC, Mathur A, Chacko SA, Malley M, Chen XQ, Shen H, Huang CS, Schumacher WA, Bostwick JS, Stewart AB, Price LA, Hua J, Li D, Levesque PC, Seiffert DA, Rehfuss R, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1294-8. doi: 10.1016/j.bmcl.2014.01.066. Epub 2014 Jan 31.

PMID:
24513044
13.

Role of T-type calcium channel subunits in post-myocardial infarction remodelling probed with genetically engineered mice.

Le Quang K, Naud P, Qi XY, Duval F, Shi YF, Gillis MA, Comtois P, Tardif JC, Li D, Levesque PC, Dobrev D, Charpentier F, Nattel S.

Cardiovasc Res. 2011 Aug 1;91(3):420-8. doi: 10.1093/cvr/cvr082. Epub 2011 May 27.

PMID:
21622683
14.

Drug safety is a barrier to the discovery and development of new androgen receptor antagonists.

Foster WR, Car BD, Shi H, Levesque PC, Obermeier MT, Gan J, Arezzo JC, Powlin SS, Dinchuk JE, Balog A, Salvati ME, Attar RM, Gottardis MM.

Prostate. 2011 Apr;71(5):480-8. doi: 10.1002/pros.21263. Epub 2010 Sep 28.

PMID:
20878947
15.

Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.

Hangeland JJ, Cheney DL, Friends TJ, Swartz S, Levesque PC, Rich AJ, Sun L, Bridal TR, Adam LP, Normandin DE, Murugesan N, Ewing WR.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):474-8. Epub 2007 Dec 3.

PMID:
18160281
16.

Tetrahydronaphthalene-derived amino alcohols and amino ketones as potent and selective inhibitors of the delayed rectifier potassium current IKs.

Ahmad S, Doweyko L, Ashfaq A, Ferrara FN, Bisaha SN, Schmidt JB, DiMarco J, Conder ML, Jenkins-West T, Normandin DE, Russell AD, Smith MA, Levesque PC, Lodge NJ, Lloyd J, Stein PD, Atwal KS.

Bioorg Med Chem Lett. 2004 Jan 5;14(1):99-102.

PMID:
14684307
17.

Expression and characterization of human transient receptor potential melastatin 3 (hTRPM3).

Lee N, Chen J, Sun L, Wu S, Gray KR, Rich A, Huang M, Lin JH, Feder JN, Janovitz EB, Levesque PC, Blanar MA.

J Biol Chem. 2003 Jun 6;278(23):20890-7. Epub 2003 Apr 2.

18.

Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers.

Lloyd J, Schmidt JB, Rovnyak G, Ahmad S, Atwal KS, Bisaha SN, Doweyko LM, Stein PD, Traeger SC, Mathur A, Conder ML, DiMarco J, Harper TW, Jenkins-West T, Levesque PC, Normandin DE, Russell AD, Serafino RP, Smith MA, Lodge NJ.

J Med Chem. 2001 Nov 8;44(23):3764-7.

PMID:
11689063
19.

Functional expression of two KvLQT1-related potassium channels responsible for an inherited idiopathic epilepsy.

Yang WP, Levesque PC, Little WA, Conder ML, Ramakrishnan P, Neubauer MG, Blanar MA.

J Biol Chem. 1998 Jul 31;273(31):19419-23.

20.

Dominant-negative KvLQT1 mutations underlie the LQT1 form of long QT syndrome.

Shalaby FY, Levesque PC, Yang WP, Little WA, Conder ML, Jenkins-West T, Blanar MA.

Circulation. 1997 Sep 16;96(6):1733-6.

PMID:
9323054
21.

KvLQT1, a voltage-gated potassium channel responsible for human cardiac arrhythmias.

Yang WP, Levesque PC, Little WA, Conder ML, Shalaby FY, Blanar MA.

Proc Natl Acad Sci U S A. 1997 Apr 15;94(8):4017-21.

22.

Cystic fibrosis gene encodes a cAMP-dependent chloride channel in heart.

Hart P, Warth JD, Levesque PC, Collier ML, Geary Y, Horowitz B, Hume JR.

Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6343-8.

23.

Unitary Cl- channels activated by cytoplasmic Ca2+ in canine ventricular myocytes.

Collier ML, Levesque PC, Kenyon JL, Hume JR.

Circ Res. 1996 May;78(5):936-44.

PMID:
8620614
24.

ATPo but not cAMPi activates a chloride conductance in mouse ventricular myocytes.

Levesque PC, Hume JR.

Cardiovasc Res. 1995 Mar;29(3):336-43.

PMID:
7540110
25.

Release of calcium from guinea pig cardiac sarcoplasmic reticulum induced by sodium-calcium exchange.

Levesque PC, Leblanc N, Hume JR.

Cardiovasc Res. 1994 Mar;28(3):370-8.

PMID:
8174158
26.

Molecular physiology of CFTR Cl- channels in heart.

Hume JR, Hart P, Levesque PC, Collier ML, Geary Y, Warth J, Chapman T, Horowitz B.

Jpn J Physiol. 1994;44 Suppl 2:S177-82.

PMID:
7752524
27.

Anion and cation modulation of the guinea-pig ventricular action potential during beta-adrenoceptor stimulation.

Levesque PC, Clark CD, Zakarov SI, Rosenshtraukh LV, Hume JR.

Pflugers Arch. 1993 Jun;424(1):54-62.

PMID:
8394573
28.

Alternative splicing of CFTR Cl- channels in heart.

Horowitz B, Tsung SS, Hart P, Levesque PC, Hume JR.

Am J Physiol. 1993 Jun;264(6 Pt 2):H2214-20.

PMID:
7686720
29.

Expression of cystic fibrosis transmembrane regulator Cl- channels in heart.

Levesque PC, Hart PJ, Hume JR, Kenyon JL, Horowitz B.

Circ Res. 1992 Oct;71(4):1002-7.

PMID:
1381291
30.
31.

Role of reverse-mode Na(+)-Ca2+ exchange in excitation-contraction coupling in the heart.

Levesque PC, Leblanc N, Hume JR.

Ann N Y Acad Sci. 1991;639:386-97.

PMID:
1785865
32.

Disruption of brain mitochondrial calcium sequestration by methylmercury.

Levesque PC, Atchison WD.

J Pharmacol Exp Ther. 1991 Jan;256(1):236-42.

PMID:
1703231
33.
34.

Interactions of mitochondrial inhibitors with methylmercury on spontaneous quantal release of acetylcholine.

Levesque PC, Atchison WD.

Toxicol Appl Pharmacol. 1987 Feb;87(2):315-24.

PMID:
2435022

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