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Items: 26

1.

Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).

Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP.

Bioorg Med Chem Lett. 2019 Jun 1;29(11):1380-1385. doi: 10.1016/j.bmcl.2019.03.039. Epub 2019 Mar 27.

PMID:
30952592
2.

Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.

He S, Lai Z, Hong Q, Shang J, Reibarkh M, Kuethe JT, Liu J, Guiadeen D, Krikorian AD, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Verras A, Sonatore LM, Wiltsie J, Chung CC, Murphy BA, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ.

Bioorg Med Chem Lett. 2019 May 15;29(10):1182-1186. doi: 10.1016/j.bmcl.2019.03.025. Epub 2019 Mar 21.

PMID:
30926247
3.

Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.

Shah SK, He S, Guo L, Truong Q, Qi H, Du W, Lai Z, Liu J, Jian T, Hong Q, Dobbelaar P, Ye Z, Sherer E, Feng Z, Yu Y, Wong F, Samuel K, Madiera M, Karanam BV, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Feng Y, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Pachanski M, Fernandez G, Nelson D, Bunting P, Morissette P, Volksdorf S, Kerr J, Zhang BB, Howard AD, Zhou YP, Pasternak A, Nargund RP, Hagmann WK.

ACS Med Chem Lett. 2015 Mar 18;6(5):513-7. doi: 10.1021/ml500514w. eCollection 2015 May 14.

4.

Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

He S, Hong Q, Lai Z, Yang DX, Ting PC, Kuethe JT, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sonatore LM, Wiltsie J, Liu J, Gorski JN, Chung CC, Gibson JT, Lisnock J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ.

ACS Med Chem Lett. 2014 Sep 8;5(10):1082-7. doi: 10.1021/ml5003426. eCollection 2014 Oct 9.

5.

Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.

He S, Hong Q, Lai Z, Wu Z, Yu Y, Kim DW, Ting PC, Kuethe JT, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sperbeck DM, Sonatore LM, Wiltsie J, Chung CC, Gibson JT, Lisnock J, Murphy BA, Gorski JN, Liu J, Chen D, Chen X, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ.

ACS Med Chem Lett. 2013 Jun 6;4(8):773-8. doi: 10.1021/ml400168h. eCollection 2013 Aug 8.

6.

Identification and characterization of sebaceous gland atrophy-sparing DGAT1 inhibitors.

Muise ES, Zhu Y, Verras A, Karanam BV, Gorski J, Weingarth D, Lin HV, Hwa J, Thompson JR, Hu G, Liu J, He S, DeVita RJ, Shen DM, Pinto S.

PLoS One. 2014 Feb 18;9(2):e88908. doi: 10.1371/journal.pone.0088908. eCollection 2014.

7.

A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain.

Hoyt SB, London C, Abbadie C, Felix JP, Garcia ML, Jochnowitz N, Karanam BV, Li X, Lyons KA, McGowan E, Priest BT, Smith MM, Warren VA, Thomas-Fowlkes BS, Kaczorowski GJ, Duffy JL.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3640-5. doi: 10.1016/j.bmcl.2013.03.121. Epub 2013 Apr 5.

PMID:
23652221
8.

Antidiabetic and antisteatotic effects of the selective fatty acid synthase (FAS) inhibitor platensimycin in mouse models of diabetes.

Wu M, Singh SB, Wang J, Chung CC, Salituro G, Karanam BV, Lee SH, Powles M, Ellsworth KP, Lassman ME, Miller C, Myers RW, Tota MR, Zhang BB, Li C.

Proc Natl Acad Sci U S A. 2011 Mar 29;108(13):5378-83. doi: 10.1073/pnas.1002588108. Epub 2011 Mar 9.

9.

In vitro and in vivo metabolism of a novel cannabinoid-1 receptor inverse agonist, taranabant, in rats and monkeys.

Reddy VB, Doss GA, Karanam BV, Samuel K, Lanza TJ Jr, Lin LS, Yu NX, Zhang AS, Raab CE, Stearns RA, Kumar S.

Xenobiotica. 2010 Sep;40(9):650-62. doi: 10.3109/00498254.2010.501117.

PMID:
20608842
10.

Discovery of imidazole carboxamides as potent and selective CCK1R agonists.

Zhu C, Hansen AR, Bateman T, Chen Z, Holt TG, Hubert JA, Karanam BV, Lee SJ, Pan J, Qian S, Reddy VB, Reitman ML, Strack AM, Tong V, Weingarth DT, Wolff MS, MacNeil DJ, Weber AE, Duffy JL, Edmondson SD.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4393-6. doi: 10.1016/j.bmcl.2008.06.057. Epub 2008 Jun 20.

PMID:
18614364
11.

Imidazopyridines: a novel class of hNav1.7 channel blockers.

London C, Hoyt SB, Parsons WH, Williams BS, Warren VA, Tschirret-Guth R, Smith MM, Priest BT, McGowan E, Martin WJ, Lyons KA, Li X, Karanam BV, Jochnowitz N, Garcia ML, Felix JP, Dean B, Abbadie C, Kaczorowski GJ, Duffy JL.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1696-701. doi: 10.1016/j.bmcl.2008.01.047. Epub 2008 Jan 18.

PMID:
18243692
12.

Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.

Hoyt SB, London C, Ok H, Gonzalez E, Duffy JL, Abbadie C, Dean B, Felix JP, Garcia ML, Jochnowitz N, Karanam BV, Li X, Lyons KA, McGowan E, Macintyre DE, Martin WJ, Priest BT, Smith MM, Tschirret-Guth R, Warren VA, Williams BS, Kaczorowski GJ, Parsons WH.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6172-7. Epub 2007 Sep 11.

PMID:
17889534
13.

The pharmacokinetics and disposition of MK-0524, a Prosglandin D2 Receptor 1 antagonist, in rats, dogs and monkeys.

Chang SW, Reddy V, Pereira T, Dean BJ, Xia YQ, Seto C, Franklin RB, Karanam BV.

Xenobiotica. 2007 May;37(5):514-33.

PMID:
17523054
14.

Effect of enalapril on the in vitro and in vivo peptidyl cleavage of a potent VLA-4 antagonist.

Karanam BV, Jayraj A, Rabe M, Wang Z, Keohane C, Strauss J, Vincent S.

Xenobiotica. 2007 May;37(5):487-502.

PMID:
17523052
15.

Mechanistic studies on the metabolic scission of thiazolidinedione derivatives to acyclic thiols.

Reddy VB, Karanam BV, Gruber WL, Wallace MA, Vincent SH, Franklin RB, Baillie TA.

Chem Res Toxicol. 2005 May;18(5):880-8.

PMID:
15892582
17.
20.

2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.

Young JR, Huang SX, Walsh TF, Wyvratt MJ, Yang YT, Yudkovitz JB, Cui J, Mount GR, Ren RN, Wu TJ, Shen X, Lyons KA, Mao AH, Carlin JR, Karanam BV, Vincent SH, Cheng K, Goulet MT.

Bioorg Med Chem Lett. 2002 Mar 11;12(5):827-32.

PMID:
11859012
21.

Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.

Ashton WT, Sisco RM, Kieczykowski GR, Yang YT, Yudkovitz JB, Cui J, Mount GR, Ren RN, Wu TJ, Shen X, Lyons KA, Mao AH, Carlin JR, Karanam BV, Vincent SH, Cheng K, Goulet MT.

Bioorg Med Chem Lett. 2001 Oct 8;11(19):2597-602.

PMID:
11551758
22.

Disposition of L-732,531, a potent immunosuppressant, in rats and baboons.

Karanam BV, Miller RR, Colletti A, Montgomery T, Carey KD, Hawkins T, Tang YS, Lavin M, Stearns RA, Chiu SH, Vincent SH.

Drug Metab Dispos. 1998 Oct;26(10):949-57.

PMID:
9763399
23.

Orally active inhibitors of human leukocyte elastase. II. Disposition of L-694,458 in rats and rhesus monkeys.

Vincent SH, Painter SK, Luffer-Atlas D, Karanam BV, McGowan E, Cioffe C, Doss G, Chiu SH.

Drug Metab Dispos. 1997 Aug;25(8):932-9.

PMID:
9280401
24.

FK 506 metabolism in human liver microsomes: investigation of the involvement of cytochrome P450 isozymes other than CYP3A4.

Karanam BV, Vincent SH, Newton DJ, Wang RW, Chiu SH.

Drug Metab Dispos. 1994 Sep-Oct;22(5):811-4. No abstract available. Erratum in: Drug Metab Dispos 1994 Nov-Dec;22(6):979.

PMID:
7530623
26.

Effects of the immunosuppressant FK-506 and its analog FK-520 on hepatic and renal cytochrome P450 mixed-function oxidase.

Vincent SH, Wang RW, Karanam BV, Klimko M, Alvaro R, Chiu SH.

Biochem Pharmacol. 1991 May 1;41(9):1325-30.

PMID:
1708254

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