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In vitro metabolism of FK-506 in rat, rabbit, and human liver microsomes: Identification of a major metabolite and of cytochrome P450 3A as the major enzymes responsible for its metabolismVincent, Styliani H ; Karanam, Bindhu V ; Painter, Susan K ; Chiu, Shuet-Hing LArchives of Biochemistry and Biophysics, 1992, Vol.294(2), pp.454-460 [Peer Reviewed Journal]Full text available |
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Material Type: Article
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Identification and Characterization of Sebaceous Gland Atrophy-Sparing DGAT1 InhibitorsMuise, Eric S ; Zhu, Yonghua ; Verras, Andreas ; Karanam, Bindhu V ; Gorski, Judith ; Weingarth, Drew ; Lin, Hua V ; Hwa, Joyce ; Thompson, John R ; Hu, Guanghui ; Liu, Jian ; He, Shuwen ; Devita, Robert J ; Shen, Dong-Ming ; Pinto, Shirly Slominski, Andrzej T. (editor)PLoS ONE, 2014, Vol.9(2) [Peer Reviewed Journal]Full text available |
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A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic painHoyt, Scott B ; London, Clare ; Abbadie, Catherine ; Felix, John P ; Garcia, Maria L ; Jochnowitz, Nina ; Karanam, Bindhu V ; Li, Xiaohua ; Lyons, Kathryn A ; Mcgowan, Erin ; Priest, Birgit T ; Smith, Mchardy M ; Warren, Vivien A ; Thomas-Fowlkes, Brande S ; Kaczorowski, Gregory J ; Duffy, Joseph LBioorganic & Medicinal Chemistry Letters, 15 June 2013, Vol.23(12), pp.3640-3645 [Peer Reviewed Journal]Full text available |
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Antidiabetic and antisteatotic effects of the selective fatty acid synthase (FAS) inhibitor platensimycin in mouse models of diabetesWu, Margaret ; Singh, Sheo B ; Wang, Jun ; Chung, Christine C ; Salituro, Gino ; Karanam, Bindhu V ; Lee, Sang Ho ; Powles, Maryann ; Ellsworth, Kenneth P ; Lassman, Michael E ; Miller, Corey ; Myers, Robert W ; Tota, Michael R ; Zhang, Bei B ; Li, CaiProceedings of the National Academy of Sciences of the United States of America, 29 March 2011, Vol.108(13), pp.5378-83 [Peer Reviewed Journal]Full text available |
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Material Type: Article
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Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid MoietyHe, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Wu, Zhicai ; Yu, Yang ; Kim, David W ; Ting, Pauline C ; Kuethe, Jeffrey T ; Yang, Ginger X ; Jian, Tianying ; Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto D ; Sperbeck, Donald M ; Sonatore, Lisa M ; Wiltsie, Judyann ; Chung, Christine C ; Gibson, Jack T ; Lisnock, Jeanmarie ; Murphy, Beth A ; Gorski, Judith N ; Liu, Jinqi ; Chen, Dunlu ; Chen, Xiaoli ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; Pinto, Shirly ; Nargund, Ravi P ; Devita, Robert JACS medicinal chemistry letters, 08 August 2013, Vol.4(8), pp.773-8 [Peer Reviewed Journal]Full text available |
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Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid MoietyHe, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Yang, David X ; Ting, Pauline C ; Kuethe, Jeffrey T ; Cernak, Timothy A ; Dykstra, Kevin D ; Sperbeck, Donald M ; Wu, Zhicai ; Yu, Yang ; Yang, Ginger X ; Jian, Tianying ; Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto D ; Sonatore, Lisa M ; Wiltsie, Judyann ; Liu, Jinqi ; Gorski, Judith N ; Chung, Christine C ; Gibson, Jack T ; Lisnock, Jeanmarie ; Xiao, Jianying ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; Pinto, Shirly ; Nargund, Ravi P ; Devita, Robert JACS medicinal chemistry letters, 09 October 2014, Vol.5(10), pp.1082-7 [Peer Reviewed Journal]Full text available |
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Species differential stereoselective oxidation of a methylsulfide metabolite of MK-0767 (+/-)-5-(2,4-dioxothiazolidin-5-yl)methyl-2-methoxy-N-(4-trifluoromethyl)phenylmethylbenzamide, a peroxisome proliferator-activated receptor dual agonistKaranam, Bindhu V ; Welch, Christopher J ; Reddy, Vijay G ; Chilenski, Jennifer ; Biba, Mirlinda ; Vincent, StellaDrug metabolism and disposition: the biological fate of chemicals, October 2004, Vol.32(10), pp.1061-8 [Peer Reviewed Journal]Full text available |
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Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 DiabetesShah, Shrenik K ; He, Shuwen ; Guo, Liangqin ; Truong, Quang ; Qi, Hongbo ; Du, Wu ; Lai, Zhong ; Liu, Jian ; Jian, Tianying ; Hong, Qingmei ; Dobbelaar, Peter ; Ye, Zhixiong ; Sherer, Edward ; Feng, Zhe ; Yu, Yang ; Wong, Frederick ; Samuel, Koppara ; Madiera, Maria ; Karanam, Bindhu V ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Feng, Yue ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Eiermann, George J ; Li, Cai ; Pachanski, Michele ; Fernandez, Guillermo ; Nelson, Donald ; Bunting, Patricia ; Morissette, Pierre ; Volksdorf, Sylvia ; Kerr, Janet ; Zhang, Bei B ; Howard, Andrew D ; Zhou, Yun-Ping ; Pasternak, Alexander ; Nargund, Ravi P ; Hagmann, William KACS medicinal chemistry letters, 14 May 2015, Vol.6(5), pp.513-7 [Peer Reviewed Journal]Full text available |
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Material Type: Article
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In vitro metabolism of MK-0767 (+/-)-5-(2,4-dioxothiazolidin-5-yl)methyl-2-methoxy-N-(4-trifluoromethyl)-phenyl methylbenzamide, a peroxisome proliferator-activated receptor alpha/gamma agonist. II. Identification of metabolites by liquid chromatography-tandem mass spectrometryLiu, David Q ; Karanam, Bindhu V ; Doss, George A ; Sidler, Rick R ; Vincent, Stella H ; Hop, Cornelis E C ADrug metabolism and disposition: the biological fate of chemicals, September 2004, Vol.32(9), pp.1023-31 [Peer Reviewed Journal]Full text available |
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Material Type: Article
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Identification and metabolism of a novel dihydrohydroxy-S-glutathionyl conjugate of a peroxisome proliferator-activated receptor agonist, MK-0767 (+/-)-5-(2,4-dioxothiazolidin-5-yl)methyl-2-methoxy-N-(4-trifluoromethyl) phenylmethylbenzamide, in ratsReddy, Vijay Bhasker G ; Doss, George A ; Creighton, Mellissa ; Kochansky, Christopher J ; Vincent, Stella H ; Franklin, Ronald B ; Karanam, Bindhu VDrug metabolism and disposition: the biological fate of chemicals, October 2004, Vol.32(10), pp.1154-61 [Peer Reviewed Journal]Full text available |
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Material Type: Article
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In vitro metabolism of MK-0767 (+/-)-5-(2,4-dioxothiazolidin-5-yl)methyl-2-methoxy-N-(4-trifluoromethyl) phenylmethylbenzamide, a peroxisome proliferator-activated receptor alpha/gamma agonist. I. Role of cytochrome P450, methyltransferases, flavin monooxygenases, and esterasesKaranam, Bindhu V ; Hop, Cornelis E C A ; Liu, David Q ; Wallace, Mike ; Dean, Dennis ; Satoh, Hiroya ; Komuro, Masakatsu ; Awano, Katsuya ; Vincent, Stella HDrug metabolism and disposition: the biological fate of chemicals, September 2004, Vol.32(9), pp.1015-22 [Peer Reviewed Journal]Full text available |
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Mechanistic studies on the metabolic scission of thiazolidinedione derivatives to acyclic thiolsReddy, Vijay Bhasker G ; Karanam, Bindhu V ; Gruber, Wendy L ; Wallace, Michael A ; Vincent, Stella H ; Franklin, Ronald B ; Baillie, Thomas AChemical research in toxicology, May 2005, Vol.18(5), pp.880-8 [Peer Reviewed Journal]Full text available |
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Imidazopyridines: A novel class of hNa v1.7 channel blockersLondon, Clare ; Hoyt, Scott B ; Parsons, William H ; Williams, Brande S ; Warren, Vivien A ; Tschirret-Guth, Richard ; Smith, Mchardy M ; Priest, Birgit T ; Mcgowan, Erin ; Martin, William J ; Lyons, Kathryn A ; Li, Xiaohua ; Karanam, Bindhu V ; Jochnowitz, Nina ; Garcia, Maria L ; Felix, John P ; Dean, Brian ; Abbadie, Catherine ; Kaczorowski, Gregory J ; Duffy, Joseph LBioorganic & Medicinal Chemistry Letters, 2008, Vol.18(5), pp.1696-1701 [Peer Reviewed Journal]Full text available |
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Discovery of imidazole carboxamides as potent and selective CCK1R agonistsZhu, Cheng ; Hansen, Alexa R ; Bateman, Thomas ; Chen, Zhesheng ; Holt, Tom G ; Hubert, James A ; Karanam, Bindhu V ; Lee, Susan J ; Pan, Jie ; Qian, Su ; Reddy, Vijay B.G ; Reitman, Marc L ; Strack, Alison M ; Tong, Vincent ; Weingarth, Drew T ; Wolff, Michael S ; Macneil, Doug J ; Weber, Ann E ; Duffy, Joseph L ; Edmondson, Scott DBioorganic & Medicinal Chemistry Letters, 2008, Vol.18(15), pp.4393-4396 [Peer Reviewed Journal]Full text available |
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Material Type: Article
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Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activityAshton, Wallace T ; Sisco, Rosemary M ; Kieczykowski, Gerard R ; Yang, Yi Tien ; Yudkovitz, Joel B ; Cui, Jisong ; Mount, George R ; Ren, Rena Ning ; Wu, Tsuei-Ju ; Shen, Xiaolan ; Lyons, Kathryn A ; Mao, An-Hua ; Carlin, Josephine R ; Karanam, Bindhu V ; Vincent, Stella H ; Cheng, Kang ; Goulet, Mark TBioorganic & Medicinal Chemistry Letters, 2001, Vol.11(19), pp.2597-2602 [Peer Reviewed Journal]Full text available |
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Benzazepinone Na v1.7 blockers: Potential treatments for neuropathic painHoyt, Scott B ; London, Clare ; Ok, Hyun ; Gonzalez, Edward ; Duffy, Joseph L ; Abbadie, Catherine ; Dean, Brian ; Felix, John P ; Garcia, Maria L ; Jochnowitz, Nina ; Karanam, Bindhu V ; Li, Xiaohua ; Lyons, Kathryn A ; Mcgowan, Erin ; Macintyre, D. Euan ; Martin, William J ; Priest, Birgit T ; Smith, Mchardy M ; Tschirret-Guth, Richard ; Warren, Vivien A ; Williams, Brande S ; Kaczorowski, Gregory J ; Parsons, William HBioorganic & Medicinal Chemistry Letters, 2007, Vol.17(22), pp.6172-6177 [Peer Reviewed Journal]Full text available |
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2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chainYoung, Jonathan R ; Huang, Song X ; Walsh, Thomas F ; Wyvratt, Matthew J ; Yang, Yi Tien ; Yudkovitz, Joel B ; Cui, Jisong ; Mount, George R ; Ren, Rena Ning ; Wu, Tsuei-Ju ; Shen, Xiaolan ; Lyons, Kathryn A ; Mao, An-Hua ; Carlin, Josephine R ; Karanam, Bindhu V ; Vincent, Stella H ; Cheng, Kang ; Goulet, Mark TBioorganic & Medicinal Chemistry Letters, 2002, Vol.12(5), pp.827-832 [Peer Reviewed Journal]Full text available |
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Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC)Yu, Yang ; Wu, Zhicai ; Shi, Zhi-Cai ; He, Shuwen ; Lai, Zhong ; Cernak, Timothy A ; Vachal, Petr ; Liu, Min ; Liu, Jian ; Hong, Qingmei ; Jian, Tianying ; Guiadeen, Deodial ; Krikorian, Arto ; Sperbeck, Donald M ; Verras, Andreas ; Sonatore, Lisa M ; Murphy, Beth A ; Wiltsie, Judyann ; Chung, Christine C ; Gorski, Judith N ; Liu, Jinqi ; Xiao, Jianying ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; De Vita, Robert J ; Pinto, Shirly ; Nargund, Ravi PBioorganic & Medicinal Chemistry Letters, 01 June 2019, Vol.29(11), pp.1380-1385 [Peer Reviewed Journal]Full text available |
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Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moietyHe, Shuwen ; Lai, Zhong ; Hong, Qingmei ; Shang, Jackie ; Reibarkh, Mikhail ; Kuethe, Jeffrey T ; Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto D ; Cernak, Timothy A ; Dykstra, Kevin D ; Sperbeck, Donald M ; Wu, Zhicai ; Yu, Yang ; Yang, Ginger X ; Jian, Tianying ; Verras, Andreas ; Sonatore, Lisa M ; Wiltsie, Judyann ; Chung, Christine C ; Murphy, Beth A ; Gorski, Judith N ; Liu, Jinqi ; Xiao, Jianying ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; Pinto, Shirly ; Nargund, Ravi P ; Devita, Robert JBioorganic & Medicinal Chemistry Letters, 15 May 2019, Vol.29(10), pp.1182-1186 [Peer Reviewed Journal]Full text available |