Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Koppara, Samuel"'
Autor:
Alexei V. Buevich, Cyndi Qixin He, Barbara Pio, Koppara Samuel, Kaushik Mitra, Edward C. Sherer, Mark T. Cancilla, Harry R. Chobanian
Publikováno v:
Chemical Research in Toxicology. 35:459-474
Acyl glucuronide (AG) metabolites of carboxylic acid-containing drugs and products of their transformations have long been implicated in drug-induced liver injury (DILI). To inform on the DILI risk arising from AG reactive intermediates, a comprehens
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aee89dbb279ea38c06843b7ee0b86434
https://doi.org/10.1021/acs.chemrestox.1c00366
https://doi.org/10.1021/acs.chemrestox.1c00366
Autor:
Barbara Pio, Ravi P. Nargund, Yan Guo, Daniel Kosinski, Josien Hubert B, Michael Wright, Michele Pachanski, Harry R. Chobanian, Xiaoping Zhang, Richard Tschirret-Guth, Melissa Kirkland, Andrew D. Howard, Sarah Souza, Eric R. Ashley, Robert K. Orr, Steven L. Colletti, Joel Mane, Jerry Di Salvo, Michael W. Miller, Boonlert Cheewatrakoolpong, Koppara Samuel, William K. Hagmann, James Lamca, Juliann Ehrhart, Maria E. Trujillo, Jackie Shang, Qing Chen, Adam B. Weinglass, Randal M. Bugianesi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1842-1848
GPR40 (FFAR1 or FFA1) is a G protein-coupled receptor, primarily expressed in pancreatic islet β-cells and intestinal enteroendocrine cells. When activated by fatty acids, GPR40 elicits increased insulin secretion from islet β-cells only in the pre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67130fd906c302e54806df711af08d1b
https://doi.org/10.1016/j.bmcl.2019.04.050
https://doi.org/10.1016/j.bmcl.2019.04.050
Autor:
Xin Gu, Brande Thomas-Fowlkes, Dorothy Levorse, Harry R. Chobanian, Timothy Cutarelli, Alexander Pasternak, Adam B. Weinglass, Ian W. Davies, Martin Koehler, Michael Margulis, Fa-Xiang Ding, Joel B. Yudkovitz, Jinlong Jiang, Haifeng Tang, Lee-Yuh Pai, Barbara Pio, Shuzhi Dong, Mengwei Hu, Kathleen A. Sullivan, Jack Gibson, Thomas Bateman, Koppara Samuel, Xiaoyan Zhou, Caryn Hampton, Reynalda deJesus, Kevin Houle, Emma R. Parmee
Publikováno v:
Journal of medicinal chemistry. 64(11)
A renal outer medullary potassium channel (ROMK, Kir1.1) is a putative drug target for a novel class of diuretics with potential for treating hypertension and heart failure. Our first disclosed clinical ROMK compound, 2 (MK-7145), demonstrated robust
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07c25db7e0321a07221c83e7a37add1c
https://pubmed.ncbi.nlm.nih.gov/34038119
https://pubmed.ncbi.nlm.nih.gov/34038119
Autor:
Koppara Samuel, Dan Tatosian, Maria Caceres, Shiyao Xu, Sanjeev Kumar, Ian Mcintosh, Diana Selverian, Eunkyung Kauh, Catherine Z. Matthews
Publikováno v:
Xenobiotica. 48:584-591
1. Omarigliptin (MARIZEV®) is a once-weekly DPP-4 inhibitor approved in Japan for the treatment of type 2 diabetes. The objective of this study was to investigate the absorption, metabolism and excretion of omarigliptin in humans. 2. Six healthy sub
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b163c3d547cfc1bb1897b3db6ca86a85
https://doi.org/10.1080/00498254.2017.1346333
https://doi.org/10.1080/00498254.2017.1346333
Autor:
Alexei V. Buevich, Richard A. Tschirret-Guth, Mark T. Cancilla, Josien Hubert B, Qing Chen, Koppara Samuel, Ann Thomas, Wei Tong, Harry R. Chobanian, Kaushik Mitra, Jackie Shang
Publikováno v:
Chemical research in toxicology. 33(1)
MK-8666, a selective GPR40 agonist developed for the treatment of type 2 diabetes mellitus, was discontinued in phase I clinical trials due to liver safety concerns. To address whether chemically reactive metabolites played a causative role in the ob
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8e042e02e861ca7bcbc70f5f6208ca9
https://pubmed.ncbi.nlm.nih.gov/31566356
https://pubmed.ncbi.nlm.nih.gov/31566356
Autor:
Shiyao, Xu, Dan, Tatosian, Ian, Mcintosh, Maria, Caceres, Catherine, Matthews, Koppara, Samuel, Diana, Selverian, Sanjeev, Kumar, Eunkyung, Kauh
Publikováno v:
Xenobiotica; the fate of foreign compounds in biological systems. 48(6)
1. Omarigliptin (MARIZEV®) is a once-weekly DPP-4 inhibitor approved in Japan for the treatment of type 2 diabetes. The objective of this study was to investigate the absorption, metabolism and excretion of omarigliptin in humans. 2. Six healthy sub
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::007d770f114e670f51370c3fa5b4127d
https://pubmed.ncbi.nlm.nih.gov/28665228
https://pubmed.ncbi.nlm.nih.gov/28665228
Autor:
Donald Nelson, Gary G. Chicchi, James Dellureficio, Ravi P. Nargund, Peter H. Dobbelaar, Liangqin Guo, Kwei-Lan Tsao, Janet S. Kerr, Bei Zhang, Zhong Lai, Patricia R. Bunting, Shrenik K. Shah, Raman K. Bakshi, Qingmei Hong, Hongbo Qi, Guillermo Fernandez, Mikhail Reibarkh, Qing Shao, Quang Truong, Koppara Samuel, Jian Liu, Sylvia Volksdorf, Zhixiong Ye, Yun-Ping Zhou, Margaret Wu, Cai Li, Stan Mitelman, Andrew D. Howard, Wu Du, Maria E. Trujillo, George J. Eiermann, Shuwen He, Vijay Bhasker G. Reddy, Tianying Jian, Pierre Morissette, Patrick Fitzgerald, Dorina Trusca, Sharon Tong, William K. Hagmann
Publikováno v:
ACS Medicinal Chemistry Letters. 5:748-753
Antagonism of somatostatin subtype receptor 3 (sstr3) has emerged as a potential treatment of Type 2 diabetes. Unfortunately, the development of our first preclinical candidate, MK-4256, was discontinued due to a dose-dependent QTc (QT interval corre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ced576c72131916fe1527dabb0d36e73
https://doi.org/10.1021/ml500028c
https://doi.org/10.1021/ml500028c
Autor:
David Wilson, Bindhu V. Karanam, Mona Purcell, Maria Madeira, Gary G. Chicchi, Jianming Bao, Liza Gantert, Robert J. DeVita, Huagang Lu, Wai-Si Eng, Sander G. Mills, Richard G. Ball, Andrew J. Kassick, Peter Lin, Sanjeev Kumar, Jaime Lynn Bunda, George A. Doss, Kwei-Lan C. Tsao, Jacquelyn J. Cook, Xinchun Tong, Richard Tschirret-Guth, Jinlong Jiang, Koppara Samuel, Richard Hargreaves, Hong Wang, Donald F. Hora
Publikováno v:
Journal of Medicinal Chemistry. 56:5940-5948
Hydroisoindoline 2 has been previously identified as a potent, brain-penetrant NK1 receptor antagonist with a long duration of action and improved profile of CYP3A4 inhibition and induction compared to aprepitant. However, compound 2 is predicted, ba
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::94febe29ddadade1fbafbe0e7e0c71d3
https://doi.org/10.1021/jm400751p
https://doi.org/10.1021/jm400751p
Autor:
Janet Kerr, Gary G. Chicchi, Margaret Wu, Cai Li, Shuwen He, Vijay Bhasker G. Reddy, Sharon Tong, William K. Hagmann, Patrick Fitzgerald, Guillermo Fernandez, Andrew D. Howard, Tianying Jian, Zhe Feng, Raman K. Bakshi, Dorina Trusca, Peter H. Dobbelaar, Donald Nelson, Mikhail Reibarkh, Qing Shao, Liangqin Guo, Yun-Ping Zhou, Ravi P. Nargund, Kwei-Lan Tsao, Edward C. Sherer, Stan Mitelman, Pierre Morissette, Maria E. Trujillo, Quang Truong, Zhixiong Ye, James D. Dellureficio, Hongbo Qi, Melissa Lin, Shrenik K. Shah, Sylvia Volksdorf, Jian Liu, Qingmei Hong, Koppara Samuel, Alexander Pasternak, George J. Eiermann, Patricia B. Bunting, Wu Du, Bei B. Zhang
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(6)
MK-4256, a tetrahydro-β-carboline sstr3 antagonist, was discontinued due to a cardiovascular (CV) adverse effect observed in dogs. Additional investigations revealed that the CV liability (QTc prolongation) was caused by the hERG off-target activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6412732d83fd31156d7974bed1994494
https://pubmed.ncbi.nlm.nih.gov/26898814
https://pubmed.ncbi.nlm.nih.gov/26898814
Autor:
Nathan X. Yu, Thomas J. Lanza, Koppara Samuel, Sanjeev Kumar, George A. Doss, Vijay Bhasker G. Reddy, Ralph A. Stearns, Bindhu V. Karanam, Linus S. Lin, Conrad E. Raab, Andy Shiqiang Zhang
Publikováno v:
Xenobiotica. 40:650-662
The metabolism and excretion of taranabant (MK-0364, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2{[5-(trifluoromethyl)pyridine-2-yl]oxy}propanamide), a potent cannabinoid-1 receptor inverse agonist, were evaluated in rat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::018365d6fb66bbbdd95a6bcd0041c218
https://doi.org/10.3109/00498254.2010.501117
https://doi.org/10.3109/00498254.2010.501117