Zobrazeno 1 - 10
of 61
pro vyhledávání: '"Margarita Garcia-Calvo"'
Autor:
Ji Zhang, Tao Wang, Ashmita Saigal, Josephine Johnson, Jennifer Morrisson, Sahba Tabrizifard, Scott A. Hollingsworth, Michael J. Eddins, Wenxian Mao, Kim O’Neill, Margarita Garcia-Calvo, Ester Carballo-Jane, DingGang Liu, Taewon Ham, Qiong Zhou, Weifeng Dong, Hsien-Wei Meng, Jacqueline Hicks, Tian-Quan Cai, Taro Akiyama, Shirly Pinto, Alan C. Cheng, Thomas Greshock, John C. Marquis, Zhao Ren, Saswata Talukdar, Hussam Hisham Shaheen, Masahisa Handa
Publikováno v:
Scientific Reports, Vol 11, Iss 1, Pp 1-15 (2021)
Abstract Lung fibrosis, or the scarring of the lung, is a devastating disease with huge unmet medical need. There are limited treatment options and its prognosis is worse than most types of cancer. We previously discovered that MK-0429 is an equipote
Externí odkaz:
https://doaj.org/article/3c77d995775e4a3aa500d4b475ea8591
Autor:
Mollie Ranalletta, Kathleen K. Bierilo, Ying Chen, Denise Milot, Qing Chen, Elaine Tung, Caroline Houde, Nadine H. Elowe, Margarita Garcia-Calvo, Gene Porter, Suzanne Eveland, Betsy Frantz-Wattley, Mike Kavana, George Addona, Peter Sinclair, Carl Sparrow, Edward A. O'Neill, Ken S. Koblan, Ayesha Sitlani, Brian Hubbard, Timothy S. Fisher
Publikováno v:
Journal of Lipid Research, Vol 51, Iss 9, Pp 2739-2752 (2010)
Cholesteryl ester transfer protein (CETP) has been identified as a novel target for increasing HDL cholesterol levels. In this report, we describe the biochemical characterization of anacetrapib, a potent inhibitor of CETP. To better understand the m
Externí odkaz:
https://doaj.org/article/ba8f1fa1fd444c148814f2a249643d10
Autor:
Sahba Tabrizifard, Hussam Hisham Shaheen, Margarita Garcia-Calvo, Jennifer Morrisson, Jacqueline D. Hicks, Michael J. Eddins, Zhao Ren, Ashmita Saigal, Josephine Johnson, Weifeng Dong, DingGang Liu, Masahisa Handa, Kim O’Neill, Taro E. Akiyama, Thomas J. Greshock, Wenxian Mao, Ester Carballo-Jane, Hsien-Wei Yvonne Meng, Tian-Quan Cai, Scott A. Hollingsworth, Saswata Talukdar, Qiong Zhou, John C. Marquis, Ji Zhang, Alan C. Cheng, Tao Wang, Shirly Pinto, Taewon Ham
Publikováno v:
Scientific Reports
Scientific Reports, Vol 11, Iss 1, Pp 1-15 (2021)
Scientific Reports, Vol 11, Iss 1, Pp 1-15 (2021)
Lung fibrosis, or the scarring of the lung, is a devastating disease with huge unmet medical need. There are limited treatment options and its prognosis is worse than most types of cancer. We previously discovered that MK-0429 is an equipotent pan-in
Autor:
Rui Liang, Xuelei Song, Sheng-Ping Wang, Gino Salituro, Dave G. McLaren, Larissa Wilsie, Ming You, Steven J. Stout, Zhe Feng, Shirly Pinto, Dong-Ming Shen, Ken Marby, Yusheng Xiong, Jim Tata, Timothy He, Andrew K.P. Taggart, Beth Ann Murphy, Margarita Garcia-Calvo, Brian K. Hubbard, Clare London, Oksana C. Palyha, Jason E. Imbriglio, Andreas Verras, Hye Won Youm, Xiaoling Jin, Diana Deckman, Seongah Han, George H. Addona, Qing Chen, Stephen F. Previs, Dan E. Metzger
Publikováno v:
Journal of Medicinal Chemistry. 58:9345-9353
DGAT2 plays a critical role in hepatic triglyceride production, and data suggests that inhibition of DGAT2 could prove to be beneficial in treating a number of disease states. This article documents the discovery and optimization of a selective small
Autor:
Elizabeth Smith, Robin E. Haimbach, Li-Jun Ma, Olga Price, David E. Kelley, Yonghua Zhu, Ji Zhang, Yanqing Kan, Xiaoyan Zhou, Margarita Garcia-Calvo, Shirly Pinto, Wei Zhu, Emanuel Zycband, Jason M. Cox, Rosemary Mayer-Ezell, Maarten Hoek
Publikováno v:
Pharmacology Research & Perspectives
Multiple integrins have been implicated in modulating renal function. Modulation of integrin function can lead to pathophysiological processes associated with diabetic nephropathy such as alterations in the glomerular filtration barrier and kidney fi
Autor:
Yong Zhang, Jeffrey J. Hale, Andreas Verras, Shirly Pinto, Huaibing He, Zhu Shen, Urmi R. Bhatt, Elaine C. Tung, John S. Debenham, Matthew J. Clements, Dunlu Chen, Dong-Ming Shen, Wayne M. Geissler, Thomas H. Graham, JeanMarie Lisnock, Qing Chen, Suoyu Xu, Xiaohua Li, Margarita Garcia-Calvo, Wensheng Liu, Xinchun Tong, Judyann Wiltsie, Christina B. Madsen-Duggan, Jeffrey T. Kuethe
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6228-6233
The synthesis, SAR, binding affinities and pharmacokinetic profiles are described for a series of cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors discovered by high throughput screening. Compounds show high levels of ex vivo target engagem
Autor:
Gaochao Zhou, Judyann Wiltsie, Jason M. Cox, Lisa Contino, Jaume Balsells, Martin Crook, Ling Xu, Joseph Clemas, Hong D. Chu, JeanMarie Lisnock, Jack Gibson, Christine Yang, Thomas Bateman, Zhicai Wu, Peter J. Sinclair, Beata Zamlynny, Hong C. Shen, Margarita Garcia-Calvo, Xinchun Tong, Alejandro Crespo, Patricia Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4388-4392
Novel oxazolidinedione analogs were discovered as potent and selective mineralocorticoid receptor (MR) antagonists. Structure–activity relationship (SAR) studies were focused on improving the potency and microsomal stability. Selected compounds dem
Autor:
Xinchun Tong, Kun Liu, Margarita Garcia-Calvo, Lisa Contino, Joseph Clemas, Ellen K. Vande Bunte, Gaochao Zhou, Judyann Wiltsie, JeanMarie Lisnock, Patricia Brown, Dennis Leung, Peter J. Sinclair, Yi Pan, Xiuying Ma, Jack Gibson, Zhongxiang Sun, Ling Xu, Alejandro Crespo, Thomas Bateman, Anthony Ogawa, Nina Jochnowitz, Martin Crook, Ping Lan, Rudrajit Mal, Beata Zamlynny
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(12)
Reported herein are a series of reverse indoles that represent novel non-steroidal mineralocorticoid receptor (MR) antagonists. The key structure–activity relationships (SAR) are presented below. This reverse indole series is exemplified by a compo
Autor:
Fa-Xiang Ding, Urmi R. Bhatt, Hong C. Shen, Wayne M. Geissler, Judith N. Gorski, Ranabir SinhaRoy, Margarita Garcia-Calvo, Jinlong Jiang, Xinchun Tong, Renee M. Chabin, Beth Ann Murphy, Dong-Ming Shen, Shirly Pinto, Jeffrey J. Hale, Dan Xie, Andreas Verras, Mike E. Lassman, Qing Chen, Suoyu Xu, Judyann Wiltsie, Zhu Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1550-1556
A series of benzodihydroisofurans were discovered as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase (PrCP) inhibitors. The structure–activity relationship (SAR) is focused on improving PrCP activity and metabolic stability,
Autor:
Thomas H. Graham, Urmi R. Bhatt, Dong-Ming Shen, Xinchun Tong, Mike E. Lassman, Kelly Bleasby, Dan Xie, Qing Chen, Shirly Pinto, Margarita Garcia-Calvo, Andreas Verras, Renee M. Chabin, Zhicai Wu, Steven L. Colletti, Suoyu Xu, Cangming Yang, James R. Tata, Zhu Shen, Ranabir SinhaRoy, Jeffrey J. Hale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1727-1730
Efforts were dedicated to develop potent and brain penetrant prolylcarboxypeptidase (PrCP) inhibitors by replacing the amide group of original leads 1 and 2 with heterocycles. Aminopyrimidines including compound 32a were identified to display good Pr