Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Dean F. Rigel"'
Autor:
Dean F. Rigel, Gary M. Coppola, Frederic Villard, Li Fan, Muneto Mogi, Emma Cody, Nikolaus Schiering, Guiqing Liang, Christian Wiesmann, Arco Y. Jeng, Yongjin Gong, Jing Liu, Paul Ramage, Fumin Fu, Alan D. Neubert, Yuki Iwaki, Allan D'Arcy, Qian Liu, Wei Chen, Jennifer Leung-Chu, Robert Sun, Rajeshri Ganesh Karki, Frederic Cumin, Toshio Kawanami, Gary Michael Ksander, Sara Ingles, Michael E. Beil
Publikováno v:
ACS Med Chem Lett
[Image: see text] Inhibition of neprilysin (NEP) is widely studied as a therapeutic target for the treatment of hypertension, heart failure, and kidney disease. Sacubitril/valsartan (LCZ696) is a drug approved to reduce the risk of cardiovascular dea
Autor:
Dean F. Rigel, Berengere Dumotier, Brian Peter Richardson, Thomas Ullrich, Moise Azria, Estelle Lach-Trifilieff, Shinji Hatakeyama, David J. Glass, Julian Bösch, David A. Sykes, Michael Kiffe, Ngoc-Hong Nguyen, Jeffrey Tsao, Steven J. Charlton, Magdalena Koziczak-Holbro, Robin Alec Fairhurst, Marie Jourdain, Ludivine Flotte, Yuichiro Adachi
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 369:188-199
The anabolic effects of β2-adrenoceptor (β2-AR) agonists on skeletal muscle have been demonstrated in various species. However, the clinical use of β2-AR agonists for skeletal muscle wasting conditions has been limited by their undesired cardiovas
Autor:
Chi Hse Tang, Mathieu Peyrou, Jonathan P. Mochel, Meindert Danhof, Dean F. Rigel, Jérôme M. Giraudel
Publikováno v:
European Journal of Pharmaceutical Sciences. 128:103-111
Simultaneous blockade of angiotensin receptors and enhancement of natriuretic peptides (NP) by the first-in-class angiotensin receptor neprilysin (NEP) inhibitor sacubitril/valsartan constitutes an effective approach to treating heart failure. This s
Autor:
Dean F. Rigel, Hidetomo Imase, Kayo Yasoshima, Darcy Kohls, Toshio Kawanami, Yukiko I. Yagi, Jun Yuan, Monish Jain, Hyi-Man Park, Upendra A. Argikar, David Yowe, Paul Taslimi, Xiaoling Xie, Yuki Iwaki, Neeraja Idamakanti, Taeyong Yoon, Ken Yamada, Vidya Kunjathoor, Keith DiPetrillo, Lingfei Xu, Mitsunori Kato, Meicheng Zhu, Julian Levell, Zachary Robinson, Lauren G. Monovich
Publikováno v:
Journal of Medicinal Chemistry. 60:7099-7107
The observed structure-activity relationship of three distinct ATP noncompetitive With-No-Lysine (WNK) kinase inhibitor series, together with a crystal structure of a previously disclosed allosteric inhibitor bound to WNK1, led to an overlay hypothes
Autor:
Liang Jin, Dean F. Rigel, Bart A Ploeger, Donald R. Stanski, Randy L. Webb, Michael E. Beil, David Louis Feldman, Olivier Luttringer, Meindert Danhof, Nelleke Snelder, Fumin Fu
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 360:356-367
Sphingosine 1-phosphate (S1P) receptor agonists are associated with cardiovascular effects in humans. This study aims to develop a systems pharmacology model to identify the site of action (i.e., primary hemodynamic response variable) of S1P receptor
Autor:
Magdalena, Koziczak-Holbro, Dean F, Rigel, Bérengère, Dumotier, David A, Sykes, Jeffrey, Tsao, Ngoc-Hong, Nguyen, Julian, Bösch, Marie, Jourdain, Ludivine, Flotte, Yuichiro, Adachi, Michael, Kiffe, Moïse, Azria, Robin A, Fairhurst, Steven J, Charlton, Brian P, Richardson, Estelle, Lach-Trifilieff, David J, Glass, Thomas, Ullrich, Shinji, Hatakeyama
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 369(2)
The anabolic effects of
Autor:
Dean F. Rigel, Jérôme M. Giraudel, Meindert Danhof, Mathieu Peyrou, Chi Hse Tang, Jonathan P. Mochel
Simultaneous blockade of angiotensin receptors and enhancement of natriuretic peptides (NP) by the first-in-class angiotensin receptor neprilysin (NEP) inhibitor sacubitril/valsartan constitutes an effective approach to treating heart failure. This s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92933c3685d1decf791bedbaae9cb947
Autor:
Dean F. Rigel, Kerry S. Russell, Lu Gan, Julien Papillon, Chii-Whei Hu, Changgang Lou, Alok K. Singh, Daniel LaSala, Wei Chen, Gary Michael Ksander, Fumin Fu, Catherine Watson, Jennifer Leung-Chu, Arco Y. Jeng, Christopher M. Adams, Guiqing Liang, John A. Vest, Michael E. Beil
Publikováno v:
Journal of Medicinal Chemistry. 58:9382-9394
Human clinical studies conducted with LCI699 established aldosterone synthase (CYP11B2) inhibition as a promising novel mechanism to lower arterial blood pressure. However, LCI699's low CYP11B1/CYP11B2 selectivity resulted in blunting of adrenocortic
Autor:
Ichiro Umemura, Hironobu Mitani, Ken Yamada, Guoming Zhu, Meihui Pan, Yuki Iwaki, Daniel LaSala, Dean F. Rigel, Akiko Iimura, Kayo Yasoshima, Kazuhiko Nonomura, Hidetomo Imase, Guiqing Liang, Osamu Ohmori, Margaret E. Brousseau, Muneto Mogi, Wataru Honma, Toshio Kawanami
Publikováno v:
Journal of medicinal chemistry. 60(20)
Herein we describe the discovery and characterization of a novel, piperidine-based inhibitor of cholesteryl ester transfer protein (CETP) with a core structure distinct from other reported CETP inhibitors. A versatile synthesis starting from 4-methox
Autor:
Shimpei Kawakami, Nikolaus Schiering, Takeru Ehara, Fumiaki Yokokawa, Hiroki Gunji, Takanori Kanazawa, Kazuhide Konishi, Takatoshi Kosaka, Yuko Hitomi, Frederic Cumin, Osamu Irie, Nils Ostermann, Trixie Wagner, Philipp Grosche, Masaki Suzuki, Werner Breitenstein, Dean F. Rigel, Randy L. Webb, Atsushi Toyao, Jürgen Maibaum
Publikováno v:
ACS Medicinal Chemistry Letters. 5:787-792
A cis-configured 3,5-disubstituted piperidine direct renin inhibitor, (syn,rac)-1, was discovered as a high-throughput screening hit from a target-family tailored library. Optimization of both the prime and the nonprime site residues flanking the cen