Zobrazeno 1 - 10
of 37
pro vyhledávání: '"Alfred P. Spada"'
Autor:
Diana Hide, Jordi Gracia-Sancho, Zoe Boyer-Diaz, Anabel Fernández-Iglesias, Alfred P. Spada, Raquel Maeso-Díaz, Sergi Guixé-Muntet, Nicolò Manicardi, Patricia C. Contreras, Héctor García-Calderó, Martí Ortega-Ribera, Jaime Bosch
Publikováno v:
Hepatology Communications
Hepatology Communications, Vol 3, Iss 7, Pp 987-1000 (2019)
Gracia-Sancho, Jordi; Manicardi, Nicolò; Ortega-Ribera, Martí; Maeso-Díaz, Raquel; Guixé Muntet, Sergi; Fernández-Iglesias, Anabel; Hide, Diana; García-Calderó, Héctor; Boyer-Díaz, Zoe; Contreras, Patricia C; Spada, Alfred; Bosch, Jaime (2019). Emricasan Ameliorates Portal Hypertension and Liver Fibrosis in Cirrhotic Rats Through a Hepatocyte-Mediated Paracrine Mechanism. Hepatology communications, 3(7), pp. 987-1000. 10.1002/hep4.1360
Hepatology Communications, Vol 3, Iss 7, Pp 987-1000 (2019)
Gracia-Sancho, Jordi; Manicardi, Nicolò; Ortega-Ribera, Martí; Maeso-Díaz, Raquel; Guixé Muntet, Sergi; Fernández-Iglesias, Anabel; Hide, Diana; García-Calderó, Héctor; Boyer-Díaz, Zoe; Contreras, Patricia C; Spada, Alfred; Bosch, Jaime (2019). Emricasan Ameliorates Portal Hypertension and Liver Fibrosis in Cirrhotic Rats Through a Hepatocyte-Mediated Paracrine Mechanism. Hepatology communications, 3(7), pp. 987-1000. 10.1002/hep4.1360
In cirrhosis, liver microvascular dysfunction is a key factor increasing hepatic vascular resistance to portal blood flow, which leads to portal hypertension. De-regulated inflammatory and pro-apoptotic processes due to chronic injury play important
Publikováno v:
Toxicological Sciences. 162:396-405
Tissue factor (TF) is the primary activator of the blood coagulation cascade. Liver parenchymal cells (ie, hepatocytes) express TF in a molecular state that lacks procoagulant activity. Hepatocyte apoptosis is an important feature of acute and chroni
Autor:
Alfred P. Spada, Gavin Wright, Gautam Mehta, Matthew C. Cave, Rajiv Jalan, Mark Morris, Catherine Frenette, David T. Hagerty, Sam Rousell, Stuart McPherson, Gary Burgess
Background Cirrhosis and acute-on-chronic liver failure (ACLF) are associated with systemic inflammation, and caspase-mediated hepatocyte cell death. Emricasan is a novel, pan-caspase inhibitor. Aims of this study were to assess the pharmacokinetics,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f344bbaa5d9064e2d7a69774a5e4b34
https://europepmc.org/articles/PMC6175779/
https://europepmc.org/articles/PMC6175779/
Autor:
Jean L. Chan, Raymond A. Rubin, Alfred P. Spada, Giuseppe Morelli, Matthew C. Cave, Jason T. Cheng, Catherine Frenette, R. Todd Frederick, Saira Khaderi, Mason Yamashita, Michael B. Fallon, James S. Park, David T. Hagerty, James M. Robinson, Nikolaos Pyrsopoulos, Mitchell L. Shiffman, Omar Massoud
Publikováno v:
Clinical Gastroenterology and Hepatology. 17:774-783.e4
Caspase-mediated apoptosis and inflammation contribute to progression of liver disease. Emricasan is a pan-caspase inhibitor that reduced serum markers of apoptosis and liver inflammation in patients with hepatitis C and non-alcoholic steatohepatitis
Autor:
Kevin J. Tomaselli, Julia Herrmann, Robert O. Sayers, Joe C. Wu, Lalitha Kodandapani, Kathy G. Jahangiri, Craig D. Fisher, David T. Winn, Edward D. Robinson, Steven P. Meduna, Robert J. Ternansky, Pauline Yeo, Karen L. Valentino, Jose-Luis Diaz, Vincent J. Kalish, Steven D. Linton, Kristen Sebring, Robert A. Armstrong, Joseph F. Krebs, Niel C. Hoglen, Alfred P. Spada, Brad P. Hirakawa, Ning Chen, Brett R. Ullman, Brett Weylan Ching, Cheng-zhi Zhang, Xu Bai, Xin Gu, Kip Nalley, Long-Shiuh Chen, Patricia L. Gladstone, Jeff McQuiston, Teresa Aja, Todd Groessl, Donald S. Karanewsky, Suzanne Weeks, Lawrence C. Fritz, Patricia C. Contreras
Publikováno v:
Journal of Medicinal Chemistry. 48:6779-6782
A series of oxamyl dipeptides were optimized for pan caspase inhibition, anti-apoptotic cellular activity and in vivo efficacy. This structure-activity relationship study focused on the P4 oxamides and warhead moieties. Primarily on the basis of in v
Autor:
Mason Helen J, Karen D. Brown, Valeria Chu, Guyan Liang, Daniel M. Green, Alfred P. Spada, Henry W. Pauls, Ross Bentley, Cuong Ly, Roderick S. Davis, Dennis J. Colussi, Daniel L. Cheney, Michael R. Becker, Y.M. Choi-Sledeski, Christopher T. Dunwiddie, Robert J. Leadley, Ewing William R, John H. Barton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2539-2544
The design, synthesis and SAR of sulfonamidopyrrolidinone fXa inhibitors incorporating a new benzamidine isostere, namely aminoisoquinolines, is described. These inhibitors have higher Caco-2 cell permeability than comparable benzamidines and attain
Autor:
Alfred P. Spada, Robert J. Leadley, Jonathan S. Mason, Dennis J. Colussi, Ewing William R, Mark H. Perrone, Karen D. Brown, Michael R. Becker, Don D. Cha, Daniel M. Green, Ross Bentley, Henry W. Pauls, Christopher T. Dunwiddie, Jean-Pierre Guilloteau, Y.M. Choi-Sledeski, Sebastien Maignan, Mason Helen J, Vincent E. Manetta, Charles Kasiewski, Valeria Chu, Roderick S. Davis, Suzanne Morgan, Daniel L. Cheney, Jeff Bostwick
Publikováno v:
Journal of Medicinal Chemistry. 42:3557-3571
The discovery of a series of non-peptide factor Xa (FXa) inhibitors incorporating 3-(S)-amino-2-pyrrolidinone as a central template is described. After identifying compound 4, improvements in in vitro potency involved modifications of the liphophilic
Autor:
Robert J. Leadley, Charles Kasiewski, Tara Wentz, Glenda E. Bilder, Jeffery Bostwick, Mark H. Perrone, Saul J. Needle, Betsey O’Conner, Christopher T. Dunwiddie, Lisa Byan, Kenneth Page, Helen Galczenski, Linda Merkel, Persons Paul E, Myers Michael R, Alfred P. Spada, Amin Dilip, Cuong Ly
Publikováno v:
Circulation. 99:3292-3299
Background —Platelet-derived growth factor (PDGF), a purported mediator of arterial response to injury, stimulates proliferation, chemotaxis, and matrix production by activation of its membrane receptor tyrosine kinase. Because these activities und
Autor:
Ewing William R, Robert J. Leadley, Alfred P. Spada, Mark H. Perrone, Christopher T. Dunwiddie, S. Morgan, Henry W. Pauls, Valeria Chu, Jeffrey S. Bostwick, Karen D. Brown, Ross Bentley
Publikováno v:
Thrombosis and Haemostasis. 81:157-160
SummaryThe in vivo antithrombotic activity of RPR120844, a novel synthetic coagulation factor Xa (fXa) inhibitor (Ki = 7 nM), was assessed by its ability to inhibit thrombus formation in a damaged segment of the rabbit jugular vein. Intravenous dose-
Autor:
Alfred P. Spada, Mark H. Perrone, Fink Cynthia A, Kenneth L. Clark, Bryan F. Cox, Michael F. Jarvis, Glenn J. Smits, Camilo J. Rojas, Linda Merkel
Publikováno v:
Drug Development Research. 45:30-43
AMP 579 1S-[1α,2β,3β,4α(S*)]-4-[7-[[1 -[(3-chloro-2-thienyl)methyl]propylamino]-3H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxy cyclopentanecarboxamide) is a novel cardioprotective adenosine agonist with the following order of affinity at ad