Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Stephen T. Rapundalo"'
Autor:
Chad A. Van Huis, Jeremy J. Edmunds, Kenneth J. Shaw, Marc Whitlow, Arnaiz Damian O, Marc Adler, Cuiman Cai, David R. Light, Kamlai Saiya-Cork, J. Adam Willardsen, Lakshmi Narasimhan, Erli Zhang, Stephen T. Rapundalo, Kevin J. Filipski, Wayne L. Cody, Kirk Mclean, Danette Dudley, Jeffrey T. Kohrt, Cecile McKnight, Robert J. Leadley, Yuo-Ling Chou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4752-4756
The activated Factor VII/tissue factor complex (FVIIa/TF) plays a key role in the formation of blood clots. Inhibition of this complex may lead to new antithrombotic drugs. An X-ray crystal structure of a fluoropyridine-based FVIIa/TF inhibitor bound
Autor:
Stephen T. Rapundalo, J. Adam Willardsen, Thomas B. McClanahan, Thomas E. Mertz, Liguo Chi, Jeremy J. Edmunds, Wayne L. Cody, Debra R. Holland, Ronald E. Potoczak, Lakshmi Narasimhan, Danette Dudley
Publikováno v:
Journal of Medicinal Chemistry. 47:4089-4099
Factor Xa (FXa) has materialized as a key enzyme for the intervention of the blood coagulation cascade and for the development of new antithrombotic agents. FXa is the lone enzyme responsible for the production of thrombin and therefore is an attract
Autor:
Stephen T. Rapundalo, Joseph Macri
Publikováno v:
Trends in Cardiovascular Medicine. 11:66-75
Proteomics involves the integration of a number of technologies with the aim of analyzing the complete complement of proteins expressed by a biological system in response to various stimuli and/or under different physiological or pathophysiological c
Publikováno v:
Tetrahedron Letters. 41:6041-6044
A small molecule factor VIIa inhibitor has recently been reported by the Ono Pharmaceutical Company. Herein, we outline an efficient and convergent, synthetic route that relies upon a palladium-catalyzed Stille coupling reaction as a key step for the
Autor:
Greg W. Kilby, Tracy I. Stevenson, Beth McGee, Joseph Macri, John N. Thomas, Ping Du, Stephen T. Rapundalo
Publikováno v:
Electrophoresis. 21:1685-1693
We evaluated the use of the alkyaryl amidosulfobetaine zwitterionic detergent, designated as C8psi, to facilitate the solubilization of cardiac subcellular, membrane-associated proteins. Hearts from 7-week-old male Sprague-Dawley rats were isolated,
Autor:
Christine Humblet, Jeremy E. Edmunds, and M. Arshad Siddiqui, ‡ Yves St-Denis, Debra R. Holland, Janet S. Plummer, Lakshmi S. Narasimhan, Stephen T. Rapundalo, J. Ronald Rubin
Publikováno v:
Journal of Medicinal Chemistry. 43:361-368
We have studied the thrombin and trypsin complexed structures of a pair of peptidomimetic thrombin inhibitors, containing different P1 fragments. The first has arginine as its P1 fragment, and the second contains the constrained arginine mimic (2S)-2
Autor:
A. Susser, Peter D. Winocour, John DiMaio, Debra R. Holland, M. Arshad Siddiqui, Kent A. Berryman, Sophie Levesque, Janet S. Plummer, D. Lafleur, Jeremy J. Edmunds, Scott R. Eaton, J. Ronald Rubin, Annette Marian Doherty, Cuiman Cai, Wayne L. Cody, Stephen T. Rapundalo, Lakshmi S. Narasimhan, Yves St-Denis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:835-840
The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors are described. We have explored the SAR around the P1' site. Modification of the P1' site has been found to affect potency and selectivity.
Autor:
J. Ronald Rubin, Darin R. Kent, Debra R. Holland, John DiMaio, Yves St-Denis, Annette Marian Doherty, Sophie Levesque, Cuiman Cai, Peter D. Winocour, Jeremy J. Edmunds, M. Arshad Siddiqui, Lakshmi S. Narasimhan, Stephen T. Rapundalo, Janet S. Plummer, John X. He, Alan J. Susser, Kent A. Berryman, Wayne L. Cody
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3409-3414
The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors is described. We have explored the SAR with modifications to the P1 site. The introduction of arginine mimetics at the P1 site led to potent and selectiv
Proteomic analysis of hyperdynamic mouse hearts with enhanced sarcoplasmic reticulum calcium cycling
Autor:
Tracy I. Stevenson, Greg W. Kilby, Guoxiang Chu, Jaclyn P. Kerr, Evangelia G. Kranias, John E. Maggio, Meilan Shen, Gregory F. Egnaczyk, Bryan Mitton, Stephen T. Rapundalo, Jenny A. Vazquez, Jerry Vockley
Publikováno v:
The FASEB Journal. 18:1725-1727
Depressed sarcoplasmic reticulum (SR) Ca-cycling is a hallmark of human and experimental heart failure. Strategies to improve this impairment by either increasing SERCA2a levels or decreasing phospholamban (PLN) activity have been suggested as promis
Autor:
Kunchur Guruprasad, Chetana Rao-Naik, Brian L. Batley, Ben M. Dunn, Tom L. Blundell, John Kay, Jeffrey Hill, Stephen T. Rapundalo
Publikováno v:
Proteins: Structure, Function, and Genetics. 22:168-181
Aspartic proteinases are produced in the human body by a variety of cells. Some of these proteins, examples of which are pepsin, gastricsin, and renin, are secreted and exert their effects in the extracellular spaces. Cathepsin D and cathepsin E on t