Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Jothirajah Marimuthu"'
Autor:
Kannan Thirunavukkarasu, Mark Chambers, Daniel R. Mudra, Michael Robert Wiley, Craig A. Swearingen, Lisa A. Adams, Timothy B. Durham, Jothirajah Marimuthu, C. Lin, James Lee Toth, Chin Liu
Publikováno v:
Journal of Medicinal Chemistry. 60:5933-5939
Aggrecanase-1 and -2 (ADAMTS-4 and ADAMTS-5) are zinc metalloproteases involved in the degradation of aggrecan in cartilage. Inhibitors could provide a means of altering the progression of osteoarthritis. We report the identification of 7 which had g
Autor:
Kannan Thirunavukkarasu, Mark Chambers, Daniel R. Mudra, Craig A. Swearingen, Lisa A. Adams, Jennifer M. Weller, P.G. Mitchell, Timothy B. Durham, Chin Liu, C. Lin, James Lee Toth, Michael Robert Wiley, Jothirajah Marimuthu
Publikováno v:
Journal of Medicinal Chemistry. 59:5810-5822
The development of reliable relationships between in vivo target engagement, pharmacodynamic activity, and efficacy in chronic disease models is beneficial for enabling hypothesis-driven drug discovery and facilitating the development of patient-focu
Autor:
C. Lin, Chin Liu, Valentine J. Klimkowski, Craig A. Swearingen, Lisa A. Adams, Stephanie L. Stout, Timothy B. Durham, Michael Robert Wiley, Kannan Thirunavukkarasu, Mark Chambers, Jim D. Durbin, Christopher John Rito, Jothirajah Marimuthu, James Lee Toth
Publikováno v:
Journal of Medicinal Chemistry. 57:10476-10485
A disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) and ADAMTS-5 are zinc metalloproteases commonly referred to as aggrecanase-1 and aggrecanase-2, respectively. These enzymes are involved in the degradation of aggrecan, a key
Autor:
C. Lin, Michael Robert Wiley, Kannan Thirunavukkarasu, Mark Chambers, P.G. Mitchell, Christopher John Rito, Chin Liu, Craig A. Swearingen, Timothy B. Durham, Jothirajah Marimuthu, Dotzlaf Joe Edward, Quincy L. Carter, Srinivasan Chandrasekhar, Kevin L. Duffin
Publikováno v:
Osteoarthritis and Cartilage. 18:1159-1166
Summary Objective To develop a short-term in vivo model in rats, with an enzyme-linked immunosorbent assay (ELISA) readout for specific aggrecanase-cleaved aggrecan fragments, to facilitate testing of aggrecanase inhibitors. Methods Monosodium iodoac
Autor:
Scott Martin Sheehan, Nikolay Y. Chirgadze, Gerald F. Smith, Jolie Anne Bastian, Michael Robert Wiley, Trelia J. Craft, Daniel Jon Sall, Jeffrey K. Smallwood, Jothirajah Marimuthu, John Walter Nr Macclesfield Liebeschuetz, Marcia K. Chastain, Philip Sipes, Jeffry Bernard Franciskovich, Brian Morgan Watson, Ronald S. Foster, Valentine J. Klimkowski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5801-5805
Analogs to a series of D-phenylglycinamide-derived factor Xa inhibitors were discovered. It was found that the S4 amide linkage can be replaced with an ether linkage to reduce the peptide character of the molecules and that this substitution leads to
Autor:
Jothirajah Marimuthu, Mark W. Farmen, Wayne W. Weber, Stuart Donald Jones, Kyle Ja, Michael Robert Wiley, John Walter Liebeschuetz, David Birenbaum Engel, Jeffrey K. Smallwood, Jeffrey B. Franciskovich, Christopher W. Murray, John Joseph Masters, Gerald F. Smith, Scott Martin Sheehan, Stephen Clinton Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2255-2259
A novel isonitrile derivative was synthesized and used in an Ugi four component coupling reaction to explore aryl group substitution effects on inhibition of the coagulation cascade serine protease factor Xa.
Autor:
Robert W. Siegel, Dotzlaf Joe Edward, John W. Carpenter, Dawn P. G. Brown, Chin Liu, P.G. Mitchell, Michael Robert Wiley, Kannan Thirunavukkarasu, D. A. Laska, Jothirajah Marimuthu, Quincy L. Carter, I.J. Brittain, Craig A. Swearingen, James Lee Toth, Timothy B. Durham, Kevin L. Duffin
Publikováno v:
Osteoarthritis and cartilage. 18(9)
Summary Objective Proteolytic degradation of aggrecan in articular cartilage is a hallmark feature of osteoarthritis (OA). The present study was aimed at developing a sensitive enzyme linked immunosorbent assay (ELISA) for the detection of aggrecanas