Zobrazeno 1 - 10
of 61
pro vyhledávání: '"James M, Trevillyan"'
Autor:
Bradley J. Backes, Bryan F. Cox, Ryan M. Fryer, P N Banfor, Stephen J. Ballaron, D L Widomski, James M. Trevillyan, Jason A. Segreti, T.W. von Geldern, Chun W. Lin, Glenn A. Reinhart
Publikováno v:
British Journal of Pharmacology. 153:947-955
Background and purpose: Inhibition of bradykinin metabolizing enzymes (BMEs) can cause acute angioedema, as demonstrated in a recent clinical trial in patients administered the antihypertensive, omapatrilat. However, the relative contribution of spec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b207da8ed1bcbee1fabaffa6b126cf3a
https://doi.org/10.1038/sj.bjp.0707641
https://doi.org/10.1038/sj.bjp.0707641
Autor:
Stevan W. Djuric, Kennan C. Marsh, Gin C. Hsieh, Michael P. Sheets, Yung-Wu Chen, Thomas A. Fey, Cindy Henry, Karl W. Mollison, Rolf Wagner, Donna M. Gauvin, George W. Carter, James M. Trevillyan, Teresa A. Rosenberg, Sandra E. Burke, Steve J. Ballaron, Joy Bauch, Morey L. Smith
Publikováno v:
Journal of Cardiovascular Pharmacology. 49:228-235
Sirolimus (rapamycin) is an immunosuppressant used in preventing allograft rejection and in drug-eluting stents to prevent restenosis after angioplasty. Zotarolimus, an analogue of sirolimus, was designed to have a shorter in vivo half-life. Zotaroli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66d70a94a47632b4c29594455a56393e
https://doi.org/10.1097/fjc.0b013e3180325b0a
https://doi.org/10.1097/fjc.0b013e3180325b0a
Autor:
Deanna L. Haasch, Hing L. Sham, Rebecca J. Gum, James M. Trevillyan, Elizabeth H. Fry, Cele Abad-Zapatero, Gang Liu, Mei Liu, Jill E. Clampit, Sanyi Wang, Cristina M. Rondinone
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:668-672
A new series of 4-anilinopyrimidines has been synthesized and evaluated as JNK1 inhibitors. SAR studies led to the discovery of potent JNK1 inhibitors with good enzymatic activity as well as cellular potency represented by compound 2b. Kinase selecti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::113d54228f101f627d32e8d9184ef361
https://doi.org/10.1016/j.bmcl.2006.10.093
https://doi.org/10.1016/j.bmcl.2006.10.093
Autor:
David W A Beno, Gang Liu, Zhili Xin, James S. Polakowski, Nathan L. Lubbers, Bo Liu, Mei Liu, James M. Trevillyan, Hongyu Zhao, Michael D. Serby, Hing L. Sham, D. L. Widomski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:495-500
The hemodynamic effects of a series of potent and selective 4-aminopyridine carboxamide-based pan-JNK inhibitors were assessed in an anesthetized rat model. The effects of these agents on mean arterial pressure, heart rate, cardiac contractility, and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3186ce4d7b1307f25f3eb4289460d9f
https://doi.org/10.1016/j.bmcl.2006.10.013
https://doi.org/10.1016/j.bmcl.2006.10.013
Autor:
Hing L. Sham, Zhili Xin, Christi Kosogof, Terry Pederson, Hongyu Zhao, Cele Abad-Zapatero, Bo Liu, Michael D. Serby, Bruce G. Szczepankiewicz, Gang Liu, Cristina M. Rondinone, Nelson Lissa T, Deanna L. Haasch, Jill E. Clampit, Sanyi Wang, Rebecca J. Gum, James M. Trevillyan, Elizabeth H. Fry, Eric F. Johnson, Mei Liu
Publikováno v:
Journal of Medicinal Chemistry. 49:4455-4458
C-Jun NH2 terminal kinases (JNKs) are important cell signaling enzymes. JNK1 plays a central role in linking obesity and insulin resistance. JNK2 and JNK3 may be involved in inflammatory and neurological disorders, respectively. Small-molecule JNK in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc463ce3c72249463613b7043f83c6a3
https://doi.org/10.1021/jm060465l
https://doi.org/10.1021/jm060465l
Autor:
James M. Trevillyan, Elizabeth H. Fry, Eric F. Johnson, Chaohong Sun, Hing L. Sham, Charles W. Hutchins, Thomas H. Lubben, Bruce G. Szczepankiewicz, Edward T. Olejniczak, Michael A. Stashko, Cele Abad-Zapatero, Michael D. Serby, Rebecca J. Gum, Hongyu Zhao, Kristi Haskins, Zhili Xin, Bo Liu, Sarah A Dorwin, Jill E. Clampit, Nelson Lissa T, Gang Liu, Mei Liu, Christi Kosogof, Cristina M. Rondinone, Sanyi Wang, Deanna L. Haasch
Publikováno v:
Journal of Medicinal Chemistry. 49:3563-3580
The c-Jun N-terminal kinases (JNK-1, -2, and -3) are members of the mitogen activated protein (MAP) kinase family of enzymes. They are activated in response to certain cytokines, as well as by cellular stresses including chemotoxins, peroxides, and i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a5bb3bc96de29a87b4ec28bbfc5f96f
https://doi.org/10.1021/jm060199b
https://doi.org/10.1021/jm060199b
Autor:
Gang Liu, Zhili Xin, James M. Trevillyan, Elizabeth H. Fry, Deanna L. Haasch, Rebecca J. Gum, Cele Abad-Zapatero, Jill E. Clampit, Sanyi Wang, Mei Liu, Hing L. Sham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2590-2594
A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as c-Jun-N-terminal kinase (JNK) inhibitors is described. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxypyrazoles. The structure–activit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb7aa9b2a85c03096204cc36631f7f17
https://doi.org/10.1016/j.bmcl.2006.02.046
https://doi.org/10.1016/j.bmcl.2006.02.046
Publikováno v:
Drug Development Research. 67:627-642
Inhibitors of the enzyme dipeptidyl peptidase-IV (DPP-IV) appear poised to become the next major advance in the treatment of type 2 diabetes mellitus (T2DM). Glucagon-like peptide-1 (GLP-1) is an "incretin hormone" released from L cells in the small
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ff7fa933c212c039e1a1b4ae6ef18891
https://doi.org/10.1002/ddr.20138
https://doi.org/10.1002/ddr.20138
Autor:
Noah Tu, Kennan C. Marsh, Karl W. Mollison, Rolf Wagner, Gin C. Hsieh, Cynthia L. Henry, Merrill Nuss, Jay R. Luly, Denise Wilcox, Nwe Y. Bamaung, Benjamin C. Lane, Richard P. Carlson, Yung-Wu Chen, Thomas A. Fey, Luping Liu, Paul E. Wiedeman, Yat-Sun Or, James M. Trevillyan, George W. Carter, Peer B. Jacobson, Teresa A. Rosenberg, Stevan W. Djuric
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5340-5343
The synthesis and biological activities of rapamycin (I) analogs modified at the C-40 position are reported. Emphasis placed on compounds that potentially have an improved safety profile on account of their shorter in vivo half-life when compared wit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::036756a7d35bbf41755d205775e590ad
https://doi.org/10.1016/j.bmcl.2005.06.106
https://doi.org/10.1016/j.bmcl.2005.06.106
Autor:
James M. Trevillyan, Paul E. Wiedeman
Publikováno v:
Drug Discovery Today: Therapeutic Strategies. 2:143-149
Therapeutic agents targeting the incretin axis are poised for clinical utility in the treatment of metabolic diseases. The incretin hormone, glucagon-like peptide-1 (GLP-1), plays a significant role in glycemic control. The focus here is on the maint
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5d00264def8edcb7861d0455d90de725
https://doi.org/10.1016/j.ddstr.2005.05.020
https://doi.org/10.1016/j.ddstr.2005.05.020