Zobrazeno 1 - 10
of 99
pro vyhledávání: '"James M. Trzaskos"'
Autor:
Rosemary Zhang, Mary F. Malley, Sidney Pitt, John S. Sack, Gary L. Schieven, Susan E. Kiefer, Stephen T. Wrobleski, John A. Newitt, James M. Trzaskos, Kevin Kish, Shuqun Lin, Joel C. Barrish, John H. Dodd, Murray McKinnon, Katerina Leftheris, John Hynes, Arthur M. Doweyko, Yi Fan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5864-5868
The design, synthesis, and structure–activity relationships (SAR) of a series of 2-aminothiazol-5-yl-pyrimidines as novel p38α MAP kinase inhibitors are described. These efforts led to the identification of 41 as a potent p38α inhibitor that util
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c09b23115c3b132f803f180d2db1d1d
https://doi.org/10.1016/j.bmcl.2010.07.102
https://doi.org/10.1016/j.bmcl.2010.07.102
Autor:
Gregory R. Ott, Krishna Vaddi, Rui-Qin Liu, Rajan Anand, Jingwu Duan, James M. Trzaskos, Maryanne B. Covington, David D. Christ, Zhonghui Lu, Mingxin Qian, Robert C. Newton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1958-1962
Potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) were discovered with several new heterocyclic P1' groups in conjunction with cyclic beta-amino hydroxamic acid scaffolds. Among them, the pyrazolopyridine provide
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f246d04dc5f8f53a5a66321c035d9eea
https://doi.org/10.1016/j.bmcl.2008.01.120
https://doi.org/10.1016/j.bmcl.2008.01.120
Autor:
Maryanne B. Covington, Zhonghui Lu, Rui-Qin Liu, James M. Trzaskos, Rajan Anand, Gregory R. Ott, Jingwu Duan, Robert C. Newton, Krishna Vaddi, Mingxin Qian, Naoyuki Asakawa, David D. Christ
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1577-1582
Novel ((2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamides were found to be excellent P1' substituents in conjunction with unique constrained beta-amino hydroxamic acid scaffolds for the discovery of potent selective inhibitors of TNF-alpha Con
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2b6f2a36e543037e9fb95cda7154bf4
https://doi.org/10.1016/j.bmcl.2008.01.075
https://doi.org/10.1016/j.bmcl.2008.01.075
Publikováno v:
Drug Discovery Today: Therapeutic Strategies. 4:39-47
With an increased understanding of the cellular and molecular mechanisms whereby inhaled allergens trigger T-cell dependent airway inflammation, new therapeutic strategies have emerged in the treatment of allergic airways disease. Here we review the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a97e6111b1b370c9a2024c5a080b8f8d
https://doi.org/10.1016/j.ddstr.2007.06.001
https://doi.org/10.1016/j.ddstr.2007.06.001
Autor:
Joseph J. Petraitis, Margaret F. Favata, Joseph B. Santella, Robert A. Copeland, John Wityak, Ronald L. Magolda, James M. Trzaskos, Bruce D. Jaffe, George L. Trainor, Gardner Daniel S, Peggy A. Scherle, Kurumi Y. Horiuchi, Jung-Hui Sun, Frank W. Hobbs, Andrea J. Daulerio, John V. Duncia
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1483-1486
Employing phenylmalonitrile dianion chemistry, a large number of analogues of MEK inhibitor lead SH053 (IC(50)=140 nM) were rapidly synthesized leading to single digit nM inhibitors, displaying submicromolar AP-1 transcription inhibition in COS-7 cel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47c68052de8368fc45bc4db9534d3974
https://doi.org/10.1016/j.bmcl.2004.01.012
https://doi.org/10.1016/j.bmcl.2004.01.012
Autor:
Chu-Biao Xue, Xiaohua He, John Roderick, Ronald L Corbett, James J.-W Duan, Rui-Qin Liu, Maryanne B Covington, Mingxin Qian, Maria D Ribadeneira, Krishna Vaddi, David D Christ, Robert C Newton, James M Trzaskos, Ronald L Magolda, Ruth R Wexler, Carl P Decicco
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4299-4304
Modifications of the lead TACE inhibitor 1 (N-hydroxy-trans-2-{[4-(4-quinolinyloxymethyl)anilinyl]carbonyl}-1-cyclohexanecarboxamide) at the cyclohexyl ring and the quinoline moiety led to the identification of a series of piperidine containing TACE
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e77c3dec33f6160bdbe29873bacd31d0
https://doi.org/10.1016/j.bmcl.2003.09.057
https://doi.org/10.1016/j.bmcl.2003.09.057
Publikováno v:
International Immunopharmacology. 3:1803-1817
By co-expressing glucocorticoid receptor (GR) and transcriptional reporter systems in GR-deficient Cos-7 cells, we profiled potency and efficacy of a panel of GR ligands as a function of GR expression levels (density). Our results show that potency a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c17076bdf29b061e37345b75570b3928
https://doi.org/10.1016/j.intimp.2003.08.005
https://doi.org/10.1016/j.intimp.2003.08.005
Autor:
James M. Trzaskos, Carl P. Decicco, Jingwu Duan, Chu-Biao Xue, Robert C. Newton, Rui-Qin Liu, Zelda R. Wasserman, Jennifer L. Seng, Zhonghui Lu, Ronald L. Magolda, Xiaohua He, John Roderick, Maryanne B. Covington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2035-2040
New inhibitors of tumor necrosis factor-α converting enzyme (TACE) were discovered using an N -hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamide scaffold. The series was found to be potent in a porcine TACE (pTACE) assay with IC 50 s typically below 5 nM. F
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0eecef0fc1e086cce3db1b3112350ee7
https://doi.org/10.1016/s0960-894x(03)00313-5
https://doi.org/10.1016/s0960-894x(03)00313-5
Autor:
James M. Trzaskos, Rui-Qin Liu, Elizabeth C. Arner, David D. Christ, Carl P. Decicco, Wenqing Yao, Robert J. Cherney, Maryanne B. Covington, Mingxin Qian, Robert C. Newton, Ron L Magolda, Dayton T. Meyer, Zelda R. Wasserman, Ruowei Mo, Micky D. Tortorella, Li Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1297-1300
Anti-succinate hydroxamates with cyclic P1 motifs were synthesized as aggrecanase inhibitors. The N-methanesulfonyl piperidine 23 and the N-trifluoroacetyl azetidine 26 were the most potent aggrecanase inhibitors both having an IC50=3 nM while mainta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::297fbc397746e76e53e9b9952620e792
https://doi.org/10.1016/s0960-894x(03)00124-0
https://doi.org/10.1016/s0960-894x(03)00124-0
Autor:
Gary L Davis, Rui-Qin Liu, Robert A. Copeland, Michael A. Pratta, James M. Trzaskos, Jeffery A Miller
Publikováno v:
Analytical Biochemistry. 314:260-265
We have identified a 41-residue peptide, bracketing the aggrecanase cleavage site of aggrecan, that serves as a specific substrate for this enzyme family. Biotinylation of the peptide allowed its immobilization onto streptavidin-coated plates. Aggrec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dad274f7df2d51e45790702cc0184d05
https://doi.org/10.1016/s0003-2697(02)00638-3
https://doi.org/10.1016/s0003-2697(02)00638-3