T C Major
Parke-Davis
16 Papers
545 Citations
T C Major is an academic researcher from Parke-Davis. The author has contributed to research in topics: Angiotensin II & Angiotensin II receptor type 1. The author has an hindex of 12, co-authored 16 publications.
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Papers
Structure−Activity Relationships for a Novel Series of Pyrido[2,3-d]pyrimidine Tyrosine Kinase Inhibitors
James Marino Hamby,C. J. C. Connolly,Mel C. Schroeder,R. Thomas Winters,H. D. Hollis Showalter,Robert L. Panek,T C Major,Bronislawa Olsewski,Michael J. Ryan,Tawny K. Dahring,Gina H. Lu,Joan A. Keiser,Aneesa Amar,Cindy Shen,Alan J. Kraker,Veronika Slintak,James M. Nelson,David W. Fry,Laura A. Bradford,and Hussein Hallak,Annette Marian Doherty +20 more
TL;DR: Screening of a compound library for inhibitors of the fibroblast growth factor and platelet-derived growth factor receptor tyrosine kinases led to the development of a novel series of ATP competitive pyrido[2,3-d]pyrimidine tyrosinesine kinase inhibitors, resulting in new analogs with improved potency, solubility, and bioavailability relative to the initial lead.
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Synthesis and Tyrosine Kinase Inhibitory Activity of a Series of 2-Amino-8H-pyrido[2,3-d]pyrimidines: Identification of Potent, Selective Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitors
Diane H. Boschelli,Zhipei Wu,Sylvester Klutchko,H. D. Hollis Showalter,James Marino Hamby,Gina H. Lu,T C Major,Tawny K. Dahring,Brian L. Batley,Robert L. Panek,Joan A. Keiser,Brian G. Hartl,Alan J. Kraker,Wayne D. Klohs,Bill J. Roberts,Sandra J. Patmore,William L. Elliott,Randy Steinkampf,Laura A. Bradford,Hussein Hallak,Annette Marian Doherty +20 more
TL;DR: Variation of the aromatic group at C-6 and of the alkyl group at N-8 of the pyrido[2,3-d]pyrimidine core provided several analogues that retained potency, including derivatives that were biased toward inhibition of the TK activity of PDGFr.
140
The ACAT Inhibitor Avasimibe Reduces Macrophages and Matrix Metalloproteinase Expression in Atherosclerotic Lesions of Hypercholesterolemic Rabbits
Thomas M.A. Bocan,Brian R. Krause,Wendy S. Rosebury,Sandra Bak Mueller,Xiaokang Lu,Catherine Dagle,T C Major,Chetan D. Lathia,Helen T. Lee +8 more
TL;DR: It is concluded that the bioavailable ACAT inhibitor avasimibe can directly limit macrophage accumulation, resulting in the histological appearance of mainly fibromuscular lesions, and can potentially stabilize preestablished atherosclerotic lesions by reducing MMP expression within the lesion.
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Multiple binding modes for the receptor-bound conformations of cyclic AII agonists.
K. Plucinska,T. Kataoka,Yodo M,Wayne L. Cody,John X. He,Christine Humblet,Gina Lu,Elizabeth A. Lunney,T C Major,Panek Rl +9 more
TL;DR: Analysis of the conformational constraints imposed in these active analogs suggests that AII agonists bind to their receptor with different backbone conformations in the region of the central tyrosine residue.
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