Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Michael F. Addo"'
Autor:
Hong Ye, Annette J. Eckardt, Charles E. Smith, Han-Cheng Zhang, David F. McComsey, Bruce E. Maryanoff, Wai-man Cheung, Bruce P. Damiano, Claudia K. Derian, Keith T. Demarest, Stuart Emanuel, Patricia Andrade-Gordon, Kimberly White, Diane R. Croll, Bruce R. Conway, Leonard R. Hecker, Michael F. Addo, Jian Li, Quan Li
Publikováno v:
Journal of Medicinal Chemistry. 48:1725-1728
Novel indolylindazolylmaleimides were synthesized and examined for kinase inhibition. We identified low-nanomolar inhibitors of PKC-beta with good to excellent selectivity vs other PKC isozymes and GSK-3beta. In a cell-based functional assay, 8f and
Autor:
Donna Oksenberg, Bruce E. Maryanoff, Han-Cheng Zhang, David F. McComsey, Claudia K. Derian, Michael F. Addo, Patricia Andrade-Gordon, Kimberly White
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2105-2109
A novel, 10-step, solid-phase method, based on a secondary amide linker, was developed to construct a diverse library of indole-based SFLLR peptide mimetics as thrombin receptor (protease-activated receptor 1, PAR-1) antagonists. The key steps includ
Autor:
W.J. Hoekstra, Claudia K. Derian, Bruce E. Maryanoff, Michael F. Addo, Glenn D. Prestwich, D.G. Ahern, John T. Elliott
Publikováno v:
The Journal of Peptide Research. 57:494-506
Six photoactivatable analogs of the human thrombin receptor activating peptide (TRAP), SFLLRN-NH2, were synthesized by substituting the photoactive amino acid, p-benzoylphenylalanine (Bpa), into each position of the peptide sequence. Platelet aggrega
Autor:
Andrew L. Darrow, Hoekstra William J, Patricia Andrade-Gordon, Charles E. Smith, Rosemary J. Santulli, Michael F. Addo, Bruce E. Maryanoff, David F. McComsey, Kenway Hoey
Publikováno v:
Archives of Biochemistry and Biophysics. 386:195-204
Protease-activated receptor-2 (PAR-2) is a tethered-ligand, G-protein-coupled receptor that is activated by proteolytic cleavage or by small peptides derived from its cleaved N-terminal sequence, such as SLIGRL-NH2. To assess specific PAR activity, w
Autor:
Patricia Andrade-Gordon, David F. McComsey, Donna Oksenberg, Bruce E. Maryanoff, Michael J. Hawkins, Michael F. Addo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:1423-1428
The thrombin receptor PAR-1 is activated by α-thrombin to stimulate cells, including platelets, through the tethered-ligand sequence SFLLRN. We have discovered a novel series of heterocycle-peptide hybrids comprised of a tripeptide segment, such as
Autor:
Maryanoff Bruce E, Michael F. Addo, Leonard R. Hecker, Mccomsey David F, Patricia Andrade-Gordon
Publikováno v:
ChemInform. 30
The thrombin receptor (PAR-1) is activated by alpha-thrombin to stimulate various cell types, including platelets, through the tethered-ligand sequence SFLLRN. Macrocyclic peptide analogues of SFLLRN were synthesized and evaluated in vitro. In genera
Autor:
Maryanoff Bruce E, Michael F. Addo, Jack A. Kauffman, Bruce P. Damiano, John A. Mitchell, Patricia Andrade-Gordon, Edward C. Lawson, Hoekstra William J
Publikováno v:
ChemInform. 33
Conformationally constrained analogues of the GPIIb/IIIa antagonist elarofiban (RWJ-53308) have been synthesized and biologically evaluated. The 1,2,4-triazolo[3,4- a ]pyridine scaffold provided potent antagonists with favorable pharmacodynamic and p
Autor:
Bruce P. Damiano, Jun Z. Xu, Michael F. Addo, Han-Cheng Zhang, Diane R. Croll, Lori Westover, Bruce E. Maryanoff, Richard Look, Patricia Andrade-Gordon, Gee-Hong Kuo, Jian Li, Keith T. Demarest, Bruce R. Conway, Leonard R. Hecker, Hong Ye, Claudia K. Derian
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(12)
A novel series of acyclic 3-(7-azaindolyl)-4-(aryl/heteroaryl)maleimides was synthesized and evaluated for activity against GSK-3beta and selectivity versus PKC-betaII, as well as a broad panel of protein kinases. Compounds 14 and 17c potently inhibi
Autor:
Han-Cheng Zhang, David F. McComsey, Richard Look, Patricia Andrade-Gordon, Annette J. Eckardt, Lori Westover, Keith T. Demarest, Bruce R. Conway, Bruce E. Maryanoff, Stuart Emanuel, Jun Z. Xu, Kimberly White, Michael F. Addo, Hong Ye, Claudia K. Derian
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(18)
Efficient methods were developed to synthesize a novel series of macrocyclic bisindolylmaleimides containing linkers with multiple heteroatoms. Potent inhibitors (single digit nanomolar IC(50)) for PKC-beta and GSK-3beta were identified, and compound
Autor:
Andrew L. Darrow, Mark Nedelman, Claudia K. Derian, Michael F. Addo, Bruce E. Maryanoff, Michael R. D'Andrea, Bruce P. Damiano, Patricia Andrade-Gordon, Han-Cheng Zhang
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 304(2)
Although it is well recognized that human platelet responses to alpha-thrombin are mediated by the protease-activated receptors PAR-1 and PAR-4, their role and relative importance in platelet-dependent human disease has not yet been elucidated. Becau