Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Susan, Pav"'
Publikováno v:
International Journal of Peptide and Protein Research. 48:401-410
The solution conformations of three polyhydroxymonoamide renin inhibitors which differ in the relative configuration and position of the hydroxyl groups at the P3, position were investigated by NMR spectroscopy. The NMR data are consistent with a pre
Autor:
Pier F. Cirillo, Susan Pav, John R. Regan, L. Churchill, Eugene R. Hickey, A. G. Graham, Liang Tong, Gilmore Thomas A, Neil Moss, Peter M. Grob, Christopher Pargellis
Publikováno v:
Nature Structural Biology. 9:268-272
The p38 MAP kinase plays a crucial role in regulating the production of proinflammatory cytokines, such as tumor necrosis factor and interleukin-1. Blocking this kinase may offer an effective therapy for treating many inflammatory diseases. Here we r
Publikováno v:
Journal of Structural Biology. 127:72-75
Human mitochondrial NAD(P) + -dependent malic enzyme was overexpressed in Escherichia coli and purified by anion-exchange, ATP affinity, and gel filtration chromatography. The protein was crystallized with the hanging-drop vapor diffusion method. Man
Autor:
Sheri Rogers, Charles L. Cywin, Liang Tong, Susan Pav, Della White, Kathy Crane, Christopher Pargellis, Maryanne L. Brown
Publikováno v:
Nature Structural Biology. 4:311-316
The crystal structure of human p38 mitogen-activated protein (MAP) kinase in complex with a potent and highly specific pyridinyl-imidazole inhibitor has been determined at 2.0 A resolution. The structure of the kinase, which is in its unphosphorylate
Autor:
Maryanne L. Brown, Walter Davidson, Kathy Crane, Charles L. Cywin, Jerry L. Hopkins, Christopher Pargellis, Susan Pav, Liang Tong, Della White, Sheri Rogers
Publikováno v:
Protein Science. 6:242-245
The recombinant human p38 MAP kinase has been expressed and purified from both Escherichia coli and SF9 cells, and has been crystallized in two forms by the hanging drop vapor diffusion method using PEG as precipitant. Both crystal forms belong to sp
Publikováno v:
Journal of Enzyme Inhibition. 11:151-169
Peptide boronic acid dipeptide compounds were analyzed for their ability to inhibit recombinant human dipeptidylpeptidase IV (CD26, DPPIV). Rate constants for the peptide boronates are difficult to obtain because the active boronic acid dipeptide exi
Autor:
Susan Pav, Louise Pilote, Paul C. Anderson, Steven R. LaPlante, Liang Tong, Grace Jung, Daniel Lamarre
Publikováno v:
Journal of Molecular Biology. 250:211-222
The crystal structures of recombinant glycosylated human renin in complex with several polyhydroxymonoamide inhibitors have been determined at up to 1.8 A resolution. The high resolution structures permit a detailed analysis of the conformation of re
Autor:
Yong Wang, Anthony S. Prokopowicz, Suresh R. Kapadia, Matt Aaron Tschantz, Maret Panzenbeck, Jonathan Tan, Pla Xiong, John P. Wolak, Xiao-Jun Wang, Susan Pav, Susan Lukas, Scott Jakes, Tina Morwick, Mario G. Cardozo, Usha R. Patel, Tanja Butz, Gregory W. Peet, Hidenori Takahashi, Neil Moss, Robert J. Eckner, Jeffrey D. Peterson, Abdelhakim Hammach, Mohammed A. Kashem, Daniel R. Goldberg, Jessica Huang, Roger J. Snow, Rosemarie Sellati
Publikováno v:
Journal of medicinal chemistry. 46(8)
The tyrosine kinase p56lck (lck) is essential for T cell activation; thus, inhibitors of lck have potential utility as autoimmune agents. Our initial disclosure of a new class of lck inhibitors based on the phenylaminoimidazoisoquinolin-9-one showed
Autor:
Jerry L. Hopkins, Deborah D. Jeanfavre, James M. Stevenson, Kathleen Last-Barney, Chungeng Qian, Leah L. Frye, Terence A. Kelly, Christine A. Grygon, Renee Zindell, Mario G. Cardozo, Liang Tong, Walter Davidson, Susan Pav
Publikováno v:
Journal of the American Chemical Society. 123(24)
The binding site on the lymphocyte function-associated antigen-1 (LFA-1) of a class of hydantoin-based antagonists of leukocyte cell adhesion has been identified. This site resides in the inserted-domain (I-domain) of the CD11a chain at a location th
Autor:
Louis Plamondon, William Paris, Francine Liard, Daniel Lamarre, Paul C. Anderson, Pierre L. Beaulieu, Gilbert Croteau, Dominik Wernic, Francois Soucy, Liang Tong, Vida Gorys, Susan Pav, Diane Thibeault, Dale R. Cameron, Chantal Grand-Maître, Christiane Yoakim
Publikováno v:
Journal of medicinal chemistry. 43(6)
Starting from palinavir (1), our lead HIV protease inhibitor, we have discovered a new series of truncated analogues in which the P(3)-P(2) quinaldic-valine portion of 1 was replaced by 2', 6'-dimethylphenoxyacetyl. With EC(50)'s in the 1-2 nM range,