Zobrazeno 1 - 10 of 152 pro vyhledávání: '"R. W. Friesen"'
1
Design, synthesis, and evaluation of novel 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective CXCR2 chemokine receptor antagonists
Autor: YiLi Ding, Yongxin Han, François G. Gervais, Shilan Liu, Leanne Bedard, Robert B. Lobell, Hongmei Wang, Shuhui Chen, Angela Wong, Martin Henault, Jingchao Dong, David M. Stout, Hao Wu, Ge Li, Stacia Kargman, Nicole Sawyer, R. W. Friesen, Yinhui Liu, Manuel Chan
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:5741-5745
We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazin
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dffc3d9548b1256ab1668d8e9a829d4a
https://doi.org/10.1016/j.bmcl.2009.08.014
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2
Conformation-assisted Inhibition of Protein-tyrosine Phosphatase-1B Elicits Inhibitor Selectivity over T-cell Protein-tyrosine Phosphatase
Autor: Caroline Desponts, Ernest Asante-Appiah, Yves Leblanc, Brian P. Kennedy, Sangita B. Patel, Claude Dufresne, Cheuk K. Lau, R. W. Friesen, Giovanna Scapin, Joseph W. Becker, Jillian M. Taylor, Michel Therien
Publikováno v: Journal of Biological Chemistry. 281:8010-8015
PTP-1B represents an attractive target for the treatment of type 2 diabetes and obesity. Given the role that protein phosphatases play in the regulation of many biologically relevant processes, inhibitors against PTP-1B must be not only potent, but a
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c540ae1c13d462238e7eaec6e783eea
https://doi.org/10.1074/jbc.m511827200
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3
The YRD Motif Is a Major Determinant of Substrate and Inhibitor Specificity in T-cell Protein-tyrosine Phosphatase
Autor: Caroline Desponts, Paul Payette, Christopher I. Bayly, Kevin P. Bateman, Ernest Asante-Appiah, Kathryn Skorey, Chidambaram Ramachandran, Robert Zamboni, Giovanna Scapin, Brian P. Kennedy, R. W. Friesen, Kristen Ball
Publikováno v: Journal of Biological Chemistry. 276:26036-26043
We have studied T-cell protein-tyrosine phosphatase (TCPTP) as a model phosphatase in an attempt to unravel amino acid residues that may influence the design of specific inhibitors. Residues 48--50, termed the YRD motif, a region that is found in pro
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e441bcb00194a9df63cf7379636ae2c
https://doi.org/10.1074/jbc.m011697200
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