Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Lucie Gonneville"'
Autor:
Erin McLaughlin, Richard Wynn, Brent Douty, Brian Wayland, Andrew P. Combs, Mary Becker-Pasha, Amy Takvorian, Brian M. Glass, Lucie Gonneville, Eddy W. Yue, Timothy Burn, Matthew L. Crawley, Richard B. Sparks, Gregory Hollis, Milton Hillman, Paul J. Ala, Padmaja Polam
Publikováno v:
Journal of Biological Chemistry. 281:38013-38021
Structural analyses of the protein-tyrosine phosphatase 1B (PTP1B) active site and inhibitor complexes have aided in optimization of a peptide inhibitor containing the novel (S)-isothiazolidinone (IZD) phosphonate mimetic. Potency and permeability we
Autor:
Brian Wayland, Andrew P. Combs, Matthew L. Crawley, Amy Takvorian, Yanlong Li, Eddy W. Yue, Lucie Gonneville, Brent Douty, Erin McLaughlin, Min Wei, Zelda Wasserman, Michael J. Bower, Phillip Liu, Richard Wynn, Timothy Burn, Paul J. Ala
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:5833-5849
The structure-based design and discovery of the isothiazolidinone (IZD) heterocycle as a mimic of phosphotyrosine (pTyr) has led to the identification of novel IZD-containing inhibitors of protein tyrosine phosphatase 1B (PTP1B). The structure–acti
Autor:
Brian Wayland, Brian M. Glass, Padmaja Polam, Wenyu Zhu, Amy Takvorian, Milton Hillman, Yanlong Li, Lucie Gonneville, Matthew L. Crawley, Brian Metcalf, Richard B. Sparks, Mary Becker-Pasha, Eddy W. Yue, Reid Huber, Laurine G. Galya, Erin McLaughlin, Dilip P. Modi, Richard Wynn, Brent Douty, Timothy Burn, Brian Reid, Michael J. Bower, Andrew P. Combs, Mei Li, Zelda Wasserman, Phillip Liu, Ronald M. Klabe, Min Wei, Karl F Blom, Paul J. Ala, James Russell Pruitt, Lori L. Bostrom, Gregory Hollis
Publikováno v:
Journal of Medicinal Chemistry. 48:6544-6548
Structure-based design led to the discovery of novel (S)-isothiazolidinone ((S)-IZD) heterocyclic phosphotyrosine (pTyr) mimetics that when incorporated into dipeptides are exceptionally potent, competitive, and reversible inhibitors of protein tyros
Autor:
Richard Wynn, Brian Wayland, Ronald M. Klabe, Brent Douty, Andrew P. Combs, Eddy W. Yue, Min Wei, Lucie Gonneville, Paul J. Ala, Timothy Burn, Lori L. Bostrom, Michael J. Bower, Phillip Liu, James Russell Pruitt
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(1)
The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I c
Autor:
Timothy Burn, Phillip C.C. Liu, Yanlong Li, Nancy J. Taylor, Matthew L. Crawley, Paul J. Ala, Erin McLaughlin, Wenyu Zhu, Amy Takvorian, Padmaja Polam, Andrew P. Combs, Min Wei, Lucie Gonneville, Richard Wynn, Richard B. Sparks
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(3)
Benzothiazole benzimidazole (S)-isothiazolidinone ((S)-IZD) derivatives 5 were discovered through a peptidomimetic modification of the tripeptide (S)-IZD protein tyrosine phosphatase 1B (PTP1B) inhibitor 1. These derivatives are potent, competitive,
Autor:
Milton Hillman, Andrew P. Combs, Paul J. Ala, Ronald M. Klabe, Brian Wayland, Brent Douty, Michael J. Bower, Min Wei, Eddy W. Yue, Brian Reid, Mary Becker-Pasha, Gregory Hollis, Timothy Burn, Lucie Gonneville, Padmaja Polam, Richard Wynn, Zelda Wasserman
Publikováno v:
The Journal of biological chemistry. 281(43)
Crystal structures of protein-tyrosine phosphatase 1B in complex with compounds bearing a novel isothiazolidinone (IZD) heterocyclic phosphonate mimetic reveal that the heterocycle is highly complementary to the catalytic pocket of the protein. The h
Autor:
Richard Wynn, Swamy Yeleswaram, Eddy W. Yue, Gregory Hollis, Nancy Taylor, Padmaja Polam, Paul J. Ala, Zelda Wasserman, Andrew P. Combs, Dawn Ellis, Richard B. Sparks, Wenyu Zhu, Amy Takvorian, Michael J. Bower, Brian M Reid, Phillip Liu, Lucie Gonneville, Timothy Burn, Min Wei, Erin McLaughlin, Mark Rupar, Thomas Emm, Brian Metcalf, Matthew L. Crawley, Dilip P. Modi, Yanlong Li, Brian M. Glass
Publikováno v:
Journal of medicinal chemistry. 49(13)
Potent nonpeptidic benzimidazole sulfonamide inhibitors of protein tyrosine phosphatase 1B (PTP1B) were derived from the optimization of a tripeptide containing the novel (S)-isothiazolidinone ((S)-IZD) phosphotyrosine (pTyr) mimetic. An X-ray cocrys