Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Brian Wayland"'
Autor:
Brian M. Glass, Padmaja Polam, Tom Emm, Kevin Bowman, Jordan S. Fridman, Holly Koblish, Richard Wynn, Michael Hansbury, Yanlong Li, Eddy W. Yue, Brian Metcalf, Michael J. Bower, Min Wei, Richard B. Sparks, Peggy Scherle, Xiangdong Liu, Andrew P. Combs, Timothy Burn, Dilip P. Modi, Brian Wayland, Qian Wang, Lynn Leffet, Brent Douty, Wenyu Zhu, Amy Takvorian, Joseph Glenn
Publikováno v:
ACS Medicinal Chemistry Letters
A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 4f, INCB24360 (epacadostat). The molecular structure of INCB24360 contains several previously unknown or underutilized functional groups in drug
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c5e3f5ea28d700b9b9ea48bc68260b0
http://europepmc.org/articles/PMC5430407
http://europepmc.org/articles/PMC5430407
Autor:
Swamy Yeleswaram, Thomas Maduskuie, Brian Wayland, Hao Feng, Patricia Feldman, Niu Shin, Yanlong Li, Chu-Biao Xue, Peggy Scherle, Song Mei, Kathy Wang, Maryanne Covington, Wenqing Yao, Padmaja Polam, Richard B. Sparks, Wenyu Zhu, Xin He, Sharon Diamond, Eddy W. Yue, Chunhong He, Brian Metcalf, Holly Koblish, Ke Zhang, Nikoo Falahatpisheh, Brent Douty, Leslie Hall, Yu Li, Andrew P. Combs, Joseph Glenn, Kamna Katiyar, Yun-Long Li
Publikováno v:
ACS Med Chem Lett
[Image: see text] A medicinal chemistry effort focused on identifying a structurally diverse candidate for phosphoinositide 3-kinase delta (PI3Kδ) led to the discovery of clinical candidate INCB050465 (20, parsaclisib). The unique structure of 20 co
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3cb077aa93316c89804bca15aea78a20
https://pubmed.ncbi.nlm.nih.gov/31749910
https://pubmed.ncbi.nlm.nih.gov/31749910
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4dc56472deabeab69da8f0d1a3343f0e
https://doi.org/10.1074/jbc.m607913200
https://doi.org/10.1074/jbc.m607913200
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37cbcb8ee9e18b5c0ccf88d99607e6cf
https://doi.org/10.1016/j.bmc.2006.05.032
https://doi.org/10.1016/j.bmc.2006.05.032
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3391b69bc36449813d723f802b9d79a
https://doi.org/10.1021/jm0504555
https://doi.org/10.1021/jm0504555
Autor:
Xiangdong Liu, Andrew P. Combs, Min Wei, Changnian Liu, Peggy Scherle, Kevin Bowman, Timothy Burn, Jordan S. Fridman, Yanlong Li, Brian Wayland, Richard Wynn, Brent Douty, Holly Koblish, Brian Metcalf, Michael J. Bower, Lynn Leffet, Michael Hansbury, Qian Wang, Eddy W. Yue
Publikováno v:
Journal of medicinal chemistry. 52(23)
A hydroxyamidine chemotype has been discovered as a key pharmacophore in novel inhibitors of indoleamine 2,3-dioxygenase (IDO). Optimization led to the identification of 5l, which is a potent (HeLa IC(50) = 19 nM) competitive inhibitor of IDO. Testin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c08716dd7a70b41a58e004af922d972
https://pubmed.ncbi.nlm.nih.gov/19507862
https://pubmed.ncbi.nlm.nih.gov/19507862
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2630cdf27b46ce4cb4099aed23de6264
https://pubmed.ncbi.nlm.nih.gov/18037290
https://pubmed.ncbi.nlm.nih.gov/18037290
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26917bc8c3c72958fbfd5b19d9ebd2f2
https://pubmed.ncbi.nlm.nih.gov/16916797
https://pubmed.ncbi.nlm.nih.gov/16916797
Autor:
Eddy W. Yue, Brent Douty, Brian Wayland, Michael Bower, Xiangdong Liu, Lynn Leffet, Qian Wang, Kevin J. Bowman, Michael J. Hansbury, Changnian Liu, Min Wei, Yanlong Li, Richard Wynn, Timothy C. Burn, Holly K. Koblish, Jordan S. Fridman, Brian Metcalf, Peggy A. Scherle, Andrew P. Combs
Publikováno v:
Journal of Medicinal Chemistry; Dec2009, Vol. 52 Issue 23, p7364-7367, 4p