Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Brent, Douty"'
Autor:
Diana A. Arias, Stephen Douglass, Lisa Truong, Qian Wang, Kathy H. Wang, Gengjie Yang, Michael Hansbury, Sybil O’Connor, Kevin Bowman, Robert Collins, Matthew Stubbs, Leslie Hall, Christina Stevens, Christopher Maddage, Brent Douty, Maryanne Covington, Lynn Leffet, Eddy Yue, Andrew Combs, Sunkyu Kim, Niu Shin, Holly Koblish, Rodrigo Hess
Publikováno v:
Cancer Research. 83:5162-5162
Immune checkpoint blockade has shown impressive efficacy in patients with inflamed tumors, although minimal activity has been observed in tumors lacking T cells. Myeloid cells are one of the most abundant cell types in both inflamed and non-inflamed
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5d70ba6e6ea112a6dd6efc2ea6e08d53
https://doi.org/10.1158/1538-7445.am2023-5162
https://doi.org/10.1158/1538-7445.am2023-5162
Autor:
Qian Wang, Sybil O'Connor, Alan Roberts, Brian W. Metcalf, Leslie Hall, Maxim Soloviev, Michael Hansbury, Greg Hollis, Xin He, Matthew C. Stubbs, Niu Shin, Wenqing Yao, Kamna Katiyar, Phillip C.C. Liu, Kathy Wang, Sharon Diamond, Brent Douty, Gengjie Yang, Dana Shuey, Maryanne B. Covington, Paul Collier, Mingming Gao, Patricia Feldman, Peggy Scherle, Timothy Burn, Andrew P. Combs, Yun-Long Li, Lynn Leffet, Robert C. Newton, Paul Waeltz, Holly Koblish, Jin Lu, Swamy Yeleswaram, Yanlong Li, Reid Huber, Robert Collins, Eddy W. Yue
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 374:211-222
The clinical use of first-generation phosphoinositide 3-kinase (PI3K)δ inhibitors in B-cell malignancies is hampered by hepatotoxicity, requiring dose reduction, treatment interruption, and/or discontinuation of therapy. In addition, potential molec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::450ddea425cecfdf40bf1184c7e8c723
https://doi.org/10.1124/jpet.120.265538
https://doi.org/10.1124/jpet.120.265538
Autor:
Niu, Shin, Matthew, Stubbs, Holly, Koblish, Eddy W, Yue, Maxim, Soloviev, Brent, Douty, Kathy He, Wang, Qian, Wang, Mingming, Gao, Patricia, Feldman, Gengjie, Yang, Leslie, Hall, Michael, Hansbury, Sybil, O'Connor, Lynn, Leffet, Robert, Collins, Kamna, Katiyar, Xin, He, Paul, Waeltz, Paul, Collier, Jin, Lu, Yun-Long, Li, Yanlong, Li, Phillip C C, Liu, Timothy, Burn, Maryanne, Covington, Sharon, Diamond, Dana, Shuey, Alan, Roberts, Swamy, Yeleswaram, Greg, Hollis, Brian, Metcalf, Wenqing, Yao, Reid, Huber, Andrew, Combs, Robert, Newton, Peggy, Scherle
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 374(1)
The clinical use of first-generation phosphoinositide 3-kinase (PI3K)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::14a526e7b4c814d8f260a1bead68f92f
https://pubmed.ncbi.nlm.nih.gov/32345620
https://pubmed.ncbi.nlm.nih.gov/32345620
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:
Paul Waeltz, Liang-Chuan S. Wang, Gregory Hollis, Yue Zhang, Eddy W. Yue, Nikoo Falahatpisheh, Reid Huber, Peggy Scherle, Timothy Burn, Thomas Maduskuie, Brent Douty, Yun-Long Li, Gengjie Yang, Andrew P. Combs, Holly Koblish, Mark Rupar, Michael Hansbury
Publikováno v:
Journal for Immunotherapy of Cancer
Pharmacological inhibition of the oncogenic PI3Kδ pathway has been shown to be efficacious in patients with hematopoietic malignancies. However, its therapeutic application in patients with solid tumors has not yet been tested. Recently, genetic ina
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::082544aa6faad2cf25e7c48ca3046208
https://doi.org/10.1186/2051-1426-3-s2-p377
https://doi.org/10.1186/2051-1426-3-s2-p377
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:
Peggy Scherle, Timothy Burn, Eddy W. Yue, Brent Douty, Yue Zhang, Yun-Long Li, Gengjie Yang, Liang-Chuan Wang, Michael Hansbury, Reid Huber, Gregory Hollis, Paul Waeltz, Nikoo Falahatpisheh, Holly Koblish, Thomas Maduskuie, Mark Rupar, Andrew P. Combs
Publikováno v:
Molecular Cancer Therapeutics. 14:C103-C103
Understanding the in vivo responses to immunoregulatory agents provides a basis for building more efficacious combination regimens. Pharmacologic inhibition of the oncogenic PI3Kδ pathway has been shown to be active in patients with hematopoietic ma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::43f13443a8797f78286cae13abd9a727
https://doi.org/10.1158/1535-7163.targ-15-c103
https://doi.org/10.1158/1535-7163.targ-15-c103