Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Aihe Zhou"'
Autor:
BinQing Wei, Kirk Robarge, Sharada S. Labadie, Jinhua Chen, Laura B. Corson, Antonio DiPasquale, Peter S. Dragovich, Charles Eigenbrot, Marie Evangelista, Benjamin P. Fauber, Anna Hitz, Rebecca Hong, Kwong Wah Lai, Wenfeng Liu, Shuguang Ma, Shiva Malek, Thomas O'Brien, Jodie Pang, David Peterson, Laurent Salphati, Deepak Sampath, Steven Sideris, Mark Ultsch, Zijin Xu, Ivana Yen, Dong Yu, Qin Yue, Aihe Zhou, Hans E. Purkey
Publikováno v:
Bioorganicmedicinal chemistry letters. 59
Structure-based design was utilized to optimize 6,6-diaryl substituted dihydropyrone and hydroxylactam to obtain inhibitors of lactate dehydrogenase (LDH) with low nanomolar biochemical and single-digit micromolar cellular potencies. Surprisingly the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0770db4a66cefb70bb9bee4bcf37ca52
https://pubmed.ncbi.nlm.nih.gov/35065235
https://pubmed.ncbi.nlm.nih.gov/35065235
Autor:
Charles Z. Ding, Laurent Salphati, Hans E. Purkey, HongXiu Ge, Qin Yue, Antonio G. DiPasquale, Charles Eigenbrot, Qunh Ho, Kwong Wah Lai, Thomas O'Brien, Sharada Labadie, Zhongguo Chen, David A. Peterson, Shiva Malek, Laura Corson, Wenfeng Liu, Mark Ultsch, Jinhua Chen, Anna Hitz, Yajing Liu, Kirk Robarge, Jodie Pang, Chiho Li, Peter S. Dragovich, Binqing Wei, Shuguang Ma, Huihui Zhang, Steve Sideris, Zhenting Gao, Marie Evangelista, Ivana Yen, Aihe Zhou, Benjamin Fauber
Publikováno v:
ACS Medicinal Chemistry Letters. 7:896-901
A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f0532bd0e9287d033f18781fd7cf755
https://doi.org/10.1021/acsmedchemlett.6b00190
https://doi.org/10.1021/acsmedchemlett.6b00190
Autor:
Gary Salmon, Harvey Wong, Maxine Norman, Adrian Barnard, Aihe Zhou, Julie Hawkins, Benjamin Fauber, Adam R. Johnson, Arunima Ganguli, Yuzhong Deng, Susan Summerhill, Kirk Robarge, Celine Eidenschenk, Wenjun Ouyang, Christine Everett, Jianhua Cao, Wei Tang, Hank La, Alberto Gobbi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2907-2912
The nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORγ, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in the production of the pro-inflammatory cytokine int
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa9c3898f9ddd336ebaff802da33874c
https://doi.org/10.1016/j.bmcl.2015.05.055
https://doi.org/10.1016/j.bmcl.2015.05.055
Autor:
Binqing Wei, Erica VanderPorten, Mark Ultsch, Jason Boggs, Peter S. Dragovich, S. Sideris, Jinhua Chen, Huihui Zhang, Sharada Labadie, Qin Yue, Charles Z. Ding, Kirk Robarge, David Peterson, Shuguang Ma, Hans E. Purkey, Benjamin Fauber, HongXiu Ge, Aihe Zhou, Kwong Wah Lai, Qunh Ho, Shiva Malek, Xuying Zhang, Ivana Yen, Laura Corson, Charles Eigenbrot, Qing Xu, Laurent Salphati
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:75-82
Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enone using structure-based design strategies resulted in inhibitors with considerable improvement in biochemical potency against human lactate dehydrogenase A (LDHA). These potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::921f2e384863aba9482741802d507295
https://doi.org/10.1016/j.bmcl.2014.11.008
https://doi.org/10.1016/j.bmcl.2014.11.008
Autor:
Peter S. Dragovich, Benjamin P. Fauber, Jason Boggs, Jinhua Chen, Laura B. Corson, Charles Z. Ding, Charles Eigenbrot, HongXiu Ge, Anthony M. Giannetti, Thomas Hunsaker, Sharada Labadie, Chiho Li, Yichin Liu, Yingchun Liu, Shuguang Ma, Shiva Malek, David Peterson, Keith E. Pitts, Hans E. Purkey, Kirk Robarge, Laurent Salphati, Steve Sideris, Mark Ultsch, Erica VanderPorten, Jing Wang, BinQing Wei, Qing Xu, Ivana Yen, Qin Yue, Huihui Zhang, Xuying Zhang, Aihe Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3764-3771
A novel class of 3-hydroxy-2-mercaptocyclohex-2-enone-containing inhibitors of human lactate dehydrogenase (LDH) was identified through a high-throughput screening approach. Biochemical and surface plasmon resonance experiments performed with a scree
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4ed0191d5c5ad01b10f95a841198637
https://doi.org/10.1016/j.bmcl.2014.06.076
https://doi.org/10.1016/j.bmcl.2014.06.076
Autor:
John Moffat, Marcia Belvin, Lichuan Liu, Jocelyn Chan, Li Ren, Kirk Robarge, Francis J. Sullivan, Jeffrey Stults, Jonas Grina, David A. Moreno, Ann Qin, Matthew Martinson, Stephen E. Gould, Jacob Schwarz, Kang-Jye Chou, Sheerin K. Shahidi-Latham, Lars Mueller, John Gaudino, Aihe Zhou, James F. Blake, Weiru Wang, Danette Dudley, Christine Orr, Michael Burkard, Thomas Hunsaker, Dolores Diaz, Mark Merchant, Huifen Chen, Jianping Yin, Patricia Pacheco, Kevin Rasor
Publikováno v:
Journal of medicinal chemistry. 59(12)
The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations in BRAF or RAS or by upstream oncogenic signaling. While targeting upstream n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8d609114730026c9434727995874843
https://pubmed.ncbi.nlm.nih.gov/27227380
https://pubmed.ncbi.nlm.nih.gov/27227380
Autor:
Janusz J. Kulagowski, Claire Morris, Leslie Lee, Kathy Barrett, Sean P. Flynn, Richard Pastor, Michael Siu, Charles Eigenbrot, Deepak Sampath, Christine Chang, Jane R. Kenny, Aihe Zhou, Jeremy Murray, Joseph P. Lyssikatos, Christopher A. Hurley, Emily J. Hanan, Jeffrey M. Blaney, Wade S. Blair, Tom Rawson, Paul Gibbons, Steven Magnuson, Mark Ultsch, Anne van Abbema
Publikováno v:
Journal of Medicinal Chemistry. 55:10090-10107
The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2 inhibitors for use in treating these disorders. A high-throughput screening effort identified
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b38641cff96060895c55ccc721612a54
https://doi.org/10.1021/jm3012239
https://doi.org/10.1021/jm3012239
Autor:
Laura Corson, Thomas Hunsaker, Yingqing Ran, Andrea G. Cochran, Elizabeth Blackwood, Hans-Willi Krell, Leslie Walker, Jun Li, Birong Zhang, Aihe Zhou, Jason Halladay, Thomas E. Rawson, Bing-Yan Zhu, Carter Fields, Brian Safina, Mark Ultsch, Matthias Rüth, Tracy Kleinheinz, Angela McNutt, Dan Burdick, Jun Liang, Jason Drummond, Petra Rüger, Christian Wiesmann, Bernhard Goller, Guy Georges, Gail Lewis Phillips, Anja Limberg, John Moffat, Jenna Dotson
Publikováno v:
Journal of Medicinal Chemistry. 51:4465-4475
Aurora kinase inhibitors have attracted a great deal of interest as a new class of antimitotic agents. We report a novel class of Aurora inhibitors based on a pentacyclic scaffold. A prototype pentacyclic inhibitor 32 (AKI-001) derived from two early
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6298eaa13aa6a279801fb4d948e210a7
https://doi.org/10.1021/jm800052b
https://doi.org/10.1021/jm800052b
Autor:
Mark McCleland, David Peterson, Anneleen Daemen, Deepak Sampath, Alexander N. Vanderbilt, Rebecca Hong, Christopher Del Nagro, Simon Williams, Raju V. Pusapati, Binqing Wei, Shuguang Ma, Hans E. Purkey, Tommy Lai, Aihe Zhou, Mandy Kwong, Laurent Salphati, Jodie Pang, Aaron Boudreau, Shiva Malek, Peter K. Jackson, Steve Sideris, Yingjie Li, Ron Firestein, Min Gao, Laura Corson, Charles Eigenbrot, Thomas O'Brien, Kirk Robarge, Sharada Labadie, Anna Hitz, Zhongguo Chen, Marcia Belvin, Marie Evangelista, Ivana Yen, Georgia Hatzivassiliou
Publikováno v:
Nature chemical biology. 12(10)
Metabolic reprogramming in tumors represents a potential therapeutic target. Herein we used shRNA depletion and a novel lactate dehydrogenase (LDHA) inhibitor, GNE-140, to probe the role of LDHA in tumor growth in vitro and in vivo. In MIA PaCa-2 hum
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78f042da2eb1ecc9b37304d9eb24d494
https://pubmed.ncbi.nlm.nih.gov/27479743
https://pubmed.ncbi.nlm.nih.gov/27479743
Autor:
Binqing Wei, Qin Yue, Aihe Zhou, David A. Peterson, Shiva Malek, Peter S. Dragovich, Hans E. Purkey, Benjamin Fauber, Ivana Yen, Sharada Labadie, Steve Sideris, Charles Z. Ding, Laura Corson, Charles Eigenbrot, Mark Ultsch, Jinhua Chen, Kirk Robarge
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(24)
A series of 3,6-disubstituted dihydropyrones were identified as inhibitors of human lactate dehydrogenase (LDH)-A. Structure activity relationships were explored and a series of 6,6-spiro analogs led to improvements in LDHA potency (IC50
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cbe4e61cbeea45b3bca848d1de408cb9
https://pubmed.ncbi.nlm.nih.gov/25467161
https://pubmed.ncbi.nlm.nih.gov/25467161