Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Peter Yakowec"'
Autor:
Jason Duquette, Xin Huang, Dongyin Yu, Yun Ling, Jing Zhou, Yu Chung Wang, Daqing Sun, Sarah Wortman, John Eksterowicz, Qiuping Ye, Min Jiang, Jonathan D. Oliner, Lixia Jin, Alexander M. Long, Ana Z. Gonzalez, Peter Yakowec, Yihong Li, Steven H. Olson, Anne Y. Saiki, Hilary Plake Beck, Yosup Rew, Lawrence R. McGee, Julio C. Medina, Jonathan B. Houze, Jiasheng Fu, Jude Canon, Mcintosh Joel, Ada Chen, Brian M. Fox, Mei-Chu Lo, Xuelei Yan, Paul L. Shaffer, Zhihong Li, Tao Osgood, Xiaoning Zhao
Publikováno v:
Journal of Medicinal Chemistry. 57:10499-10511
Structure-based rational design and extensive structure-activity relationship studies led to the discovery of AMG 232 (1), a potent piperidinone inhibitor of the MDM2-p53 association, which is currently being evaluated in human clinical trials for th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6411aa1211e82e797ec19f5aeedd623
https://doi.org/10.1021/jm501550p
https://doi.org/10.1021/jm501550p
Autor:
Lawrence R. McGee, Jeffrey T. Mihalic, Yingcai Wang, Mei-Chu Lo, Jing Zhou, Steven H. Olson, Xiaoqi Chen, Frank Kayser, Jiang Zhu, Ada Chen, Jeffrey Deignan, Jonathan D. Oliner, Alexander M. Long, Daqing Sun, Ming Yu, Xin Huang, Qiuping Ye, Jiwen Jim Liu, Peter Yakowec, Julio C. Medina
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3782-3785
We recently reported on the discovery of AMG 232, a potent and selective piperidinone inhibitor of the MDM2-p53 interaction. AMG 232 is being evaluated in human clinical trials for cancer. Continued exploration of the N-alkyl substituent of this seri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb62da92063f4e1d74dae97a63a686bb
https://doi.org/10.1016/j.bmcl.2014.06.073
https://doi.org/10.1016/j.bmcl.2014.06.073
Autor:
Leszek Poppe, Paul D. Schnier, John B. Jordan, Jeffrey Lewis, Klaus Michelsen, Peter Yakowec, Evelyn Yang, Xin Huang, Jing Zhou, Alexander M. Long, Yosup Rew
Publikováno v:
Journal of the American Chemical Society. 134:17059-17067
Restoration of p53 function through the disruption of the MDM2-p53 protein complex is a promising strategy for the treatment of various types of cancer. Here, we present kinetic, thermodynamic, and structural rationale for the remarkable potency of a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4fff8be8f55551048557839aeaff38f8
https://doi.org/10.1021/ja305839b
https://doi.org/10.1021/ja305839b
Autor:
Peter Yakowec, Jin Tang, Violeta Yu, Alexander M. Long, Ralf Schwandner, Tanja Fisch, Josie Han Lee, Renee Emkey, Markus Hierl, Hao Chen
Publikováno v:
SLAS Discovery. 17:27-38
Lysine demethylase 1 (LSD1) and Jumonji C domain-containing oxygenase D2C (JMJD2C) participate in regulating the methylation status of histone H3 lysine residues. In some contexts, LSD1 and JMJD2C activity causes enhanced cellular proliferation, whic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c215ec6a75a7c52375efa2d47a93203f
https://doi.org/10.1177/1087057111418228
https://doi.org/10.1177/1087057111418228
Autor:
Jing Zhou, Xiaoning Zhao, Yihong Li, Lixia Jin, David Chow, Lawrence R. McGee, Steven H. Olson, Paul L. Shaffer, Jonathan D. Oliner, Xin Huang, Ana Z. Gonzalez, Jonathan B. Houze, Yun Ling, Zhihong Li, Hilary Plake Beck, Ada Chen, Tao Osgood, Jason Duquette, Sarah Wortman, Dongyin Yu, Alexander M. Long, Xuelei Yan, Daqing Sun, Peter Yakowec, Yosup Rew, Brian M. Fox, Julio C. Medina, Qiuping Ye, Anne Y. Saiki, Jiasheng Fu, Mcintosh Joel, Jude Canon, Mei-Chu Lo, John Eksterowicz
Publikováno v:
Journal of medicinal chemistry. 57(7)
We previously reported the discovery of potent and selective morpholinone and piperidinone inhibitors of the MDM2-p53 interaction. These inhibitors have in common a carboxylic acid moiety that engages in an electrostatic interaction with MDM2-His96.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::696ea31016294428e56ba942b0710fda
https://pubmed.ncbi.nlm.nih.gov/24601644
https://pubmed.ncbi.nlm.nih.gov/24601644
Autor:
Yosup Rew, Steve Schneider, Peter Yakowec, Lisa Julian, Jude Canon, Alexander M. Long, Xuelei Yan, Julio C. Medina, Xin Huang, Jonathan D. Oliner, Hilary Plake Beck, Felix Gonzalez-Lopez de Turiso, Dongyin Yu, Shou-Hua Xiao, Ada Chen, Mei-Chu Lo, Xiaoning Zhao, Anne Y. Saiki, David Chow, Michael D. Bartberger, Jing Zhou, Qiuping Ye, Tiffany L. Correll, Daqing Sun, Frank Kayser, Steven H. Olson, Jay P. Powers, Tao Osgood, Dustin McMinn, Paul L. Shaffer
Publikováno v:
Journal of medicinal chemistry. 56(10)
Structural analysis of both the MDM2-p53 protein-protein interaction and several small molecules bound to MDM2 led to the design and synthesis of tetrasubstituted morpholinone 10, an MDM2 inhibitor with a biochemical IC50 of 1.0 μM. The cocrystal st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21b2b421ad8ad7c0f32d30da3d1a9de9
https://pubmed.ncbi.nlm.nih.gov/23597064
https://pubmed.ncbi.nlm.nih.gov/23597064
Autor:
Felix Gonzalez-Lopez de Turiso, Ada Chen, Steven H. Olson, Xin Huang, Jude Canon, Anne Y. Saiki, Michael D. Bartberger, Hilary Plake Beck, Jonathan D. Oliner, David J. Kopecky, Xuelei Yan, Jing Zhou, Maria M. Toteva, Min Jiang, Mei-Chu Lo, Alexander M. Long, Darin J. Gustin, Klaus Michelsen, Tao Osgood, Steve Schneider, Qiuping Ye, Jeffrey Deignan, Yosup Rew, Peter Yakowec, Daqing Sun, Xianyun Jiao, Lixia Jin, Dongyin Yu, David Chow, Julio C. Medina, Frank Kayser, Mark L. Ragains, Yihong Li, Xiaoning Zhao, Brian M. Fox
Publikováno v:
Journal of medicinal chemistry. 55(11)
Structure-based rational design led to the discovery of novel inhibitors of the MDM2–p53 protein–protein interaction. The affinity of these compounds for MDM2 was improved through conformational control of both the piperidinone ring and the appen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e801db16462f352d2d21a52ca43e600
https://pubmed.ncbi.nlm.nih.gov/22624960
https://pubmed.ncbi.nlm.nih.gov/22624960
Autor:
Yang Xu, Leeanne Zalameda, Raju Subramanian, Erin L. Mullady, Michael Schrag, Kevin Yang, Daniel J. Freeman, Jian Jiang, Longbin Liu, Tian Wu, Derin C. D'amico, John D. McCarter, Noel D'angelo, Sean Caenepeel, Peter Yakowec, Ling Wang, Mark H. Norman, Robert C. Wahl, Tisha San Miguel, Jin Tang, Douglas A. Whittington, Paul E. Hughes, Shon Booker, Ning Xi, Tae-Seong Kim, Kui Chen, Nancy Zhang, Kristin L. Andrews
Publikováno v:
Journal of medicinal chemistry. 54(6)
Phosphoinositide 3-kinase α (PI3Kα) is a lipid kinase that plays a key regulatory role in several cellular processes. The mutation or amplification of this kinase in humans has been implicated in the growth of multiple tumor types. Consequently, PI
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3ef766c5554069d71d128a5c63ff879f
https://pubmed.ncbi.nlm.nih.gov/21332118
https://pubmed.ncbi.nlm.nih.gov/21332118
Autor:
Adrian L. Smith, Jeffrey Petkus, Carol Babij, Nick A. Paras, Joseph L. Kim, Frenel Fils Demorin, Kristen Hess, Q.T. Le, Josette Carnahan, Andrew Tasker, Linda F. Epstein, Pedro J. Beltran, Douglas A. Whittington, Mark J. Rose, Mquele Ncube, Matthew R. Lee, Qi Huang, Elizabeth M. Doherty, Peter Yakowec, Manory Fernando
Publikováno v:
Cancer Research. 70:2681A-2681A
The Ras-Raf-MAPK signaling pathway plays a central role in diverse cellular processes including differentiation, proliferation and survival. This pathway is activated in a large percentage of cancers as a result of mutations in Ras or in B-Raf Ser/Th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::490386bfce8e500a88dfe80448fb35d4
https://doi.org/10.1158/1538-7445.am10-2681a
https://doi.org/10.1158/1538-7445.am10-2681a
Autor:
John G. Allen, Matthew P. Bourbeau, G. Erich Wohlhieter, Michael D. Bartberger, Klaus Michelsen, Randall Hungate, Robert C. Gadwood, Rick D. Gaston, Bruce Evans, Larry W. Mann, Michael E. Matison, Stephen Schneider, Xin Huang, Dongyin Yu, Paul S. Andrews, Andreas Reichelt, Alexander M. Long, Peter Yakowec, Evelyn Y. Yang, Tani Ann Lee
Publikováno v:
Journal of Medicinal Chemistry; Nov2009, Vol. 52 Issue 22, p7044-7053, 10p