Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Kwong Wah, Lai"'
Autor:
Kuen Yeap, John S. Wai, Maia Vinogradova, Yu Zhong, Lori Friedman, Xiaojing Wang, Daniel Otwine, Jiangpeng Liao, Nick Ray, James R. Kiefer, Vidhi Mody, Jun Li, Fabien Roussel, Deepak Sampath, Simon Charles Goodacre, Jun Liang, Michelle Nannini, Sharada Labadie, Xiaoping Zheng, Ellen Ingalla, Steven J. Hartman, Birong Zhang, Jae H. Chang, Tao Wang, Yingqing Ran, Jason R. Zbieg, Amy Sambrone, Kwong Wah Lai, Amy Young, Ciara Metcalfe, Neville James Mclean, Robert A. Blake, Tracy Kleinheinz
Publikováno v:
ACS Med Chem Lett
[Image: see text] Estrogen receptor alpha (ERα) is a well-validated drug target for ER-positive (ER+) breast cancer. Fulvestrant is FDA-approved to treat ER+ breast cancer and works through two mechanisms—as a full antagonist and selective estroge
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
Autor:
P. Andrew Evans, Erich W. Baum, Aleem N. Fazal, Kwong Wah Lai, John E. Robinson, James R. Sawyer
Publikováno v:
ARKIVOC, Vol 2006, Iss 7, Pp 338-358 (2006)
Externí odkaz:
https://doaj.org/article/465c28a2d43341528671c7d9e0b5082b
Autor:
Jodie Pang, Lunbin Deng, Girish Bankar, Jun Chen, Sultan Chowdhury, William R Proctor, Philippe Bergeron, Jennifer Vogt, Daniel F. Ortwine, Daniel P. Sutherlin, Jian Payandeh, Lilia Schumann, Shannon D. Shields, Christoph Martin Dehnhardt, Jae H. Chang, David H. Hackos, Elisa Ballini, Teresa Nguyen, Pengfei Ji, Glauco Tarozzo, Charles J. Cohen, Antonio G. DiPasquale, Kwong Wah Lai, Jonathan Maher, Kuldip Khakh, Steven J. McKerrall, Tania Chernov-Rogan, Wenfeng Liu, Brian Safina, Sophia Lin, Abid Hasan, J. P. Johnson
Publikováno v:
Journal of Medicinal Chemistry. 62:4091-4109
Using structure- and ligand-based design principles, a novel series of piperidyl chromane arylsulfonamide Nav1.7 inhibitors was discovered. Early optimization focused on improvement of potency through refinement of the low energy ligand conformation
Autor:
Maureen Beresini, Vickie Tsui, John S. Wai, F. Anthony Romero, Gladys de Leon Boenig, Patrick Cyr, Xiaoyu Zhu, Kevin X. Chen, Jiangpeng Liao, Edna F. Choo, Susan Kaufman, Fei Wang, Kwong Wah Lai, Caicai Zhu, Zhongguo Chen, Terry Crawford, Weichao Shen, Wenfeng Liu, Jeremy Murray, Yingjie Li, Sarah M. Bronner, Steven Magnuson, Justin Ly
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:15-23
A novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP, compound 35 (GNE-207), has been identified through SAR investigations focused on optimizing al bicyclic heteroarene to replace the aniline present in the published GNE-272
Autor:
Steven J, McKerrall, Teresa, Nguyen, Kwong Wah, Lai, Philippe, Bergeron, Lunbin, Deng, Antonio, DiPasquale, Jae H, Chang, Jun, Chen, Tania, Chernov-Rogan, David H, Hackos, Jonathan, Maher, Daniel F, Ortwine, Jodie, Pang, Jian, Payandeh, William R, Proctor, Shannon D, Shields, Jennifer, Vogt, Pengfei, Ji, Wenfeng, Liu, Elisa, Ballini, Lilia, Schumann, Glauco, Tarozzo, Girish, Bankar, Sultan, Chowdhury, Abid, Hasan, J P, Johnson, Kuldip, Khakh, Sophia, Lin, Charles J, Cohen, Christoph M, Dehnhardt, Brian S, Safina, Daniel P, Sutherlin
Publikováno v:
Journal of medicinal chemistry. 62(8)
Using structure- and ligand-based design principles, a novel series of piperidyl chromane arylsulfonamide Na
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
Autor:
Kevin R Clark, Terry Crawford, Xiaoyu Zhu, Susan Kaufman, F.A. Romero, G. de Leon Boenig, A. Zheng, Edna F. Choo, Maureen Beresini, Yingjie Li, Jiangpeng Liao, Steven Magnuson, Hariharan Jayaram, Patrick Cyr, John S. Wai, Jonathan Maher, Sarah M. Bronner, Fei Wang, Kwong Wah Lai, Vickie Tsui, Jeremy Murray, Xiao Huan Liang, Ruina Li, Zhongguo Chen, Wenfeng Liu, Justin Ly
Publikováno v:
Journal of medicinal chemistry. 60(24)
The epigenetic regulator CBP/P300 presents a novel therapeutic target for oncology. Previously, we disclosed the development of potent and selective CBP bromodomain inhibitors by first identifying pharmacophores that bind the KAc region and then buil
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
Autor:
Jane L. Grogan, Ruina Li, Edna F. Choo, Sarah M. Bronner, Maureen Beresini, Jonathan Maher, Patrick Cyr, Yingjie Li, Thomas Hunsaker, Brian K. Albrecht, Colin Masui, Kevin R Clark, Yingqing Ran, Jeremy Murray, Terry Crawford, Xiaorong Liang, Fei Wang, F. Anthony Romero, Xiaocang Wei, Alexander M. Taylor, Georgia Hatzivassiliou, Kyle Clagg, Kwong Wah Lai, Karen E. Gascoigne, Le An, Steven Magnuson, Mark Merchant, John S. Wai, Zhongguo Chen, Jiangpeng Liao, Vickie Tsui, Emily Chan, Kevin X. Chen, Wenfeng Liu, Wei Huang, Dong Yu, Stefan G. Koenig, Susan Kaufman, Xiaoyu Zhu, Gladys de Leon Boenig, Justin Ly, Denise E. de Almeida Nagata, Bing-Yan Zhu
Publikováno v:
Journal of medicinal chemistry. 60(22)
Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. We recently disclosed in vivo chemical tool 1 (GNE-272) for the bromodomain of CBP that was moderately potent a