Zobrazeno 1 - 10
of 68
pro vyhledávání: '"Kevin X. Chen"'
Publikováno v:
Genome Biology, Vol 24, Iss 1, Pp 1-26 (2023)
Abstract Background Enhancers are essential in defining cell fates through the control of cell-type-specific gene expression. Enhancer activation is a multi-step process involving chromatin remodelers and histone modifiers including the monomethylati
Externí odkaz:
https://doaj.org/article/54502e8e97744ae19f030b09cccac780
Enhancers are essential in defining cell fates through the control of cell type specific gene expression. Enhancer activation is a multi-step process involving chromatin remodelers and histone modifiers including the monomethylation of H3K4 (H3K4me1)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::03a09b046f8362f3d38db6b3a5f5b751
https://doi.org/10.1101/2022.10.24.513607
https://doi.org/10.1101/2022.10.24.513607
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a093625fe16457098a0a0b8d624a6c4e
https://doi.org/10.1016/j.bmcl.2017.11.025
https://doi.org/10.1016/j.bmcl.2017.11.025
Autor:
Joy Drobnick, Kevin X. Chen, Amy Sambrone, Stephen Schmidt, Lan Wang, Tao Wang, Ping Wu, Jim Nonomiya, Jinhua Chen, Seth F. Harris, Stacey Yeung, Chudi Ndubaku, Zijin Xu, Stephen E. Gould, Huifen Chen, Terry Crawford, Weilan Ye, Tanya Smyczek, Jason Boggs, Rajiv Jesudason, Erin McNamara, Philip Vitorino, Ding Charles Z, Lesley J. Murray
Publikováno v:
ACS Medicinal Chemistry Letters. 6:913-918
Diverse biological roles for mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) have necessitated the identification of potent inhibitors in order to study its function in various disease contexts. In particular, compounds that can be u
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4691b6776a7f46441928aa91ff58247f
https://doi.org/10.1021/acsmedchemlett.5b00174
https://doi.org/10.1021/acsmedchemlett.5b00174
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4920e6fdb48509b8406537a8dcd45287
https://pubmed.ncbi.nlm.nih.gov/28892380
https://pubmed.ncbi.nlm.nih.gov/28892380
Autor:
Pinto Patrick A, F. George Njoroge, Joseph A. Kozlowski, K.-C. Cheng, Hsueh-Cheng Huang, Frank Bennet, Tin-Yau Chan, Oleg Selyutin, Sony Agrawal, Yuhua Huang, Bancha Vibulbhan, Francisco Velazquez, Stuart B. Rosenblum, Srikanth Venkatraman, Yueheng Jiang, Gopinadhan N. Anilkumar, Cheng Li, Kevin X. Chen, Qingbei Zeng, Charles A. Lesburg, Neng-Yang Shih
Publikováno v:
ACS Medicinal Chemistry Letters. 5:244-248
Starting from indole-based hepatitis C virus (HCV) NS5B polymerase inhibitor lead compound 1, structure modifications were performed at multiple indole substituents to improve potency and pharmacokinetic (PK) properties. Bicyclic quinazolinone was fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56d6b7cd7274b7db5b44ce371671e837
https://doi.org/10.1021/ml400192w
https://doi.org/10.1021/ml400192w
Autor:
Stuart B. Rosenblum, Stephen Gavalas, Francisco Velazquez, Pinto Patrick A, Oleg Selyutin, Neng-Yang Shih, Yuhua Huang, Wanli Wu, Sony Agrawal, Yueheng Jiang, Srikanth Venkatraman, Joseph A. Kozlowski, Chuan-kui Jiang, Hsueh-Cheng Huang, Jose S. Duca, Anilkumar G. Nair, Bancha Vibulbhan, Eric Ferrari, Kevin X. Chen, Cheng Li, Charles A. Lesburg, F. George Njoroge, Frank Bennett, Qingbei Zeng
Publikováno v:
Bioorganic & Medicinal Chemistry. 21:2007-2017
The characterization of HCV genome has identified various vital functional proteins involved in the life cycle of hepatitis C virus. This has resulted in many novel enzymatic targets that are potential for development of therapeutic agents. The HCV R
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f016854d014a0a4d91a3500623598032
https://doi.org/10.1016/j.bmc.2013.01.024
https://doi.org/10.1016/j.bmc.2013.01.024
Autor:
Jonathan Maher, F. Anthony Romero, Samir Kharbanda, Mark Merchant, Ivana Yen, Yingjie Li, Edna F. Choo, Jiangpeng Liao, Xiaocang Wei, Kwong Wah Lai, Karen E. Gascoigne, Richard D. Cummings, Hariharan Jayaram, Thomas Hunsaker, Steven F. Bellon, Jian Wang, Cameron L. Noland, Brian K. Albrecht, Ying Jiang, Jeremy Murray, Susan Kaufman, Kerry L. Spillane, Florence Poy, Zhaowu Xu, Fei Wang, James R. Kiefer, Laura Zawadzke, Zhongguo Chen, Alexander M. Taylor, Andrew R. Conery, Xiaoyu Zhu, Wenfeng Liu, Eneida Pardo, Alexandre Côté, Andrea G. Cochran, Vickie Tsui, Steven Magnuson, Terry Crawford, Maureen Beresini, Emily Chan, Kevin X. Chen, Gladys de Leon Boenig, Justin Ly, Tracy Kleinheinz, Zhongya Xu
Publikováno v:
Journal of medicinal chemistry. 59(23)
The single bromodomain of the closely related transcriptional regulators CBP/EP300 is a target of much recent interest in cancer and immune system regulation. A co-crystal structure of a ligand-efficient screening hit and the CBP bromodomain guided i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0312372a13735186cadfcb6ec13190c
https://pubmed.ncbi.nlm.nih.gov/27682507
https://pubmed.ncbi.nlm.nih.gov/27682507
Autor:
Jun Wang, Weidong Pan, F. George Njoroge, Vinay Girijavallabhan, Ying Huang, Ping Chen, Latha G. Nair, Frank Bennett, Angela Kerekes, Ashok Arasappan, Qun Dang, Qingmei Hong, Stephane L. Bogen, Zhidan Liu, Quang Truong, Sara Esposite, Yuhua Huang, Bancha Vibulbhan, Haiyan Pu, Andrew Stamford, Dmitri A. Pissarnitski, Kevin X. Chen, David B. Olsen, Vishal Verma, David Cole, Zhiqiang Zhao, Randall R. Rossman, Alvarez Carmen S
Publikováno v:
Nucleosides, nucleotidesnucleic acids. 35(6)
Novel 2'-modified guanosine nucleosides were synthesized from inexpensive starting materials in 7-10 steps via hydroazidation or hydrocyanation reactions of the corresponding 2'-olefin. The antiviral effectiveness of the guanosine nucleosides was eva
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5a12e0b1f99db43b830f93b2c1a155d
https://pubmed.ncbi.nlm.nih.gov/27104963
https://pubmed.ncbi.nlm.nih.gov/27104963
Autor:
Ernest Asante-Appiah, Sony Agrawal, Peter T. Meinke, Ellen Xia, Anilkumar G. Nair, Joseph A. Kozlowski, Lei Chen, De-Yi Yang, Michael P. Dwyer, Craig A. Coburn, Oleg Selyutin, Michael Wong, Rong Kong, Bin Hu, George F Njoroge, Amin A. Nomeir, Tao Ji, Rong Liu, Paul Ingravallo, Ling Tong, Ying Zhai, Stuart B. Rosenblum, Yueheng Jiang, Wensheng Yu, James I. Fells, Bin Zhong, Kevin X. Chen, Qingbei Zeng
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(13)
HCV NS5A inhibitors have demonstrated impressive in vitro potency profiles in HCV replicon assays and robust HCV RNA titer reduction in the clinic making them attractive components for inclusion in an all oral fixed dose combination regimen for the t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe7b1449a073e396c15e702031383c2f
https://pubmed.ncbi.nlm.nih.gov/27180013
https://pubmed.ncbi.nlm.nih.gov/27180013