Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Denzil Bernard"'
Autor:
Guangfeng Wang, Duxin Sun, Ruijuan Luo, Ming Guo, Jianfeng Wen, Yifan Zhai, Sally Przybranowski, Bo Wen, Donna McEachern, Shaomeng Wang, Angelo Aguilar, Ding Du, Liu Liu, Jianfeng Lu, Xiaoqin Li, Denzil Bernard, Dajun Yang, Hengbang Wang
Publikováno v:
Journal of Medicinal Chemistry
We previously reported the design of spirooxindoles with two identical substituents at the carbon-2 of the pyrrolidine core as potent MDM2 inhibitors. In this paper we describe an extensive structure–activity relationship study of this class of MDM
Autor:
Shaomeng Wang, Laurent Besret, Shanghai Yu, Isabelle Meaux, Jennifer L. Meagher, Angelo Aguilar, Yujun Zhao, Donna McEachern, Cedric Barriere, Denzil Bernard, Jianfeng Lu, Laurent Debussche, Wei Sun, Cassandra Gianna Hoffman-Luca, Longchuan Bai, Jeanne A. Stuckey, Sanjeev Shangary, Stephane Guerif, Liu Liu, Dimitri Gorge-Bernat, Odette Dos-Santos, Pascal Pannier
Publikováno v:
Cancer Research. 74:5855-5865
Blocking the oncoprotein murine double minute 2 (MDM2)–p53 protein–protein interaction has long been considered to offer a broad cancer therapeutic strategy, despite the potential risks of selecting tumors harboring p53 mutations that escape MDM2
Autor:
Duxin Sun, Sanjeev Shargary, Jianfeng Lu, Shaomeng Wang, Liu Liu, Donna McEachern, Wei Sun, Shanghai Yu, Peng Zou, Ting Zhao, Denzil Bernard, Yujun Zhao, Xiaoqin Li
Publikováno v:
Journal of Medicinal Chemistry. 56:5553-5561
We previously reported the discovery of a class of spirooxindoles as potent and selective small-molecule inhibitors of the MDM2-p53 interaction (MDM2 inhibitors). We report herein our efforts to improve their pharmacokinetic properties and in vivo an
Autor:
Jian Zhang, Guoping Wang, Sanjeev Shangary, Yipin Lu, Jianyong Chen, Sanmao Kang, Rajal B. Shah, Su Qiu, Rebecca Miller, Qingyang Gu, Xiaolan Ling, Zaneta Nikolovska-Coleska, Ke Ding, Dongguang Qin, Donna McEachern, Shaomeng Wang, Ming Guo, Denzil Bernard, Kenneth J. Pienta, Dajun Yang, Yi Sun, Meilan Liu
Publikováno v:
Proceedings of the National Academy of Sciences. 105:3933-3938
We have designed MI-219 as a potent, highly selective and orally active small-molecule inhibitor of the MDM2–p53 interaction. MI-219 binds to human MDM2 with a K i value of 5 nM and is 10,000-fold selective for MDM2 over MDMX. It disrupts the MDM2
Autor:
Wei Sun, Denzil Bernard, Donna McEachern, Liu Liu, Jeffrey R. Deschamps, Jianfeng Lu, Shaomeng Wang, Angelo Aguilar
Publikováno v:
Journal of Medicinal Chemistry
Inhibition of the MDM2–p53 protein–protein interaction is being actively pursued as a new anticancer therapeutic strategy, and spiro-oxindoles have been designed as a class of potent and efficacious small-molecule inhibitors of this interaction (
Autor:
Liu Liu, Jeffrey R. Deschamps, Jianfeng Lu, Denzil Bernard, Shanghai Yu, Yujun Zhao, Duxin Sun, Xiaoqin Li, Donna McEachern, Jean Christophe Carry, Philippe Ochsenbein, Shaomeng Wang, Wei Sun, Vincent Ferey
Publikováno v:
Journal of the American Chemical Society. 135(19)
Small-molecule inhibitors that block the MDM2-p53 protein-protein interaction (MDM2 inhibitors) are being intensely pursued as a new therapeutic strategy for cancer treatment. We previously published a series of spirooxindole-containing compounds as
Publikováno v:
Journal of medicinal chemistry. 55(11)
was determined to be 2.42 μMin a competitive MDM2 binding assay. Changing thestereochemistry of one aryl and the C3 acetic acid substituentin 1 and resolution of the active enantiomer yielded compound2, whose affinity to MDM2 is 50- to 70-fold bette
Autor:
Su Qiu, Sanjeev Shangary, Meilan Liu, Guoping Wang, Donna McEachern, Carol R. Bradford, Denzil Bernard, Shaomeng Wang, Ke Ding, Thomas E. Carey, Yipin Lu, Zaneta Nikolovska-Coleska, Joshua A. Bauer
Publikováno v:
Molecular cancer therapeutics. 7(6)
MDM2 oncoprotein binds directly to the p53 tumor suppressor and inhibits its function in cancers retaining wild-type p53. Blocking this interaction using small molecules is a promising approach to reactivate p53 function and is being pursued as a new