Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Denzil Bernard"'
Autor:
Denzil Bernard, Sally Przybranowski, Jeanne A. Stuckey, Donna McEachern, Tianfeng Xu, Ke Zheng, Ester Fernandez-Salas, Liyue Huang, Krishnapriya Chinnaswamy, Liu Liu, Mi Wang, Shaomeng Wang, Caroline Foster, Shilin Xu, Angelo Aguilar
Publikováno v:
Angewandte Chemie International Edition. 57:1601-1605
The structure-based design of M-525 as the first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction is presented. M-525 targets cellular menin protein at sub-nanomolar concentrations and achieves low nanomolar
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, Denzil Bernard, Shilin Xu, James Delproposto, Ester Fernandez-Salas, Liyue Huang, Kaitlin Harvey, Jeff W. Kampf, Liu Liu, Angelo Aguilar, Jeanne A. Stuckey, Tianfeng Xu, Caroline Foster, Donna McEachern, Ke Zheng, Krishnapriya Chinnaswamy
Publikováno v:
J Med Chem
Inhibition of the menin-mixed lineage leukemia (MLL) protein-protein interaction is a promising new therapeutic strategy for the treatment of acute leukemia carrying MLL fusion (MLL leukemia). We describe herein our structure-based design, synthesis,
Publikováno v:
Journal of Medicinal Chemistry. 58:1038-1052
Design of small-molecule inhibitors (MDM2 inhibitors) to block the MDM2–p53 protein–protein interaction has been pursued as a new cancer therapeutic strategy. In recent years, potent, selective, and efficacious MDM2 inhibitors have been successfu
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 (
Publikováno v:
Journal of the American Chemical Society. 125(10)
Pharmacophores are widely used for rational drug design and include those based on receptor binding sites or on known ligands. To date, ligand-based pharmacophores have typically used one or a small number of conformers of known receptor ligands. How