Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Denzil Bernard"'
Autor:
Maibritt Kretschmer, Themistoklis Zisis, Denzil Bernard, Simone Moser, Ryan P. Pemberton, Nader Al Danaf, Angelika M. Vollmar, Shuaijun Wang, Cornelia A. Karg, Don C. Lamb, Sabine Schneider, Stefan Zahler
Publikováno v:
Angewandte Chemie (International Ed. in English)
Chlorophyll and heme are among the “pigments of life”, tetrapyrrolic structures, without which life on Earth would not be possible. Their catabolites, the phyllobilins and the bilins, respectively, share not only structural features, but also a s
Autor:
Liu Liu, Krishnapriya Chinnaswamy, Haibin Zhou, Jeanne A. Stuckey, Hong Shen, Chao Yie Yang, Jianfeng Lu, Shaomeng Wang, Donna McEachern, Yi Sun, Denzil Bernard, Liangyou Rui
Publikováno v:
Nature Communications, Vol 12, Iss 1, Pp 1-13 (2021)
Cullin-RING E3 ligases (CRLs) regulate the turnover of approximately 20% of mammalian cellular proteins. Neddylation of individual cullin proteins is essential for the activation of each CRL. We report herein the discovery of DI-1548 and DI-1859 as t
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:
Stephanie Layton, Weihua Zhou, Liu Liu, Zhen-Qiang Pan, Krishnapriya Chinnaswamy, Chao Yie Yang, Jeanne A. Stuckey, Shaomeng Wang, Haibin Zhou, Jianfeng Lu, Denzil Bernard, Ester Fernandez-Salas, Yi Sun, Qing Yu
Publikováno v:
Nature Communications, Vol 8, Iss 1, Pp 1-12 (2017)
Nature Communications
Nature Communications
The Cullin-RING E3 ubiquitin ligases (CRLs) regulate homeostasis of ~20% of cellular proteins and their activation require neddylation of their cullin subunit. Cullin neddylation is modulated by a scaffolding DCN protein through interactions with bot
Autor:
Liu Liu, Fang Cao, Shirley Y. Lee, Shaomeng Wang, Elizabeth C. Townsend, Yali Dou, Hacer Karatas, Denzil Bernard, Jing Xu
Publikováno v:
Chinese Chemical Letters. 26:455-458
We described herein structure-based design, synthesis and evaluation of conformationally constrained, cyclic peptidomimetics to block the MLL1-WDR5 protein–protein interaction as inhibitors of the MLL1 histone methyltransferase activity. Our study
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
Autor:
Denzil Bernard, Fang Cao, Ming Lei, Elizabeth C. Townsend, Liu Liu, Yong Chen, Shaomeng Wang, Yali Dou, Hacer Karatas
Publikováno v:
Journal of the American Chemical Society. 135(2)
Mixed lineage leukemia 1 (MLL1) is a histone H3 lysine 4 (H3K4) methyltransferase, and targeting the MLL1 enzymatic activity has been proposed as a novel therapeutic strategy for the treatment of acute leukemia harboring MLL1 fusion proteins. The MLL
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