南美超级胎牛血清999尝鲜特惠
吲哚-3-甲醇衍生物作为HECT结构域结合抑制剂用于乳腺癌治疗的研究
Identification of the HECT domain binding of indole-3-carbinol (I3C) derivatives for breast cancer therapy
Wenwen Zheng, Zhichao Shi, Xun Zhang, Weibin Wu, Zigao Yuan, Lei Zhao, Qinyuan Li, Zixuan Qiu, Cunlong Zhang, Bizhu Chu, Zijian Liu, Wei-Min Chen, Yuyang Jiang
Journal：Phytochemistry Letters
IF：1.7
DOI：10.1016/j.phytol.2023.01.002
PMID：
Published：2023-01-17
research field：分子生物学基因治疗细胞生物学心脏病学信号转导纤维化研究
Abstract
We designed and synthesized a series of HECT (homologous to the E6-AP carboxyl terminus) domain binding inhibitors based on indole-3-carbinol (I3C) by structure-based rational drug design . Thermal shift and MTT assays indicated that compound A3 had a good HECT domain binding capacity and potent breast cancer cells inhibition activity, respectively. Subsequent studies showed that compound A3 inhibited proliferation and invasion, induced apoptosis and S-phase cell block. Additionally, compound A3 altered the expression of apoptosis and cell cycle related protein in MDA-MB-231 cells. Finally, computational simulation indicated the proposed binding mode of A3 with the NEDD4–1 HECT domain.
本文使用的Yeasen产品
