以孤儿受体TR3为分子靶点的抗肿瘤药物筛选
Screening for Anti-cancer Drugs Targeting Orphan Nuclear Receptor TR3
Abstract
核受体是位于细胞内的一类重要的调控蛋白,目前已是药物开发的第二大靶点,迄今开发的药物中有大约13%的药物通过核受体靶点起作用。TR3是核受体家族的重要成员,在细胞分化,细胞增殖,细胞凋亡过程中发挥着关键的调控作用。在某些诱导剂的作用下,TR3可以快速地从细胞核转运到细胞质并且和Bcl-2相互作用,使Bcl-2从一个抑制凋亡的分子转变成促进细胞凋亡的杀手。由于许多治疗药物可通过调控细胞凋亡起作用,该发现提示,TR3调控的凋亡通路是开发抗肿瘤药物的新靶点。 本研究的目的就是建立一个以TR3为靶点的抗肿瘤药物筛选系统,该系统包括了药物对于TR3的表达调控,对于TR3在细胞内分区情况的影响,以及通过... Nuclear receptors (NRs), a class of proteins found within cells, represent the second most common drug target with about 13% of existing drugs acting on nuclear receptors. The orphan nuclear receptor TR3 (also known as NGFIB and Nur77) is an important member of the nuclear receptor superfamily which plays a key role in the regulation of differentiation, proliferation, apoptosis, and survival of ma...