本发明公开了一种ARE‑PROTAC类化合物及其制备方法和应用。本发明提供了一种式(Ⅰ)所示的ARE‑PROTAC类化合物,该类化合物为有效的Nrf2蛋白抑制剂,可以利用泛素‑蛋白酶体系统,高效地降解Nrf2蛋白,进而治疗Nrf2异常激活引起的疾病。以肿瘤为例,该类化合物可以高效降解肿瘤细胞,尤其是常发Nrf2组成型激活的NSCLC细...
Despite the role of STAT3 as a known driver of oncogenesis, efforts to develop therapeutic STAT3 inhibitors have thus far been unsuccessful. In this issue of Cancer Cell, Bai et al. report a potent and selective STAT3 degrader capable of producing complete and long-lasting tumor regression in...
▱protactrat110ut=grett=1setristretimg doubt, the Chinese are the ones who best understand the beauty of Peking opera. 相关知识点: 试题来源: 解析 1. Without本题主要考查介词。句意:毫无疑问,中国人是最了解京剧之美的人。根据doubt可知,毫无疑问,疑问中国人最了解京剧。without 意为“没有”。句...
产品活性:Vepdegestrant (ARV-471) 是一种用于抵抗乳腺癌的具有口服活性的雌激素受体 PROTAC 蛋白降解剂。Vepdegestrant 是一种异双功能分子,可促进雌激素受体 α 和细胞内 E3 连接酶复合物之间的相互作用。Vepdegestrant 通过蛋白酶体导致雌激素受体的泛素化和随后的降解。Vepdegestrant 可强力降解 ER 阳性乳...
PROTAC BET degraders are more broadly effective than BET inhibitorsdoi:10.1016/s0959-8049(16)32621-1WinklerYaleJ.YaleQianYaleY.YaleDongYaleH.YaleChenYaleX.YaleCrewsYaleC.YaleEuropean journal of cancer: official journal for European Organization for Research and Treatment of Cancer (EORTC) [and] ...
15 - PROTAC BET degraders are more broadly effective than BET inhibitorsdoi:10.1016/S0959-8049(16)32621-1SDOSEuropean Journal of Cancer