关键词: Hsp90 cancer chaperones diptoindonesin G inhibitors tanespimycin

Mesh : Humans Benzofurans / pharmacology HSP90 Heat-Shock Proteins / antagonists & inhibitors chemistry Protein Folding

来  源:   DOI:10.1016/j.jbc.2022.102826

Abstract:
Hsp90 is a molecular chaperone that participates in protein folding, activation, and stabilization of substrate proteins. Since many diseases, including cancer, neurodegenerative diseases, and metabolic diseases, are caused by protein misfolding, drugs that inhibit Hsp90 are being pursued as potential targets for treatments. In the recent JBC Editor\'s Pick by Donahue et al., the authors show that diptoindonesin G is a new Hsp90 inhibitor that promotes degradation of the estrogen receptor, an Hsp90 client, without inducing the heat shock response.
摘要:
Hsp90是参与蛋白质折叠的分子伴侣,激活,和底物蛋白质的稳定。因为很多疾病,包括癌症,神经退行性疾病,和代谢性疾病,是由蛋白质错误折叠引起的,抑制Hsp90的药物正被视为潜在的治疗靶点.在最近的JBC编辑选择由Donahue等人。,作者表明,地缩酮G是一种新的Hsp90抑制剂,可促进雌激素受体的降解,一个Hsp90客户端,而不会引起热休克反应。
公众号