TRAP1 and its therapeutic potential

IF 2.2 4区 医学 Q3 CHEMISTRY, MEDICINAL
Andrew Gutierrez, Jason Archdeacon, Brian S.J. Blagg
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引用次数: 0

Abstract

The mitochondrial Hsp90 isoform, Tumor Necrosis Factor Receptor Associated Protein 1 (TRAP1), is central to the pathogenesis of disease states that include cancer, ischemic retinopathy, and diabetic kidney disease among others. TRAP1 contributes to these diseases through the regulation of mitochondrial metabolism, apoptosis, oxidative stress, cell signaling and angiogenesis through interactions with client proteins. Numerous TRAP1-selective inhibitors have been developed to limit the toxicities associated with Hsp90 pan-inhibition, while leveraging the therapeutic benefits of TRAP1 inhibition. This review focuses on these inhibitors and the potential clinical uses of TRAP1-directed therapies.

Abstract Image

TRAP1及其治疗潜力。
线粒体Hsp90亚型,肿瘤坏死因子受体相关蛋白1 (TRAP1),是包括癌症、缺血性视网膜病变和糖尿病肾病等疾病的发病机制的核心。TRAP1通过与客户蛋白相互作用,调控线粒体代谢、凋亡、氧化应激、细胞信号传导和血管生成,从而导致这些疾病。许多TRAP1选择性抑制剂已经被开发出来,以限制与Hsp90泛抑制相关的毒性,同时利用TRAP1抑制的治疗益处。这篇综述的重点是这些抑制剂和trap1定向治疗的潜在临床应用。
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来源期刊
CiteScore
5.70
自引率
3.70%
发文量
463
审稿时长
27 days
期刊介绍: Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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