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Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective.
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2020-02-07 , DOI: 10.1021/acs.jmedchem.9b01509
Lucie Peterková 1 , Eva Kmoníčková 2 , Tomáš Ruml 1 , Silvie Rimpelová 1, 2
Affiliation  

The sarco/endoplasmic reticulum calcium ATPase (SERCA), which plays a key role in the maintenance of Ca2+ ion homeostasis, is an extensively studied enzyme, the inhibition of which has a considerable impact on cell life and death decision. To date, several SERCA inhibitors have been thoroughly studied and the most notable one, a derivative of the sesquiterpene lactone thapsigargin, is gradually approaching a clinical application. Meanwhile, new compounds with SERCA-inhibiting properties of natural, synthetic, or semisynthetic origin are being discovered and/or developed; some of these might also be suitable for the development of new drugs with improved performance. This review brings an up-to-date comprehensive overview of recently discovered compounds with the potential of SERCA inhibition, discusses their mechanism of action, and highlights their potential clinical applications, such as cancer treatment.

中文翻译:

Sarco /内质网钙ATPase抑制剂:抗癌视角之外。

肌钙蛋白/内质网钙ATPase(SERCA)在维持Ca2 +离子稳态中起着关键作用,是一种经过广泛研究的酶,其抑制作用对细胞的生命和死亡决定有很大影响。迄今为止,已经对几种SERCA抑制剂进行了深入研究,最著名的一种是倍半萜内酯thapsigargin的衍生物,正在逐步走向临床应用。同时,正在发现和/或开发具有天然,合成或半合成来源的具有SERCA抑制特性的新化合物。其中一些可能也适合开发性能更高的新药。这篇评论对最近发现的具有SERCA抑制作用的化合物进行了最新的全面概述,讨论了它们的作用机理,
更新日期:2020-02-17
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