Litcius/Paper detail

Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective

Lucie Peterková, Eva Kmonı́čková, Tomáš Ruml, Silvie Rimpelová

2020Journal of Medicinal Chemistry51 citationsDOIOpen Access PDF

Abstract

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.

Topics & Concepts

SERCAThapsigarginEndoplasmic reticulumChemistryATPaseCalciumCell biologyCalcium ATPaseBiochemistryEnzymeBiologyOrganic chemistryATP Synthase and ATPases ResearchEnzyme function and inhibitionBioactive Compounds and Antitumor Agents