2. Academic Validation
  3. Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective

Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective

  • J Med Chem. 2020 Mar 12;63(5):1937-1963. doi: 10.1021/acs.jmedchem.9b01509.
Lucie Peterková 1,  Eva Kmoníčková 2,  Tomáš Ruml 1,  Silvie Rimpelová 1 2
Affiliations

Affiliations

  • 1 Department of Biochemistry and Microbiology, University of Chemistry and Technology Prague, Technická 5, 166 28, Prague 6, Czech Republic.
  • 2 Faculty of Medicine in Pilsen, Charles University, Alej Svobody 76, 323 00 Pilsen, Czech Republic.
PMID: 32030976 DOI: 10.1021/acs.jmedchem.9b01509
Abstract

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.

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