Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 63, Issue 5, Pages 1937-1963Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b01509
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Funding
- Czech Science Foundation (GACR) Grant [303/14/04329-S]
- Specific University Research [MSMT 21-SVV/2019]
- Martina Roeselova Foundation, Czech Republic [OPPC CZ.2.16/3.1.00/24503, NPU I LO1601, LO1304]
- L'Oreal-UNESCO for Women in Science 2019
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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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