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Cited by 1,327

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Thapsigargin inhibits the sarcoplasmic or endoplasmic reticulum Ca-ATPase family of calcium pumps.

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Lytton, J., Westlin, M., Hanley, M.R.·1991·Journal of Biological Chemistry

Abstract

The role of ATP-dependent calcium uptake into intracellular storage compartments is an essential feature of hormonally induced calcium signaling. Thapsigargin, a non-phorboid tumor promoter, increasingly is being used to manipulate calcium stores because it induces a hormone-like elevation of cytosolic calcium. It has been suggested that thapsigargin acts through inhibition of the endoplasmic reticulum calcium pump. We have directly tested the specificity of thapsigargin on all of the known intracellular-type calcium pumps (referred to as the sarcoplasmic or endoplasmic reticulum Ca-ATPase family (SERCA]. Full-length cDNA clones encoding SERCA1, SERCA2a, SERCA2b, and SERCA3 enzymes were expressed in COS cells, and both calcium uptake and calcium-dependent ATPase activity were assayed in microsomes isolated from them. Thapsigargin inhibited all of the SERCA isozymes with equal potency. Furthermore, similar doses of thapsigargin abolished the calcium uptake and ATPase activity of sarcoplasmic reticulum isolated from fast twitch and cardiac muscle but had no influence on either the plasma membrane Ca-ATPase or Na,K-ATPase. The interaction of thapsigargin with the SERCA isoforms is rapid, stoichiometric, and essentially irreversible. These properties demonstrate that thapsigargin interacts with a recognition site found in, and only in, all members of the endoplasmic and sarcoplasmic reticulum calcium pump family.

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Metadata

Authors
Lytton, J., Westlin, M., & Hanley, M. R.
Venue
Journal of Biological Chemistry
Publisher
Elsevier BV
Published
1991-09
Volume
266
Issue
26
Pages
17067-17071
ISSN
0021-9258 (ISSN-L)
OpenAlex
W1593385535
Cited by
1,327
References
1
FWCI
29.95
Type
journal article
Language
en
Open access
hybrid

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CoChat. (2026). Citation check: Thapsigargin inhibits the sarcoplasmic or endoplasmic reticulum Ca-ATPase family of calcium pumps. https://app.cochat.ai/papers/10.1016/s0021-9258(19)47340-7
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Lytton, J., Westlin, M., & Hanley, M. R. (1991). Thapsigargin inhibits the sarcoplasmic or endoplasmic reticulum Ca-ATPase family of calcium pumps. Journal of Biological Chemistry. https://doi.org/10.1016/s0021-9258(19)47340-7

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