TY - JOUR

T1 - A tool coming of age

T2 - Thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases

AU - Treiman, M.

AU - Caspersen, C.

AU - Christensen, S. B.

PY - 1998/1/1

Y1 - 1998/1/1

N2 - Thapsigargin is the most widely used inhibitor of the ubiquitous sarco- endoplasmic reticulum Ca2+-ATPases in mammalian cells. Over the past ten years, this guaianolide compound of plant origin has become a popular tool in a host of studies directed at elucidating the mechanisms of intracellular Ca2+ signalling. Its remarkable potency and selectivity have been instrumental in widening our view of the function of intracellular Ca2+ stores to include such key aspects as store-operated Ca2+ entry or the involvement of the stores in protein synthesis or cell growth. In this article Marek Treiman, Casper Caspersen and Soren Brogger Christensen review the key pharmacological features of thapsigargin action; they also discuss some of the ways in which its unique properties have shown to be important for obtaining new insights into the biology of Ca2+ stores, and how these properties might encompass a therapeutic potential. In parallel, attention is drawn to some of the limitations and pitfalls encountered when working with thapsigargin.

AB - Thapsigargin is the most widely used inhibitor of the ubiquitous sarco- endoplasmic reticulum Ca2+-ATPases in mammalian cells. Over the past ten years, this guaianolide compound of plant origin has become a popular tool in a host of studies directed at elucidating the mechanisms of intracellular Ca2+ signalling. Its remarkable potency and selectivity have been instrumental in widening our view of the function of intracellular Ca2+ stores to include such key aspects as store-operated Ca2+ entry or the involvement of the stores in protein synthesis or cell growth. In this article Marek Treiman, Casper Caspersen and Soren Brogger Christensen review the key pharmacological features of thapsigargin action; they also discuss some of the ways in which its unique properties have shown to be important for obtaining new insights into the biology of Ca2+ stores, and how these properties might encompass a therapeutic potential. In parallel, attention is drawn to some of the limitations and pitfalls encountered when working with thapsigargin.

UR - http://www.scopus.com/inward/record.url?scp=0031960313&partnerID=8YFLogxK

U2 - 10.1016/S0165-6147(98)01184-5

DO - 10.1016/S0165-6147(98)01184-5

M3 - Journal article

C2 - 9612087

AN - SCOPUS:0031960313

VL - 19

SP - 131

EP - 135

JO - Trends in Pharmacological Sciences

JF - Trends in Pharmacological Sciences

SN - 0165-6147

IS - 4

ER -