A TOOL COMING OF AGE - THAPSIGARGIN AS AN INHIBITOR OF SARCOENDOPLASMIC RETICULUM CA2-ATPASES()

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 popu lar tool in a host of studies directed at elucidating the mechanisms o f intracellular Ca2+ signalling. its remarkable potency and selectivit y have been instrumental in widening our view of the function of intra cellular 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, Gasper Caspersen and Soren Brog ger Christensen review the key pharmacological features of thapsigargi n action; they also discuss some of the ways in which its unique prope rties have shown to be important for obtaining new insights into the b iology of Ca2+ stares, and how these properties might encompass a ther apeutic potential. In parallel, attention is drawn to some of the limi tations and pitfalls encountered when working with thapsigargin.