2010Molecular InterventionsOpen access

Pharmacology of Store-operated Calcium Channels

James W. Putney

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Abstract

Store-operated calcium entry is a process by which the depletion of calcium from the endoplasmic reticulum activates calcium influx across the plasma membrane. In the past few years, the major players in this pathway have been identified. STIM1 and STIM2 function as calcium sensors in the endoplasmic reticulum and can interact with and activate plasma membrane channels comprised of Orai1, Orai2, or Orai3 subunits. This review discusses recent advances in our understanding of this widespread signaling mechanism as well as the mechanisms by which a number of interesting pharmacological agents modify it.

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Store-operated calcium entry is a process by which the depletion of calcium from the endoplasmic reticulum activates calcium influx across the plasma membrane. In the past few years, the major players in this pathway have been identified. STIM1 and STIM2 function as calcium sensors in the endoplasmic reticulum and can interact with and activate plasma membrane channels comprised of Orai1, Orai2, or Orai3 subunits. This review discusses recent advances in our understanding of this widespread signaling mechanism as well as the mechanisms by which a number of interesting pharmacological agents modify it.

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Available abstract

Store-operated calcium entry is a process by which the depletion of calcium from the endoplasmic reticulum activates calcium influx across the plasma membrane. In the past few years, the major players in this pathway have been identified. STIM1 and STIM2 function as calcium sensors in the endoplasmic reticulum and can interact with and activate plasma membrane channels comprised of Orai1, Orai2, or Orai3 subunits. This review discusses recent advances in our understanding of this widespread signaling mechanism as well as the mechanisms by which a number of interesting pharmacological agents modify it.

Key concepts: ORAI1, Endoplasmic reticulum, STIM1, Cell biology, Calcium, Calcium signaling, Voltage-dependent calcium channel, Chemistry

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