FKBP12 Binding Modulates Ryanodine Receptor Channel Gating

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Ryanodine receptor binding to FKBP12 is modulated by channel activation state.

Ryanodine receptor (RyR) Ca2+ release channels undergo a conformational change between the open and closed states. Its protein modulator, FK506 binding protein 12 (FKBP12), stabilises the channel gating between the four subunits that surround a central Ca2+-conducting pore. To understand the interdependence of RyR and FKBP12 binding, physiological and pharmacological agents were used to modulat...

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The 12 kDa FK506-binding protein, FKBP12, modulates the Ca(2+)-flux properties of the type-3 ryanodine receptor.

We have characterised the functional regulation of the type-3 ryanodine receptor by the 12 kDa FK506-binding protein. Wild-type type-3 ryanodine receptor and mutant type-3 ryanodine receptor in which the critical valine at position 2322 in the central 12 kDa FK506-binding protein binding site was substituted by aspartate, were stably expressed in human embryonic kidney cells. In contrast to the...

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Ryanodine Receptor Permeation and Gating

Schneider (1999) recently addressed the question of whether Ca 2 1 sparks arise from the opening of a single ryanodine receptor (RyR) channel or the simultaneous opening of several channels. The discussion highlighted the importance of single RyR channel permeation and gating in the interpretation of Ca 2 1 spark data. The Schneider (1999) perspective inspired us to extend this theoretical disc...

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Crystal structures of Ryanodine Receptor SPRY1 and tandem-repeat domains reveal a critical FKBP12 binding determinant

Ryanodine receptors (RyRs) form calcium release channels located in the membranes of the sarcoplasmic and endoplasmic reticulum. RyRs play a major role in excitation-contraction coupling and other Ca(2+)-dependent signalling events, and consist of several globular domains that together form a large assembly. Here we describe the crystal structures of the SPRY1 and tandem-repeat domains at 1.2-1...

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ژورنال

عنوان ژورنال: Journal of Biological Chemistry

سال: 2001

ISSN: 0021-9258

DOI: 10.1074/jbc.m100856200