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Article

Investigating the molecular mechanism of positive and negative allosteric modulators in the calcium-sensing receptor dimer.

Scientific reports - 18 Apr 2017

Jacobsen Stine Engesgaard, Gether Ulrik, Bräuner-Osborne Hans

Abstract excerpt

Allosteric modulators that are targeting the calcium-sensing receptor (CaSR) hold great therapeutic potential, and elucidating the molecular basis for modulation would thus benefit the development of novel therapeutics. In the present study, we aimed at investigating the mechanism of allosteric modulation in CaSR by testing dimers carrying mutations in the allosteric site of one or both of the subunits. To ensure...

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Identifiers

PMID: 28417952
DOI: 10.1038/srep46355
PMCID: PMC5394417

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