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Article

Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor.

Cell research - 1 May 2016

Leach Katie, Gregory Karen J, Kufareva Irina, Khajehali Elham, Cook Anna E, Abagyan Ruben, Conigrave Arthur D, Sexton Patrick M, Christopoulos Arthur

Abstract excerpt

Drugs that allosterically target the human calcium-sensing receptor (CaSR) have substantial therapeutic potential, but are currently limited. Given the absence of high-resolution structures of the CaSR, we combined mutagenesis with a novel analytical approach and molecular modeling to develop an "enriched" picture of structure-function requirements for interaction between Ca(2+)o and allosteric modulators within...

Topics

Allosteric Regulation
Amines
Amino Acid Sequence
Amino Acids
Binding Sites
Calcium
HEK293 Cells
Humans
Mutation
Pharmaceutical Preparations
Receptors, Calcium-Sensing

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Signal Transduction

Structure-Activity Relationship

Source

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Identifiers

PMID: 27002221
DOI: 10.1038/cr.2016.36
PMCID: PMC4856764

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