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Changes in the plasma membrane in metabolic disease: impact of the membrane environment on G protein‐coupled receptor structure and function
Author(s) -
Desai Aditya J,
Miller Laurence J
Publication year - 2018
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.13943
Subject(s) - g protein coupled receptor , allosteric regulation , biology , receptor , membrane protein , function (biology) , computational biology , population , cell membrane , membrane , heterologous expression , microbiology and biotechnology , bioinformatics , biochemistry , medicine , gene , environmental health , recombinant dna
Drug development targeting GPCRs often utilizes model heterologous cell expression systems, reflecting an implicit assumption that the membrane environment has little functional impact on these receptors or on their responsiveness to drugs. However, much recent data have illustrated that membrane components can have an important functional impact on intrinsic membrane proteins. This review is directed toward gaining a better understanding of the structure of the plasma membrane in health and disease, and how this organelle can influence GPCR structure, function and regulation. It is important to recognize that the membrane provides a potential mode of lateral allosteric regulation of GPCRs and can affect the effectiveness of drugs and their biological responses in various disease states, which can even vary among individuals across the population. The type 1 cholecystokinin receptor is reviewed as an exemplar of a class A GPCR that is affected in this way by changes in the plasma membrane.