Role of cholesterol in the function and organization of G-protein coupled receptors

Progress in Lipid Research
Thomas J Pucadyil, A Chattopadhyay

Abstract

Cholesterol is an essential component of eukaryotic membranes and plays a crucial role in membrane organization, dynamics and function. The modulatory role of cholesterol in the function of a number of membrane proteins is well established. This effect has been proposed to occur either due to a specific molecular interaction between cholesterol and membrane proteins or due to alterations in the membrane physical properties induced by the presence of cholesterol. The contemporary view regarding heterogeneity in cholesterol distribution in membrane domains that sequester certain types of membrane proteins while excluding others has further contributed to its significance in membrane protein function. The seven transmembrane domain G-protein coupled receptors (GPCRs) are among the largest protein families in mammals and represent approximately 2% of the total proteins coded by the human genome. Signal transduction events mediated by this class of proteins are the primary means by which cells communicate with and respond to their external environment. GPCRs therefore represent major targets for the development of novel drug candidates in all clinical areas. In view of their importance in cellular signaling, the interaction of chole...Continue Reading

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