Description

GPCRs (G-protein coupled receptors) are “seven-transmembrane” proteins known to be ubiquitous in mammalian cells. Such receptors are involved in many diseases, and hence they are targeted by many drugs. GPCRs are “second messengers,” namely they sense chemically affine ligands outside the cell by activating signal transduction pathways leading to cellular response through the production of intracellular and extracellular cAMP (cyclic Adenosyne Mono Phosphate). This cascade of events is activated through the “key-lock” mechanism, for example, whenever affine external ligands land on the cell surface they may activate conformational changes of some transmembrane domain forming GPCRs. This activates the so-called G-Protein, which in turn produced the adenylyl cyclase, ultimately transformed in cAMP.

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GPCRs receptors prefer lipid rafts

GPCRs (G-protein coupled receptors) are “seven-transmembrane” proteins known to be ubiquitous in mammalian cells. Such receptors are involved in many diseases, and hence they are targeted by many drugs. GPCRs are “second messengers,” namely they sense chemically affine ligands outside the cell by activating signal transduction pathways leading to cellular response through the production of intracellular and extracellular cAMP (cyclic Adenosyne Mono Phosphate). This cascade of events is activated through the “key-lock” mechanism, for example, whenever affine external ligands land on the cell surface they may activate conformational changes of some transmembrane domain forming GPCRs. This activates the so-called G-Protein, which in turn produced the adenylyl cyclase, ultimately transformed in cAMP.