title: Amphipols in G protein-coupled receptor pharmacology: what are they good for?
abstract: G protein-coupled receptors are at a central node of all cell communications. Investigating their molecular functioning is therefore crucial for both academic purposes and drug design. However, getting the receptors as isolated, stable and purified proteins for such studies still stumbles over their instability out of the membrane environment. Different membrane-mimicking environments have been developed so far to increase the stability of purified receptors. Among them are amphipols. These polymers not only preserve the native fold of receptors purified from membrane fractions but they also allow specific applications such as folding receptors purified from inclusion bodies back to their native state. Of importance, amphipol-trapped G protein-coupled receptors essentially maintain their pharmacological properties so that they are perfectly adapted to further investigate the molecular mechanisms underlying signaling processes. We review here how amphipols have been used to refold and stabilize detergent-solubilized purified receptors and what are the main subsequent molecular pharmacology analyses that were performed using this strategy.
authors.affiliation: Faculté de Pharmacie, Institut des Biomolécules Max Mousseron (IBMM), CNRS UMR 5247, Université Montpellier 1 et 2, BP 14491, 15 Avenue Charles Flahault, 34093, Montpellier Cedex 5, France.
authors.forename: Sophie
authors.initials: S
authors.lastname: Mary
authors.forename: Marjorie
authors.initials: M
authors.lastname: Damian
authors.forename: Rita
authors.initials: R
authors.lastname: Rahmeh
authors.forename: Bernard
authors.initials: B
authors.lastname: Mouillac
authors.forename: Jacky
authors.initials: J
authors.lastname: Marie
authors.forename: Sébastien
authors.initials: S
authors.lastname: Granier
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Banères
mesh_terms: D000818:Animals; D002462:Cell Membrane / Q000737:chemistry*; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008565:Membrane Proteins / Q000737:chemistry; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology*; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000187:drug effects* / Q000302:isolation & purification; D012995:Solubility; D012996:Solutions; D013501:Surface-Active Agents / Q000737:chemistry*; D014867:Water / Q000737:chemistry*
chemical_list: D008565:Membrane Proteins; D011108:Polymers; D043562:Receptors, G-Protein-Coupled; D012996:Solutions; D013501:Surface-Active Agents; D014867:Water