Photoprobe Peptides to Map the Interactions of Angiotensin II with its Receptor AT1
Seven transmembrane domains (TMDs) G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors and are implicated in various pathologies. In fact, those proteins are privileged targets in pharmacotherapy since approximatively 50% of all current market drugs act via these receptors. The rational design of drugs targeting GPCRs requires a 3D molecular-based knowledge of those proteins that may be acquired by identification of ligand-receptor interactions through photoaffinity labeling . This approach allows to directly map the ligand-receptor interface by covalent bonding of the radio-labeled photoprobe ligand within the immediate molecular surroundings of its cognate receptor. This information may then be used in conjunction with computational molecular modeling procedures, based on the X-ray crystallography of bovine rhodopsin, to build and validate homology molecular models of receptors with ligand . In the present contribution, we have...
KeywordsProteinaceous Material Bovine Rhodopsin Photoaffinity Label Helical Bundle Neutral Antagonist
This ongoing study is funded by the Canadian Institutes of Health Research (CIHR) and the Quebec chapter of the Heart and Stroke Foundation of Canada (HSFC) to G.G., R.L. and E.E.
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