engleski

Towards structural studies of cannabinoid CB2 and vasopressin V2 receptors

Cannabinoid CB2 receptor and vasopressin V2 receptor are G protein-coupled receptors involved in several important physiological processes in a human organism. CB2 is a part of the “endocannabinoid system” and is predominantly present in immune and peripheral nervous systems. It is valuable drug target for treating inflammatory diseases, pain, osteoporosis, atherosclerosis and brain tumors. V2 is present in kidneys and has an important role in maintaining water homeostasis in human organism. It is targeted in treatment of diabetes insipidus and hyponatremia. In order to understand mechanisms by which different effectors modulate activities of CB2 and V2 receptors, we are aiming at determining molecular structures of these receptors with bound ligands, both agonists and antagonists. This involves stabilization and crystallization of the receptor molecules and, finally, determination of their structures by X-ray crystallography. We will present our recent advances in engineering human CB2 and V2 receptors for structural studies.

V2 receptor; CB2 receptor; GPCR

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