Using the third extracellular loop of the MC4 receptor in screening for pharmaceutical agents, e.g. for diagnosis, prevention or treatment of obesity, also new mutated MC4 receptors and their complexes

摘要

Use of the third extracellular loop (EC3) of the MC4 receptor, or part of it, for developing and/or preparing an agent for treatment, prevention and/or diagnosis of disease. Independent claims are also included for the following: (1) mutated MC4 receptors having any of 21 (combinations of) mutations, or any of 23 sequences reproduced, or encoded by nucleic acid sequences that encode these sequences, or encoded by any of 23 sequences, reproduced, or their complements; (2) complex (C), preferably isolated, comprising at least one MC4 receptor and at least one G protein-coupled receptor (X); and (3) use of nucleic acid that encodes EC3, or part of it, for preparing nucleic acid that interacts with the EC3-encoding sequence. ACTIVITY : Anorectic; Antidiabetic; Cardiant; Cytostatic; Vasotropic. MECHANISM OF ACTION : The developed agents interact with EC3, or its disulfide bridge; promote or inhibit complex formation, particularly dimerization of the MC4 receptor; interact with surface regions of the MC4-containing complex, or they interact with nucleic acid that encodes EC3 or (mutant) MC4 receptors.