title: Positive allosteric modulators for mGluR2 receptors: a medicinal chemistry perspective.
abstract: This review summarizes drug discovery efforts on mGluR2 positive allosteric modulators (PAMs) from 2000 to 2013. Medicinal chemistry programs and the identified 21 chemotypes are analyzed and compared in terms of their biological activity and ligand efficiency. Comparative analysis of ligand efficiency metrics including ligand efficiency and lipophilic ligand efficiency allowed us to identify the most promising chemotypes. The perspective of their clinical development was evaluated in the light of recent human data.
authors.forename: György
authors.initials: G
authors.lastname: Szabó
authors.affiliation: Research Centre for Natural Sciences, Hungarian Academy of Sciences, P.O. Box 17, H-1525 Budapest, Hungary. gy.keseru@ttk.mta.hu.
authors.forename: György Miklós
authors.initials: GM
authors.lastname: Keserű
mesh_terms: D000494:Allosteric Regulation; D000495:Allosteric Site; D001007:Anxiety / Q000188:drug therapy; D002626:Chemistry, Pharmaceutical; D002659:Child Development Disorders, Pervasive / Q000188:drug therapy; D003863:Depression / Q000188:drug therapy; D055808:Drug Discovery; D015507:Drugs, Investigational / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005600:Fragile X Syndrome / Q000188:drug therapy; D006801:Humans; D008024:Ligands; D011619:Psychotropic Drugs / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018094:Receptors, Metabotropic Glutamate / Q000819:agonists / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism*; D012559:Schizophrenia / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D015507:Drugs, Investigational; D008024:Ligands; D011619:Psychotropic Drugs; D018094:Receptors, Metabotropic Glutamate; C108822:metabotropic glutamate receptor 2