Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 selective ligands
- 29 January 2008
- journal article
- review article
- Published by Wiley in British Journal of Pharmacology
- Vol. 153 (2) , 335-346
- https://doi.org/10.1038/sj.bjp.0707567
Abstract
Recent developments indicate that CB2 receptor ligands have the potential to become therapeutically important. To explore this potential, it is necessary to develop compounds with high affinity for the CB2 receptor and little affinity for the CB1 receptor. This review will discuss structure‐activity relations at both receptors for classical cannabinoids and cannabimimetic indoles. Examples of CB2 selective ligands from both classes of compounds are presented and the structural features leading to selectivity are described. Two approaches, receptor mutations and molecular modelling, have been employed to investigate the interaction of ligands with both cannabinoid receptors. These results obtained from these techniques are discussed.British Journal of Pharmacology(2008)153, 335–346; doi:10.1038/sj.bjp.0707567; published online 5 November 2007Keywords
This publication has 68 references indexed in Scilit:
- G protein coupled receptor structure and activationBiochimica et Biophysica Acta (BBA) - Biomembranes, 2007
- Crystal structure of a photoactivated deprotonated intermediate of rhodopsinProceedings of the National Academy of Sciences, 2006
- The effects of charge‐neutralizing mutation D6.30N on the functions of CB1 and CB2 cannabinoid receptorsFEBS Letters, 2006
- GPR55 as a New Cannabinoid Receptor: Still a Long Way to Prove ItChemical Biology & Drug Design, 2006
- 1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indolesBioorganic & Medicinal Chemistry Letters, 2005
- Chemical modification of the naphthoyl 3-position of JWH-015: In search of a fluorescent probe to the cannabinoid CB2 receptorBioorganic & Medicinal Chemistry Letters, 2005
- Cysteine 2.59(89) in the Second Transmembrane Domain of Human CB2 Receptor Is Accessible within the Ligand Binding Crevice: Evidence for Possible CB2 Deviation from a Rhodopsin TemplateMolecular Pharmacology, 2005
- Development and validation of a genetic algorithm for flexible docking 1 1Edited by F. E. CohenJournal of Molecular Biology, 1997
- New class of potent ligands for the human peripheral cannabinoid receptorBioorganic & Medicinal Chemistry Letters, 1996
- Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptorsBioorganic & Medicinal Chemistry Letters, 1996