Conformational changes in G-protein-coupled receptors-the quest for functionally selective conformations is open. Export

@article{citeulike:2103388, abstract = {The G-protein-coupled receptors (GPCRs) represent one the largest families of drug targets. Upon agonist binding a receptor undergoes conformational rearrangements that lead to a novel protein conformation which in turn can interact with effector proteins. During the last decade significant progress has been made to prove that different conformational changes occur. Today it is mostly accepted that individual ligands can induce different receptor conformations. However, the nature or molecular identity of the different conformations is still ill-known. Knowledge of the potential functionally selective conformations will help to develop drugs that select specific conformations of a given GPCR which couple to specific signalling pathways and may, ultimately, lead to reduced side effects. In this review we will summarize recent progress in biophysical approaches that have led to the current understanding of conformational changes that occur during GPCR activation.}, address = {1Institut of Pharmacology and Toxicology, Universit\"{a}t W\"{u}rzburg, W\"{u}rzburg, Germany.}, author = {Hoffmann, C. and Z\"{u}rn, A. and B\"{u}nemann, M. and Lohse, M. J.}, citeulike-article-id = {2103388}, citeulike-linkout-0 = {http://dx.doi.org/10.1038/sj.bjp.0707615}, citeulike-linkout-1 = {http://view.ncbi.nlm.nih.gov/pubmed/18059316}, citeulike-linkout-2 = {http://www.hubmed.org/display.cgi?uids=18059316}, day = {3}, doi = {10.1038/sj.bjp.0707615}, issn = {0007-1188}, journal = {British journal of pharmacology}, keywords = {gpcrs, review}, month = {March}, posted-at = {2009-05-26 08:41:58}, priority = {5}, title = {Conformational changes in G-protein-coupled receptors-the quest for functionally selective conformations is open.}, url = {http://dx.doi.org/10.1038/sj.bjp.0707615}, volume = {153 Suppl 1}, year = {2008} }

TY - JOUR ID - citeulike:2103388 L3 - citeulike-article-id:2103388 N2 - The G-protein-coupled receptors (GPCRs) represent one the largest families of drug targets. Upon agonist binding a receptor undergoes conformational rearrangements that lead to a novel protein conformation which in turn can interact with effector proteins. During the last decade significant progress has been made to prove that different conformational changes occur. Today it is mostly accepted that individual ligands can induce different receptor conformations. However, the nature or molecular identity of the different conformations is still ill-known. Knowledge of the potential functionally selective conformations will help to develop drugs that select specific conformations of a given GPCR which couple to specific signalling pathways and may, ultimately, lead to reduced side effects. In this review we will summarize recent progress in biophysical approaches that have led to the current understanding of conformational changes that occur during GPCR activation. JF - British journal of pharmacology SN - 0007-1188 AD - 1Institut of Pharmacology and Toxicology, Universität Würzburg, Würzburg, Germany. TI - Conformational changes in G-protein-coupled receptors-the quest for functionally selective conformations is open. VL - 153 Suppl 1 KW - gpcrs KW - review AU - Hoffmann, C AU - Zürn, A AU - Bünemann, M AU - Lohse, MJ PY - 2008/03/03/ UR - http://dx.doi.org/10.1038/sj.bjp.0707615 ER -