Physiological relevance of GPCR oligomerization and its impact on drug discovery. Export

@article{citeulike:3416825, abstract = {The potentially large functional and physiological diversity of G-protein coupled receptor (GPCR) dimers has generated a great deal of excitement about the opportunity that dimerization provides for enabling novel drug discovery. The discovery of physiologically relevant GPCR dimers suggests that new drug targets for diseases such as schizophrenia and pre-eclampsia can be developed by targeting dimers. Most of the previous work on GPCR dimers made use of the overexpression of differentially tagged GPCRs in heterologous cell systems. Current emphasis on the development of physiologically relevant cell systems that endogenously express the appropriate combination of GPCR dimers and accessory proteins is leading to dramatic increases in our understanding of GPCR dimers. These and other new tools such as GPCR-specific antibodies will be required to develop GPCR dimer specific drugs. Given that ligands are available for only a small percentage of the large number of potentially druggable GPCRs, the use of GPCR dimers might provide the necessary targets to increase the breadth and depth of receptors available for therapeutic interventions.}, author = {Panetta, Rosemarie and Greenwood, Michael T.}, citeulike-article-id = {3416825}, citeulike-linkout-0 = {http://dx.doi.org/10.1016/j.drudis.2008.09.002}, citeulike-linkout-1 = {http://linkinghub.elsevier.com/retrieve/pii/S1359644608003073}, citeulike-linkout-2 = {http://view.ncbi.nlm.nih.gov/pubmed/18824244}, citeulike-linkout-3 = {http://www.hubmed.org/display.cgi?uids=18824244}, day = {14}, doi = {10.1016/j.drudis.2008.09.002}, issn = {1359-6446}, journal = {Drug discovery today}, keywords = {dimer, disease, drug, gpcr, ligands, pharmacology, review}, month = {December}, number = {23-24}, pages = {1059--1066}, posted-at = {2008-10-16 09:57:50}, priority = {2}, title = {Physiological relevance of GPCR oligomerization and its impact on drug discovery.}, url = {http://dx.doi.org/10.1016/j.drudis.2008.09.002}, volume = {13}, year = {2008} }

TY - JOUR ID - citeulike:3416825 L3 - citeulike-article-id:3416825 N2 - The potentially large functional and physiological diversity of G-protein coupled receptor (GPCR) dimers has generated a great deal of excitement about the opportunity that dimerization provides for enabling novel drug discovery. The discovery of physiologically relevant GPCR dimers suggests that new drug targets for diseases such as schizophrenia and pre-eclampsia can be developed by targeting dimers. Most of the previous work on GPCR dimers made use of the overexpression of differentially tagged GPCRs in heterologous cell systems. Current emphasis on the development of physiologically relevant cell systems that endogenously express the appropriate combination of GPCR dimers and accessory proteins is leading to dramatic increases in our understanding of GPCR dimers. These and other new tools such as GPCR-specific antibodies will be required to develop GPCR dimer specific drugs. Given that ligands are available for only a small percentage of the large number of potentially druggable GPCRs, the use of GPCR dimers might provide the necessary targets to increase the breadth and depth of receptors available for therapeutic interventions. IS - 23-24 JF - Drug discovery today SN - 1359-6446 EP - 1066 TI - Physiological relevance of GPCR oligomerization and its impact on drug discovery. VL - 13 SP - 1059 KW - dimer KW - disease KW - drug KW - gpcr KW - ligands KW - pharmacology KW - review AU - Panetta, Rosemarie AU - Greenwood, Michael PY - 2008/12/14/ UR - http://dx.doi.org/10.1016/j.drudis.2008.09.002 ER -