Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach. Export

@article{citeulike:2251486, abstract = {We disclose the first selective, nonpeptidic, small-molecule somatostatin receptor subtype 5 (SST5R) antagonists that were identified by a chemogenomics approach based on the analysis of the homology of amino acids defining the putative consensus drug binding site of SST5R. With this strategy, opioid, histamine, dopamine, and serotonine receptors were identified as the closest neighbors of SST5R. The H1 antagonist astemizole was chosen as a seed structure and subsequently transformed into a SST5 receptor antagonist with nanomolar binding affinity devoid of the original target activity.}, address = {rainer\_e.martin@roche.com.}, author = {Martin, R. E. and Green, L. G. and Guba, W. and Kratochwil, N. and Christ, A.}, citeulike-article-id = {2251486}, citeulike-linkout-0 = {http://dx.doi.org/10.1021/jm701143p}, citeulike-linkout-1 = {http://pubs.acs.org/doi/abs/10.1021/jm701143p}, citeulike-linkout-2 = {http://view.ncbi.nlm.nih.gov/pubmed/18020390}, citeulike-linkout-3 = {http://www.hubmed.org/display.cgi?uids=18020390}, day = {13}, doi = {10.1021/jm701143p}, issn = {0022-2623}, journal = {J Med Chem}, keywords = {drug, drugdiscovery, screening}, month = {December}, number = {25}, pages = {6291--6294}, posted-at = {2008-01-18 16:02:24}, priority = {2}, title = {Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.}, url = {http://dx.doi.org/10.1021/jm701143p}, volume = {50}, year = {2007} }

TY - JOUR ID - citeulike:2251486 L3 - citeulike-article-id:2251486 N2 - We disclose the first selective, nonpeptidic, small-molecule somatostatin receptor subtype 5 (SST5R) antagonists that were identified by a chemogenomics approach based on the analysis of the homology of amino acids defining the putative consensus drug binding site of SST5R. With this strategy, opioid, histamine, dopamine, and serotonine receptors were identified as the closest neighbors of SST5R. The H1 antagonist astemizole was chosen as a seed structure and subsequently transformed into a SST5 receptor antagonist with nanomolar binding affinity devoid of the original target activity. IS - 25 JF - J Med Chem SN - 0022-2623 AD - rainer_e.martin@roche.com. EP - 6294 TI - Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach. VL - 50 SP - 6291 KW - drug KW - drugdiscovery KW - screening AU - Martin, RE AU - Green, LG AU - Guba, W AU - Kratochwil, N AU - Christ, A PY - 2007/12/13/ UR - http://dx.doi.org/10.1021/jm701143p ER -