Millipore Technical Publications |
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GPCRProfiler Allosteric Services: AllostericProfiler and AllostericScreener | ||
| Lit No: | DS1064EN00 | |
| Year: | 2009 | |
Allosteric compounds—the future of GPCR Drug DiscoveryHistorically, GPCR/7TM drug development has been focused on compounds that interact with the receptors’ orthosteric site, the site at which the native ligand binds. Even though the GPCR family has been a prolific drug target demonstrating the past success of this approach, there are clear limitations that have hampered past and recent drug development campaigns. For example, the orthosteric binding site can be highly conserved within a ligand family making it extremely difficult to generate receptor-specific compounds. Moreover, intellectual property has severely restricted the chemical space in which to work for orthosteric ligands thus hindering drug development for many valuable receptors. More and more researchers recognize that many of these constraints can be surmounted by exploiting completely new GPCR interaction sites that are topographically distinct from a receptor’s orthosteric site, otherwise know as allosteric sites. Click the PDF above for the full document. | |
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