Abstract：
:In recent years, the concept of allosteric modulation of G-protein-coupled receptors (GPCRs) has matured and now represents an increasingly viable approach to drug discovery. This is evident in the fact that allosteric modulators have been reported for every class of GPCR, and several are currently in clinical trials with one drug example approved and launched. The allosteric approach has been highlighted for the potential of identifying highly selective compounds with a minimal propensity to produce adverse effect. While much has been written regarding the promises of this approach, important challenges, caveats, and pitfalls exist that are often overlooked. Therefore, a balanced overview of the field that describes both the promises and the challenges of discovering allosteric modulators of GPCRs as novel drugs is presented.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Raddatz R,Schaffhauser H,Marino MJdoi
10.1016/j.bcp.2007.05.007subject
Has Abstractpub_date
2007-08-01 00:00:00pages
383-91issue
3eissn
0006-2952issn
1873-2968pii
S0006-2952(07)00299-7journal_volume
74pub_type
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