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Journal of Psychopharmacology, Vol. 20, No. 4 suppl, 41-46 (2006)
DOI: 10.1177/1359786806066045

Screening the receptorome

Wesley K. Kroeze

Department of Biochemistry, Case Western Reserve University Medical School, Cleveland, OH, USA.

Bryan L. Roth

Departments of Biochemistry, Psychiatry, Neurosciences and Oncology, Case Western Reserve University Medical School and NIMH Psychoactive Drug Screening Program, Cleveland, OH, USA.

The term ‘receptorome’ is now being used to describe receptors, ion channels and transporters in the human genome that are potential drug targets. These proteins comprise a considerable fraction of the human genome, and include the G protein-coupled receptors, which are the targets for many medications. In this review, we summarize recent advances in the field, including the concept that the ultimate goal of drug discovery may not be the development of highly selective single-target drugs, the idea that potential side-effects can also be the goal of multi-target drug screening, and a discussion of the application of computational screening and public domain databases available to interested investigators.

Key Words: receptorome • G protein-coupled receptors (GPCR) • high-throughput screening • selectivity • salvinorin A • fen-phen • HERG • weight gain • database


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