Abstract
With the recently completed sequencing and annotation of the human genome, it has become clear that a significant portion of the genome encodes signal-transducing molecules including receptors, protein kinases, ion channels, transporters and coupling proteins. This review focuses on membrane-localized receptors, which represent the largest single group of signal-transducing molecules. Indeed, one can estimate that nearly 10% of the human genome encodes membrane- localized receptors (e.g. G-protein coupled receptors, ligand-gated ion channels and transporters). We have defined that portion of the human genome that encodes receptors the receptorome. In this article, we will demonstrate how the massively parallel screening of the receptorome provides a facile and under-utilized screening platform for drug discovery. Using case studies, we will show how receptorome-based screening elucidates the mechanisms responsible for serious side-effects of both approved and investigational medications. Additionally, we will provide evidence that receptorome- based screening provides insights into novel therapeutic indications of approved medications and serves to validate targets for therapeutic drug discovery.
Keywords: Obesity-Related Molecular Targets, In Silico Receptoromics, Receptor Databases, GPCR, NC-IUPHAR, Weight Gain
Current Pharmaceutical Design
Title: Screening the Receptorome Yields Validated Molecular Targets for Drug Discovery
Volume: 12 Issue: 14
Author(s): Wesley K. Kroeze and Bryan L. Roth
Affiliation:
Keywords: Obesity-Related Molecular Targets, In Silico Receptoromics, Receptor Databases, GPCR, NC-IUPHAR, Weight Gain
Abstract: With the recently completed sequencing and annotation of the human genome, it has become clear that a significant portion of the genome encodes signal-transducing molecules including receptors, protein kinases, ion channels, transporters and coupling proteins. This review focuses on membrane-localized receptors, which represent the largest single group of signal-transducing molecules. Indeed, one can estimate that nearly 10% of the human genome encodes membrane- localized receptors (e.g. G-protein coupled receptors, ligand-gated ion channels and transporters). We have defined that portion of the human genome that encodes receptors the receptorome. In this article, we will demonstrate how the massively parallel screening of the receptorome provides a facile and under-utilized screening platform for drug discovery. Using case studies, we will show how receptorome-based screening elucidates the mechanisms responsible for serious side-effects of both approved and investigational medications. Additionally, we will provide evidence that receptorome- based screening provides insights into novel therapeutic indications of approved medications and serves to validate targets for therapeutic drug discovery.
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Cite this article as:
Kroeze K. Wesley and Roth L. Bryan, Screening the Receptorome Yields Validated Molecular Targets for Drug Discovery, Current Pharmaceutical Design 2006; 12 (14) . https://dx.doi.org/10.2174/138161206776873680
DOI https://dx.doi.org/10.2174/138161206776873680 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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