Abstract
To date, the pharmaceutical industry has placed a considerable amount of interest in the discovery of drug targets and diagnostics. One of the most challenging areas of drug discovery today is the search for novel receptor-ligand pairs. Nuclear receptors comprise a large superfamily of ligand-dependent transcription factors that regulate the expression of genes critical for a variety of biological processes, including development, growth, differentiation, and homeostasis. Orphan nuclear receptors, for which the ligands are not yet identified, represent the most ancient component of the nuclear receptor superfamily. Orphan nuclear receptors not only offer a unique system to uncover novel signaling pathways that impact human health, but also provide excellent targets of drug discoveries for a variety of human diseases. This review highlights advances made on ligand identification for orphan nuclear receptors using transgenic mouse models, cell-based screening, direct binding, structure-based assays, and computer-aided virtual screening. With rapid advances in combinatorial chemistry and high throughput screening, along with other modern technologies, this field promises a bountiful harvest.
Keywords: Ligand identification, cell-based screening, FRET assay, AlphaScreen, structure-based assay, virtual screening, selective nuclear receptor modulators
Combinatorial Chemistry & High Throughput Screening
Title: Orphan Nuclear Receptors, Excellent Targets of Drug Discovery
Volume: 9 Issue: 9
Author(s): Yanhong Shi
Affiliation:
Keywords: Ligand identification, cell-based screening, FRET assay, AlphaScreen, structure-based assay, virtual screening, selective nuclear receptor modulators
Abstract: To date, the pharmaceutical industry has placed a considerable amount of interest in the discovery of drug targets and diagnostics. One of the most challenging areas of drug discovery today is the search for novel receptor-ligand pairs. Nuclear receptors comprise a large superfamily of ligand-dependent transcription factors that regulate the expression of genes critical for a variety of biological processes, including development, growth, differentiation, and homeostasis. Orphan nuclear receptors, for which the ligands are not yet identified, represent the most ancient component of the nuclear receptor superfamily. Orphan nuclear receptors not only offer a unique system to uncover novel signaling pathways that impact human health, but also provide excellent targets of drug discoveries for a variety of human diseases. This review highlights advances made on ligand identification for orphan nuclear receptors using transgenic mouse models, cell-based screening, direct binding, structure-based assays, and computer-aided virtual screening. With rapid advances in combinatorial chemistry and high throughput screening, along with other modern technologies, this field promises a bountiful harvest.
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Cite this article as:
Shi Yanhong, Orphan Nuclear Receptors, Excellent Targets of Drug Discovery, Combinatorial Chemistry & High Throughput Screening 2006; 9 (9) . https://dx.doi.org/10.2174/138620706778700125
DOI https://dx.doi.org/10.2174/138620706778700125 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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