摘要
G-protein coupled receptor (GPCR) is one of the most important protein families for drug target. GPCR agonists and antagonists occupy approximately one third of the world small molecule drug market. Much effort has been invested in GPCR study by both academic institutions and pharmaceutical industries. With seven-transmembrane do-mains, GPCR plays significant roles in intercellular signal transduction and is involved in a variety of biological path-ways. With the availability of sequence data of human and other mammalian genomes, as well as their expressed se-quence tag (EST) data, the bioinformatics and genomics approaches can be applied to identifying novel GPCR in the post genomic era. Deorphanizing GPCR or matching ligands with GPCR greatly facilitates target validation process and automatically provides a possible compound screening assay. Similarly, bioinformatics data mining approach could also be applied to the identification of GPCR peptide or protein ligands. Here we give a general review of recent advances in the study of GPCR structure, function, as well as GPCR and ligand identification with the emphasis on the bioinformatics database mining of GPCR and their peptide or protein ligands.
G-protein coupled receptor (GPCR) is one of the most important protein families for drug target. GPCR agonists and antagonists occupy approximately one third of the world small molecule drug market. Much effort has been invested in GPCR study by both academic institutions and pharmaceutical industries. With seven-transmembrane do-mains, GPCR plays significant roles in intercellular signal transduction and is involved in a variety of biological path-ways. With the availability of sequence data of human and other mammalian genomes, as well as their expressed se-quence tag (EST) data, the bioinformatics and genomics approaches can be applied to identifying novel GPCR in the post genomic era. Deorphanizing GPCR or matching ligands with GPCR greatly facilitates target validation process and automatically provides a possible compound screening assay. Similarly, bioinformatics data mining approach could also be applied to the identification of GPCR peptide or protein ligands. Here we give a general review of recent advances in the study of GPCR structure, function, as well as GPCR and ligand identification with the emphasis on the bioinformatics database mining of GPCR and their peptide or protein ligands.
基金
supposed by the State“863”High-tech Program of China(Grant No.2001AA231011).
