Linked Life Data

11579442

Source:http://linkedlifedata.com/resource/pubmed/id/11579442

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
2001-10-1
pubmed:abstractText
G-protein-coupled receptors (GPCRs) allow cells to respond to calcium, hormones, and neurotransmitters. Not surprisingly, they currently make up the largest family of validated drug targets. Rational drug design for molecular regulators targeting GPCRs has been limited to theoretical-based computational approaches. X-ray crystallography of intact GPCRs has provided the topological orientation of the seven transmembrane helices, but limited structural information of the extracellular and intracellular loops and protein termini. In this review we detail an NMR-based approach which provides the high-resolution structural features on the extracellular domains of GPCRs and the ligand/receptor complexes formed upon titration of the peptide hormone. The results provide important contact points and a high-resolution description of the ligand/receptor interactions, which may be useful for the rational design of therapeutic agents targeting GPCRs. Recent results from our investigation of the cholecystokinin peptide hormone system are used to highlight this approach.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0198-6325
pubmed:author
pubmed:copyrightInfo
Copyright 2001 John Wiley & Sons, Inc. Med Res Rev, 21, No. 5, 450-471, 2001
pubmed:issnType
Print
pubmed:volume
21
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
450-71
pubmed:dateRevised
2007-3-22
pubmed:meshHeading
pubmed:year
2001
pubmed:articleTitle
Peptide hormone binding to G-protein-coupled receptors: structural characterization via NMR techniques.
pubmed:affiliation
Department of Molecular Pharmacology, Division of Biology & Medicine, Brown University, Providence, Rhode Island 02912, USA. dale_mierke@brown.edu
pubmed:publicationType
Journal Article, Review