Linked Life Data

12695527

Source:http://linkedlifedata.com/resource/pubmed/id/12695527

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
2003-4-15
pubmed:abstractText
The amino-terminal domain of class B G protein-coupled receptors is critically important for natural peptide agonist binding and action. The precise role it plays and the molecular basis of the interaction between ligand and this domain are not well understood. In the current work, we have developed a new probe for affinity labeling the secretin receptor through a photolabile benzoyl-phenylalanine residue in position 13. This represented a high affinity ligand (K(i) = 56 +/- 8 nM) that was a potent full agonist to stimulate cellular cAMP (EC(50) = 236 +/- 22 pM). It covalently labeled the secretin receptor saturably in a single site. This was localized to the amino-terminal domain near the first transmembrane segment using a series of chemical and enzymatic digestions. Edman degradation sequencing of radiolabeled cyanogen bromide and skatole digestion products that were attached to glass beads and further cleaved with endoproteinase Asp-N demonstrated that the labeled residue represented Val(103). This is in contrast with previous photoaffinity labeling through positions 6, 18, 22, and 26 of secretin that all labeled the distal end of the amino terminus of this receptor. Together, these five pairs of residue-residue approximations provide important constraints to better understand the molecular conformation of the agonist-bound receptor.
pubmed:grant
pubmed:commentsCorrections
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0026-895X
pubmed:author
pubmed:issnType
Print
pubmed:volume
63
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
993-1001
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
2003
pubmed:articleTitle
Spatial approximation between a photolabile residue in position 13 of secretin and the amino terminus of the secretin receptor.
pubmed:affiliation
Cancer Center and the Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic Scottsdale, Scottsdale, Arizona 85259, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't