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Identification of an N-formyl peptide receptor ligand binding domain by a gain-of-function approach
Quehenberger O.2; Pan Z.K.1; Prossnitz E.R.1; Cavanagh S.L.1; Cochrane C.G.1; Ye R.D.1
1997-09-18
Source PublicationBiochemical and Biophysical Research Communications
ISSN0006291X
Volume238Issue:2Pages:377-381
AbstractReplacement of N-formyl peptide receptor (FPR) domains with those from a homologous receptor, FPR2, resulted in chimeric receptors displaying low binding affinity to fMet-Leu-Phe (fMLF). To characterize fMLF binding domain, we adopted a 'gain-of-function' approach by selective replacement of non-conserved residues in the FPR2 portion of the chimeric receptors with those from the FPR. This led to the identification of 3 clusters of residues required for high-affinity fMLF binding. Introduction of 2 positively charged amino acids, Arg and Lys, dramatically improved binding affinity of one chimeric receptor (K(d) from 105 nM to 1.6 nM). Similarly, restoration of either Gly/His or Phe/Thr improved the binding affinity of another chimeric receptor from a K(d) of 275 nM to a 2.3 K(d) and 3.3 nM, respectively. Increased ligand binding affinity was accompanied by a gain in calcium mobilization capability, suggesting functional coupling to G proteins. These results demonstrate the presence of structural determinants in the first extracellular loop and its adjacent transmembrane domains that are essential for high affinity fMLF binding.
DOI10.1006/bbrc.1997.7298
URLView the original
Language英語
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Cited Times [WOS]:23   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.Scripps Research Institute
2.University of California, San Diego
Recommended Citation
GB/T 7714
Quehenberger O.,Pan Z.K.,Prossnitz E.R.,et al. Identification of an N-formyl peptide receptor ligand binding domain by a gain-of-function approach[J]. Biochemical and Biophysical Research Communications,1997,238(2):377-381.
APA Quehenberger O.,Pan Z.K.,Prossnitz E.R.,Cavanagh S.L.,Cochrane C.G.,&Ye R.D..(1997).Identification of an N-formyl peptide receptor ligand binding domain by a gain-of-function approach.Biochemical and Biophysical Research Communications,238(2),377-381.
MLA Quehenberger O.,et al."Identification of an N-formyl peptide receptor ligand binding domain by a gain-of-function approach".Biochemical and Biophysical Research Communications 238.2(1997):377-381.
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