Met174 side chain is the site of photoinsertion of a substance P competitive peptide antagonist photoreactive in position 8

Numerous photoaffinity studies of the NK-1 receptor have been carried out with peptide agonist analogues of substance P (SP). However, no information is available with regard to the domain interaction of peptide antagonists within this receptor. We describe herein the photoaffinity labelling of the...

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Bibliographic Details
Published in:FEBS letters 2003-06, Vol.544 (1), p.45-49
Main Authors: Sachon, E, Bolbach, G, Lavielle, S, Karoyan, P, Sagan, S
Format: Article
Language:English
Subjects:
Animals
Antagonist
Bapa, biotinyl sulfone aminopentanoic acid
Binding Sites
CHO Cells
Cricetinae
Cyanogen Bromide - pharmacology
hNK-1, human NK-1
Ligands
Light
Matrix-assisted laser desorption/ionization time of flight mass spectrometry
Methionine - chemistry
NK-1 receptor
pBzl, para-benzoyl
Peptides - chemistry
Photolabelling
Receptors, Neurokinin-1 - chemistry
SP, substance P: H-Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Substance P
Substance P - chemistry
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Description
Summary:Numerous photoaffinity studies of the NK-1 receptor have been carried out with peptide agonist analogues of substance P (SP). However, no information is available with regard to the domain interaction of peptide antagonists within this receptor. We describe herein the photoaffinity labelling of the SP receptor with a peptide antagonist analogue, Bapa 0[( pBzl)Phe 8, DPro 9,MePhe 10,Trp(CHO) 11]SP. Photolabelling, enzymatic or chemical cleavage of the covalent complex, purification via streptavidin-coated beads and matrix-assisted laser desorption/ionization time of flight mass spectrometry analysis led us to show that the methyl of Met174 side chain, within the receptor’s second extracellular loop, is covalently linked to the antagonist photoreactive at position 8.
ISSN:0014-5793
1873-3468
DOI:10.1016/S0014-5793(03)00447-2