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Synthesis and characterization of photoactivatable peptide agonists of the human thrombin receptor
Author(s) -
Bischoff Rainer,
Cordier Yves,
Rasmussen Ulla B.,
Schlesinger Yasmin,
Gachet Christian,
Jaquinod Michel,
Tripet Brian,
Chong Pele C.S.,
Pavirani Andrea
Publication year - 1994
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(93)00692-b
Subject(s) - agonist , chemistry , peptide , receptor , thrombin , biotin , biochemistry , phenylalanine , stereochemistry , amino acid , biology , platelet , immunology
Chemical synthesis and biochemical analysis of modified agonist peptides of the human thrombin receptor derived from the sequence SFLLRNP containing photoactivatable azido groups and biotin for sensitive detection is described. Substitution of leucine in position three with p ‐azidophenylalanine and extension of the C‐terminus with a KGGK spacer containing biotin covalently linked to the side chain of the C‐terminal lysine residue resulted in an active receptor agonist as determined by intracellular Ca 2+ mobilization in human erythroleukemia (HEL) cells. In contrast, substitution of phenylalanine in position two with p ‐azidophenylalanine reduced agonist activity significantly.