The "two-headed" peptide inhibitors of interleukin-1 action.
Two peptide fragments of IL-1 family proteins, ITGSE and VTKFYF compete with IL-1 for the cellular receptor. We synthesized a series of peptides composed of the sequences ITGSE and VTKFYK bound directly to each other or connected by such linkers as (Gly)(n), L- and D-Pro residues, Glu and Lys residues (with peptide bond formed by main amino and carboxy groups or by side chain groups), and beta-alanine and its homologues. Peptide IX with a gamma-Glu linker was the most potent inhibitor of IL-1 action. It was twice as potent as both of the peptides indicated.
Kluczyk
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Faculty of Chemistry, University of Wroclaw, Joliot-Curie 14, 50-383, Wroclaw, Poland.
Siemiona
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Wieczorek
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D000818:Animals; D000917:Antibody Formation / Q000187:drug effects; D001667:Binding, Competitive; D007111:Immunity, Cellular / Q000187:drug effects; D007375:Interleukin-1 / Q000037:antagonists & inhibitors*; D051379:Mice; D008808:Mice, Inbred CBA; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology*
D007375:Interleukin-1; D009842:Oligopeptides