A hexapeptide VTKFYF from C-terminal part of interleukin-1 receptor antagonist, an inhibitor of IL-1-IL-1 receptor interaction.
In order to find the low-molecular-weight interleukin-1 (IL-1) inhibitors we synthesized a series of peptides, derived from three regions of interleukin-1 receptor antagonist (IL-1ra): N-terminal (residues 5-9), central (90-98) and C-terminal (143-148). The decision was based on the thorough analysis of structural and functional properties of IL-1 proteins and the resemblance of some fragments of IL-1ra to well-known immunomodulators, like thymopentin and tuftsin. The competition between our peptides and IL-1 was measured as the inhibition of IL-1 induced IL-2 production in LBRM/CTLL cell line system. The activity of tuftsin (TKPR), a peptide immunomodulator derived from IgG molecule, was also examined. All peptides presented some activity, although the most interesting results (when the range of activity and dose-dependence were taken into account) were obtained for tuftsin and peptide VTKFYF from the C-terminal part of IL-1ra, which is in agreement with the latest reports on the structure of IL-1ra-receptor complex.
Wieczorek
Z
Z
Institute of Immunology and Experimental Therapy, Wrocław, Poland.
Kluczyk
A
A
Słoń-Usakiewicz
J J
JJ
Siemion
I Z
IZ
D002460:Cell Line; D003124:Colorimetry; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D007375:Interleukin-1 / Q000037:antagonists & inhibitors / Q000737:chemistry; D007376:Interleukin-2 / Q000096:biosynthesis; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017472:Receptors, Interleukin-1 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship; D014405:Tuftsin / Q000494:pharmacology
D007375:Interleukin-1; D007376:Interleukin-2; D009842:Oligopeptides; D017472:Receptors, Interleukin-1; D014405:Tuftsin