Lebetin peptides: potent platelet aggregation inhibitors

Haemostasis
Naziha MarrakchiMohamed El Ayeb

Abstract

Lebetins from Macrovipera lebetina snake venom constitute a new class of inhibitors of platelet aggregation. There are two groups of peptides: lebetin 1 (L1; 11- to 13-mer) and lebetin 2 (L2; 37- to 38-mer). The short lebetins are identical to the N-terminal segments of the longer ones. They inhibit platelet aggregation induced by various agonists (e.g. thrombin, PAF-acether or collagen). The shortest lebetin (11-mer) shows potent inhibition of rabbit (IC(50) = 7 nM) and human (IC(50) = 5 nM) platelets. They prevent collagen-induced thrombocytopenia in rats. N- and C-terminal-truncated synthetic L1gamma (sL1gamma; 11-mer) is less active in inhibiting platelet aggregation than the native peptide. Results from Ala scan studies of the sL1gamma peptide indicated that replacement of the residues (P3, G7, P8, P9 or N10) resulted in a remarkable drop in the activity, whereas replacement of residues K2, P4 or K6 by Ala resulted in enhancement of the antiplatelet activity by at least 10-fold. To examine the activity of multimeric L1gamma, several multimeric peptides were synthesized using the multiple-antigen peptide system assembled on a branched lysine core and their antiplatelet activity was evaluated in vitro. The largest multimeric...Continue Reading

Citations

May 31, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Julien DimastromatteoCatherine Ghezzi
Jul 11, 2007·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·K HagiharaT Ikeda
Oct 1, 2005·Journal of Peptide Science : an Official Publication of the European Peptide Society·Petr NiederhafnerJan Jezek

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