LDV peptidomimetics equipped with biotinylated spacer-arms: synthesis and biological evaluation on CCRF-CEM cell line.

Gérard, Estelle [UCL] Meulle, Aline [UCL] Feron, Olivier [UCL] Marchand-Brynaert, Jacqueline [UCL]

The tripeptide Leu-Asp-Val (LDV) is known to bind α(4)β(1) integrin in leukemia cells. Here we have synthesized a LDV peptidomimetic equipped with a biotin-conjugated spacer-arm. Compound 9 acts as an inhibitor of the α(4)β(1) integrin in an adhesion assay using fluorescently labeled, α(4)β(1) integrin-expressing leukemia CCRF-CEM cells. Furthermore, when bound to neutravidin-coated plates, compound 9 could capture CCRF-CEM cells. Such biotin-conjugated LDV peptidomimetic may thus represent a novel tool for biotechnological applications using avidin interaction for leukapheresis or leukemia cell targeting.