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

Gérard, Estelle;Meulle, Aline;Feron, Olivier;Marchand-Brynaert, Jacqueline
(2012) Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology — Vol. 22, n° 1, p. 586-590 (2012)

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Authors
  • Gérard, EstelleUCLouvain
    Author
  • Meulle, AlineUCLouvain
    Author
  • Author
  • Marchand-Brynaert, JacquelineUCLouvain
    Author
Abstract
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.
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Citations

Gérard, E., Meulle, A., Feron, O., & Marchand-Brynaert, J. (2012). LDV peptidomimetics equipped with biotinylated spacer-arms: synthesis and biological evaluation on CCRF-CEM cell line. Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology, 22(1), 586-590. https://doi.org/10.1016/j.bmcl.2011.10.078 (Original work published 2012)