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Chembiochem. 2017 Apr 18;18(8):782-789. doi: 10.1002/cbic.201600673. Epub 2017 Mar 22.

Lactosamine-Based Derivatives as Tools to Delineate the Biological Functions of Galectins: Application to Skin Tissue Repair.

Author information

1
Faculté des Sciences et des Techniques, Unité Fonctionnalité et Ingénierie des Protéines (UFIP), Université de Nantes, UMR CNRS 6286, 2 chemin de la Houssinière, B. P. 92208, 44322, Nantes Cedex 3, France.
2
Université Paris Diderot-Paris 7 Sorbonne Paris Cité, Institut Jacques Monod, UMR CNRS 7592, 15 rue Hélène Brion, 75205, Paris Cedex 13, France.

Abstract

Galectins have been recognized as potential novel therapeutic targets for the numerous fundamental biological processes in which they are involved. Galectins are key players in homeostasis, and as such their expression and function are finely tuned in vivo. Thus, their modes of action are complex and remain largely unexplored, partly because of the lack of dedicated tools. We thus designed galectin inhibitors from a lactosamine core, functionalized at key C2 and C3' positions by aromatic substituents to ensure both high affinity and selectivity, and equipped with a spacer that can be modified on demand to further modulate their physico-chemical properties. As a proof-of-concept, galectin-3 was selectively targeted. The efficacy of the synthesized di-aromatic lactosamine tools was shown in cellular assays to modulate collective epithelial cell migration and to interfere with actin/cortactin localization.

KEYWORDS:

cell migration; drug design; galectin-3; inhibitors; skin tissue repair; wound healing

PMID:
28166391
DOI:
10.1002/cbic.201600673
[Indexed for MEDLINE]

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