Galectins, a family of animal lectins, are involved in numerous types of cancer.1 They exhibit a characteristic carbohydrate-recognition domain and interact selectively with glycoconjugates of cell surfaces. These interactions introduce biomolecular processes as immune reactions, cell growth and tumor progression. 2-4 An improved understanding of the underlying mechanisms may provide further opportunities for developing therapies based on the immunoregulatory properties of this protein family.Galectin-1, a prominent member of this protein family, is overexpressed in malignant tissues and binds �-galactosides.3,4 The binding constants of such natural carbohydrates presented on cell surfaces range in the micromolar and demonstrate the need for the identification and development of highly affine and selective ligands.We present a self-generating approach for the synthesis of promising binding partners of Galectin-1.Such studies combine docking experiments, synthesis and activity assays on living cells.  (1)     Thijssen, V.; Poirier, F.; Baum, L. G.; Griffioen, A. W. Blood 2007 , 110, 2819.(2)     Rabinovich, G. A.; Toscano, M. A. Nat. Rev. Immunol. 2009 , 9, 338.(3)     Vasta, G. R. Nat. Rev. Microbiol. 2009 , 7, 424.(4)     Camby, I.; Le Mercier, M.; Lefranc, F.; Kiss, R. Glycobiolgy 2006 , 16, 137R.

Self-generating synthesis for the design of Galectin-1 inhibitors

243rd National Meeting (2012)

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