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Bioorg Med Chem Lett. 2008 Dec 1;18(23):6240-3. doi: 10.1016/j.bmcl.2008.09.101. Epub 2008 Oct 2.

Synthesis of new sulfonate and phosphonate derivatives for cation-independent mannose 6-phosphate receptor targeting.

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Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Université Montpellier 2 et 1, Bâtiment de Recherche Max Mousseron, Ecole Nationale Supérieure de Chimie de Montpellier, 8 Rue de l'Ecole Normale, F-34296 Montpellier Cedex 05, France.


The cation-independent mannose 6-phosphate receptor (CI-M6PR) is essential for the endocytosis of proteins bearing the mannose 6-phosphate (M6P) recognition marker. This study described the synthesis of M6P and M6S analogs presenting greater affinity for CI-M6PR than their natural compounds. Moreover, the finding of their lack of cytotoxicity for human cells and of their increased stability in human serum supports the high potential of these isosteric derivatives in therapies requiring CI-M6PR targeting.

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