Skip to main content
placeholder image

Inhibitors of galectins and implications for structure-based design of galectin-specific therapeutics

Journal Article


Abstract


  • Galectins are a family of galactoside-specific lectins that are involved in a myriad of metabolic and disease processes. Due to roles in cancer and inflammatory and heart diseases, galectins are attractive targets for drug development. Over the last two decades, various strategies have been used to inhibit galectins, including polysaccharide-based therapeutics, multivalent display of saccharides, peptides, peptidomimetics, and saccharide-modifications. Primarily due to galectin carbohydrate binding sites having high sequence identities, the design and development of selective inhibitors targeting particular galectins, thereby addressing specific disease states, is challenging. Furthermore, the use of different inhibition assays by research groups has hindered systematic assessment of the relative selectivity and affinity of inhibitors. This review summarises the status of current inhibitors, strategies, and novel scaffolds that exploit subtle differences in galectin structures that, in conjunction with increasing available data on multiple galectins, is enabling the feasible design of effective and specific inhibitors of galectins.

Publication Date


  • 2014

Citation


  • Blanchard, H., Bum-Erdene, K., & Hugo, M. W. (2014). Inhibitors of galectins and implications for structure-based design of galectin-specific therapeutics. Australian Journal of Chemistry, 67(12), 1763-1779. doi:10.1071/CH14362

Scopus Eid


  • 2-s2.0-84915822447

Start Page


  • 1763

End Page


  • 1779

Volume


  • 67

Issue


  • 12

Abstract


  • Galectins are a family of galactoside-specific lectins that are involved in a myriad of metabolic and disease processes. Due to roles in cancer and inflammatory and heart diseases, galectins are attractive targets for drug development. Over the last two decades, various strategies have been used to inhibit galectins, including polysaccharide-based therapeutics, multivalent display of saccharides, peptides, peptidomimetics, and saccharide-modifications. Primarily due to galectin carbohydrate binding sites having high sequence identities, the design and development of selective inhibitors targeting particular galectins, thereby addressing specific disease states, is challenging. Furthermore, the use of different inhibition assays by research groups has hindered systematic assessment of the relative selectivity and affinity of inhibitors. This review summarises the status of current inhibitors, strategies, and novel scaffolds that exploit subtle differences in galectin structures that, in conjunction with increasing available data on multiple galectins, is enabling the feasible design of effective and specific inhibitors of galectins.

Publication Date


  • 2014

Citation


  • Blanchard, H., Bum-Erdene, K., & Hugo, M. W. (2014). Inhibitors of galectins and implications for structure-based design of galectin-specific therapeutics. Australian Journal of Chemistry, 67(12), 1763-1779. doi:10.1071/CH14362

Scopus Eid


  • 2-s2.0-84915822447

Start Page


  • 1763

End Page


  • 1779

Volume


  • 67

Issue


  • 12