Selective Galectin‐8N Ligands: The Design and Synthesis of Phthalazinone‐d‐Galactals

Ligand selectivity among the highly conserved galectins has been an ever-challenging objective. For galectin-8, a protein ubiquitous in both pathology and tissue distribution, we report phthalazinone–galactals that show excellent selectivity for the galectin-8 N-terminal domain. A dissection of structure-activity relationships of the phthalazinone and an extensive molecular dynamics meta-analysis accompany the discovery of the selective galectin-8N ligands presented here. These selective compounds will facilitate the study of galectin-8 biology and may have pharmaceutical relevance in the wide range of galectin-8 associated pathologies.

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