Identification of potent inhibitors of the sortilin-progranulin interaction.
Bioorganic & Medicinal Chemistry Letters(2020)
Abstract
High-throughput screening methods have been used to identify two novel series of inhibitors that disrupt progranulin binding to sortilin. Exploration of structure-activity relationships (SAR) resulted in compounds with sufficient potency and physicochemical properties to enable co-crystallization with sortilin. These co-crystal structures supported observed SAR trends and provided guidance for additional avenues for designing compounds with additional interactions within the binding site.
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Key words
Sortilin,Progranulin,Protein-protein interaction inhibitor,Structure activity relationship
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