Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1361714 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
Described are the syntheses of three sansalvamide A derivatives that contain biotinylated tags at individual positions around the macrocycle. The tagged derivatives indicated in protein pull-down assays that they bind to Hsp90 at the same binding site (N-Middle domain) as the San A-amide peptide. Further, these compounds inhibit binding between Hsp90 and multiple C-terminal client proteins. This interaction is unique to the San A analogs indicating they can be tuned for selectivity against Hsp90 client/co-chaperone proteins.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Joseph B. Kunicki, Mark N. Petersen, Leslie D. Alexander, Veronica C. Ardi, Jeanette R. McConnell, Shelli R. McAlpine,