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Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kunicki JB,Petersen MN,Alexander LD,Ardi VC,McConnell JR,McAlpine SR

doi

10.1016/j.bmcl.2011.06.083

subject

Has Abstract

pub_date

2011-08-15 00:00:00

pages

4716-9

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00866-3

journal_volume

21

pub_type

杂志文章

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