A spiroligomer α-helix mimic that binds HDM2, penetrates human cells and stabilizes HDM2 in cell culture.

We demonstrate functionalized spiroligomers that mimic the HDM2-bound conformation of the p53 activation domain. Spiroligomers are stereochemically defined, functionalized, spirocyclic monomers coupled through pairs of amide bonds to create spiro-ladder oligomers. Two series of spiroligomers were sy...

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Bibliographic Details
Main Authors: Zachary Z Brown, Kavitha Akula, Alla Arzumanyan, Jennifer Alleva, Marcus Jackson, Eugeney Bichenkov, Joel B Sheffield, Mark A Feitelson, Christian E Schafmeister
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2012-01-01
Series:PLoS ONE
Online Access:http://europepmc.org/articles/PMC3475717?pdf=render