Computationally Designed Peptide Inhibitors of the Ubiquitin E3 Ligase SCFFbx4. Issue 4 (11th February 2013)

• Record Type: Journal Article
• Authors: Lee, Junglim; Sammond, Deanne W.; Fiorini, Zeno; Saludes, Jonel P.; Resch, Michael G.; Hao, Bing; Wang, Wei; Yin, Hang; Liu, Xuedong
• Is Part Of: Chembiochem. Volume 14:Issue 4(2013)
• Page Start: 445
• Page End: 451
• Publication Date: 2013-02-11
• Subjects: Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1002/cbic.201200777
• Languages: English
• ISSNs: 1439-4227

Abstract

<abstract abstract-type="graphical" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>A structure‐based computational approach</bold> was used to rationally design peptide inhibitors that can target an E3 ligase (SCF^Fbx4)–substrate (TRF1) interface and subsequent ubiquitylation. Characterization of the inhibitors demonstrates that our sequence‐optimization protocol results in an increase in peptide–TRF1 affinity without compromising peptide–protein specificity.<boxed-text content-type="graphic" position="anchor" orientation="portrait"><graphic position="anchor" mimetype="image" xlink:href="ark:/27927/pgg1v4bc03x" orientation="portrait" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /></boxed-text></p> </abstract>