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Computationally Designed Peptide Inhibitors of the Ubiquitin E3 Ligase SCF Fbx4
Author(s) -
Lee Junglim,
Sammond Deanne W.,
Fiorini Zeno,
Saludes Jonel P.,
Resch Michael G.,
Hao Bing,
Wang Wei,
Yin Hang,
Liu Xuedong
Publication year - 2013
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201200777
Subject(s) - peptide , dna ligase , ubiquitin ligase , computer science , computational biology , ubiquitin , combinatorial chemistry , chemistry , biochemistry , biology , enzyme , gene
A structure‐based computational approach 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.