A new strategy for the in vitro selection of stapled peptide inhibitors by mRNA display.

Chem Commun (Camb)

Department of Chemistry, Virginia Commonwealth University, 1001 West Main Street, P. O. Box 842006, Richmond, VA 23284, USA. and Massey Cancer Center, Virginia Commonwealth University, 401 College Street, Richmond, VA 23298, USA.

Published: August 2019

AI Article Synopsis

  • Hydrocarbon stapled peptides are potential drugs that can block interactions between proteins inside cells.
  • A new method using mRNA display is created to quickly discover these stapled peptides, utilizing α-methyl cysteine and m-dibromoxylene for cyclization.
  • The research specifically aims to find a peptide that can effectively bind to the HPV16 E2 protein, which is relevant for HPV-related diseases.

Article Abstract

Hydrocarbon stapled peptides are promising therapeutics for inhibition of intracellular protein-protein interactions. Here we develop a new high-throughput strategy for hydrocarbon stapled peptide discovery based on mRNA display of peptides containing α-methyl cysteine and cyclized with m-dibromoxylene. We focus on development of a peptide binder to the HPV16 E2 protein.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7077329PMC
http://dx.doi.org/10.1039/c8cc10192bDOI Listing

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