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Ineffective current treatments for esophagus squamous cell carcinoma (ESCC) is one of the main reasons for its low 5-year survival (20%). Transforming growth factor beta-1 stimulated clone 22 - isoform 4 (Tsc22D4/THG-1) is overexpressed in 92.6% of ESCC specimens while strictly resided in mitotically active basal layer of normal squamous epithelial tissue. Knockout of THG-1 caused reduction in cancer cells growth, invasion and tumorigenesis. Experimentally, protein-protein interactions (PPIs) were identified as THG-1 mechanism to promote cancer progression. Well-known cellular regulators', Keap1, PHD2, TBLR1 and NRBP1, functional interactions are disrupted in the present of THG-1. To develop THG-1 PPIs antagonist, Random non-standard Peptide Integrated Discovery (RaPID) system was employed. In this system, D-stereochemistry, unusual side chains and N- methylation containing macrocyclic peptides was generated and screened against THG-1. High-specificity, flat-surface binding ability, rigidity make those peptides to be more advantageous for PPIs blocking compare to small molecules and antibodies. Herein, I discuss the process to identify potential lead compounds for ESCC therapeutic by blocking THG-1 PPIs.

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Copyright: The Authors. This is an open access article distributed under the terms of the Creative Commons Attribution License CC-BY 4.0., which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

 How to Cite
Tran, D. (2017). ID2007 In vitro selection of macrocyclic peptides against THG-1 for Esophagus Squamous Cell Carcinomas therapeutic lead compounds. Biomedical Research and Therapy, 4(S), S40.

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