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Peptide aptamer identified by molecular docking targeting translationally controlled tumor protein in leukemia cells

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Summary

Bioinformatics screening and molecular docking analyses were utilized to select high affinity peptides targeting translationally controlled tumor protein (TCTP). Selected peptide aptamers were tested towards cancer cell lines with different levels of TCTP expression. One peptide (WGQWPYHC) revealed specific cytotoxicity according to the TCTP expression in tumor cells without affecting normal cells. Western blot analysis showed peptide-induced down-regulation of TCTP as primary target as well as of cell-cycle related downstream proteins (CDK2, CDK6, Cyclin D3) in MOLT-4 leukemia cells. “WGQWPYHC” deserves further analysis for targeted therapy of TCTP-expressing tumor cells.

Molecular docking on TCTP, cytotoxicity toward MOLT-4 leukemia cell line and downregulation of CDK2, CDK6, CyclinD3 and TCTP proteins

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  1. Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, University of Mainz, Staudinger Weg 5, 55128, Mainz, Germany

    Onat Kadioglu & Thomas Efferth

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Correspondence to Thomas Efferth.

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Kadioglu, O., Efferth, T. Peptide aptamer identified by molecular docking targeting translationally controlled tumor protein in leukemia cells. Invest New Drugs 34, 515–521 (2016). https://doi.org/10.1007/s10637-016-0339-6

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