A Genetically Selected Cyclic Peptide Inhibitor of BCL6 Homodimerization

Publication date: Available online 9 March 2018
Source:Bioorganic & Medicinal Chemistry
Author(s): Eliot L. Osher, Francisco Castillo, Nagarajan Elumalai, Michael J. Waring, Garry Pairaudeau, Ali Tavassoli
We report an inhibitor of the homodimeric protein-protein interaction of the BCL6 oncoprotein, identified from a genetically encoded SICLOPPS library of 3.2 million cyclic hexpeptides in combination with a bacterial reverse two-hybrid system. This cyclic peptide is shown to bind the BTB domain of BCL6, disrupts its homodimerization, and subsequent binding of the SMRT2 corepressor peptide.

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