A genetically selected cyclic peptide inhibitor of BCL6 homodimerization. Issue 11 (15th July 2018)

• Record Type: Journal Article
• Authors: Osher, Eliot L.; Castillo, Francisco; Elumalai, Nagarajan; Waring, Michael J.; Pairaudeau, Garry; Tavassoli, Ali
• Is Part Of: Bioorganic & medicinal chemistry. Volume 26:Issue 11(2018)
• Page Start: 3034
• Page End: 3038
• Publication Date: 2018-07-15
• Subjects: Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2018.03.012
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: 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 hexapeptides 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.