A genetically selected cyclic peptide inhibitor of BCL6 homodimerization

A genetically selected cyclic peptide inhibitor of BCL6 homodimerization Bioorganic & Medicinal Chemistry 26 (2018) 3034–3038 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc a a a b Eliot L. Osher , Francisco Castillo , Nagarajan Elumalai , Michael J. Waring , c a, Garry Pairaudeau , Ali Tavassoli Chemistry, University of Southampton, Southampton SO17 1BJ, UK Northern Institute for Cancer Research, Chemistry, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, UK AstraZeneca, Cambridge Science Park, 310 Milton Rd. Cambridge CB40FZ, UK ar ti c l e i nf o ab stra ct Article history: We report an inhibitor of the homodimeric protein-protein interaction of the BCL6 oncoprotein, identi- Received 12 February 2018 fied from a genetically encoded SICLOPPS library of 3.2 million cyclic hexapeptides in combination with Revised 3 March 2018 a bacterial reverse two-hybrid system. This cyclic peptide is shown to bind the BTB domain of BCL6, dis- Accepted 7 March 2018 rupts its homodimerization, and subsequent binding of the SMRT2 corepressor peptide. Available online 9 March 2018 2018 Elsevier Ltd. All rights reserved. 1. Introduction extensively explored and a number of inhibitors of this protein- 13–17 protein interaction (PPI) have been reported. There are cur- 1,2 The B-cell lymphoma 6 http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Bioorganic & Medicinal Chemistry Elsevier

A genetically selected cyclic peptide inhibitor of BCL6 homodimerization

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Publisher
Elsevier
Copyright
Copyright © 2018 Elsevier Ltd
ISSN
0968-0896
D.O.I.
10.1016/j.bmc.2018.03.012
Publisher site
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Abstract

Bioorganic & Medicinal Chemistry 26 (2018) 3034–3038 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc a a a b Eliot L. Osher , Francisco Castillo , Nagarajan Elumalai , Michael J. Waring , c a, Garry Pairaudeau , Ali Tavassoli Chemistry, University of Southampton, Southampton SO17 1BJ, UK Northern Institute for Cancer Research, Chemistry, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, UK AstraZeneca, Cambridge Science Park, 310 Milton Rd. Cambridge CB40FZ, UK ar ti c l e i nf o ab stra ct Article history: We report an inhibitor of the homodimeric protein-protein interaction of the BCL6 oncoprotein, identi- Received 12 February 2018 fied from a genetically encoded SICLOPPS library of 3.2 million cyclic hexapeptides in combination with Revised 3 March 2018 a bacterial reverse two-hybrid system. This cyclic peptide is shown to bind the BTB domain of BCL6, dis- Accepted 7 March 2018 rupts its homodimerization, and subsequent binding of the SMRT2 corepressor peptide. Available online 9 March 2018 2018 Elsevier Ltd. All rights reserved. 1. Introduction extensively explored and a number of inhibitors of this protein- 13–17 protein interaction (PPI) have been reported. There are cur- 1,2 The B-cell lymphoma 6

Journal

Bioorganic & Medicinal ChemistryElsevier

Published: Jul 15, 2018

References

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