Shading the TRF2 recruiting function: a new horizon in drug development

J Am Chem Soc. 2014 Dec 3;136(48):16708-11. doi: 10.1021/ja5080773. Epub 2014 Nov 19.

Abstract

The shelterin protein TRF2 has come to the limelight for its role in telomere maintenance and tumorigenesis. Herein, the application of rational design and synthesis allowed identifying the first TRF2TRFH binder able to elicit a marked DNA damage response in cancer cells. This work paves the way for the unprecedented employment of a chemical tool to finely tune specific mechanisms underlying telomere maintenance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Design*
  • Humans
  • Models, Molecular
  • Peptides, Cyclic / chemical synthesis
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / pharmacology*
  • Telomeric Repeat Binding Protein 2 / antagonists & inhibitors*
  • Telomeric Repeat Binding Protein 2 / metabolism

Substances

  • Peptides, Cyclic
  • TERF2 protein, human
  • Telomeric Repeat Binding Protein 2