4.8 Article

Shading the TRF2 Recruiting Function: A New Horizon in Drug Development

Journal

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 136, Issue 48, Pages 16708-16711

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ja5080773

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Funding

  1. Italian MIUR
  2. Italian Association for Cancer Research (A.I.R.C.) [11567, 11947]
  3. ligue contre le Cancer
  4. Umberto Veronesi Foundaion
  5. A.I.R.C.

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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 TRF2(TRFH) 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.

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