Transcription Factor DLX5 As a New Target for Promising Antitumor Agents

RA Timakhov, PO Fedichev, AA Vinnik, JR Testa, OO Favorova

Research output: Contribution to journalArticlepeer-review

Abstract

The crystal structure of the human transcription factor DLX5 has been used for the screening of a library consisting of 10(6 )compounds by the molecular docking technique.In vitro testsof the 14 top-rated ligands showed that compound Q12 displays the best ability to inhibit the proliferation ofDlx5 positive mouse lymphoma cells, which correlates with the down-regulation ofc-mycexpression. Compound Q12 has low toxicity on normal human ovarian epithelial cells and mouse lymphoma cells with absent expression ofDlx5, and can be used for further chemical optimization and for the development of novel, highly efficient cancer treatments.

Original languageAmerican English
Pages (from-to)47-51
Number of pages5
JournalActa Naturae
Volume3
Issue number3
DOIs
StatePublished - Jul 2011

Keywords

  • DLX5
  • Cancer
  • Molecular docking
  • Small molecules
  • Transcription factor

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