Transcription Factor DLX5 As a New Target for Promising Antitumor Agents

R A Timakhov; P O Fedichev; A A Vinnik; J R Testa; O O Favorova

Transcription Factor DLX5 As a New Target for Promising Antitumor Agents

Acta Naturae. 2011 Jul;3(3):47-51.

Authors

R A Timakhov¹, P O Fedichev, A A Vinnik, J R Testa, O O Favorova

Affiliation

¹ Quantum Pharmaceuticals, Russia.

PMID: 22649693
PMCID: PMC3347611

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.

Keywords: DLX5; cancer; molecular docking; small molecules; transcription factor.