Transcription Factor DLX5 As a New Target for Promising Antitumor Agents

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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 tests of the 14 top-rated ligands showed that compound Q12 displays the best ability to inhibit the proliferation of Dlx5 positive mouse lymphoma cells, which correlates with the down-regulation of c-myc expression. Compound Q12 has low toxicity on normal human ovarian epithelial cells and mouse lymphoma cells with absent expression of Dlx5, and can be used for further chemical optimization and for the development of novel, highly efficient cancer treatments.

Transcription Factor DLX5 As a New Target for Promising Antitumor Agents

R A Timakhov

Quantum Pharmaceuticals; Pirogov Russian National Research Medical University; Fox Chase Cancer Centre

Email: timakhov@gmail.com
Russia; Philadelphia, USA

P O Fedichev

Quantum Pharmaceuticals

Russia

A A Vinnik

Quantum Pharmaceuticals

Russia

J R Testa

Fox Chase Cancer Centre

Philadelphia, USA

O O Favorova

Pirogov Russian National Research Medical University

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Copyright (c) 2011 Timakhov R.A., Fedichev P.O., Vinnik A.A., Testa J.R., Favorova O.O.

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