Acta NaturaeActa NaturaeActa Naturae2075-8251Acta Naturae Ltd1067610.32607/20758251-2011-3-3-47-51ArticlesСтатьиResearch ArticleTranscription Factor DLX5 As a New Target for Promising Antitumor AgentsTranscription Factor DLX5 As a New Target for Promising Antitumor AgentsTimakhovR Atimakhov@gmail.comFedichevP OVinnikA ATestaJ RFavorovaO OQuantum PharmaceuticalsPirogov Russian National Research Medical UniversityFox Chase Cancer CentreFox Chase Cancer CentrePirogov Russian National Research Medical University1509201133VOL 3, NO3 (2011)ТОМ 3, №3 (2011)475117012020Copyright ©; 2011, Timakhov R.A., Fedichev P.O., Vinnik A.A., Testa J.R., Favorova O.O.Copyright ©; 2011, Timakhov R.A., Fedichev P.O., Vinnik A.A., Testa J.R., Favorova O.O.2011Timakhov R.A., Fedichev P.O., Vinnik A.A., Testa J.R., Favorova O.O.Timakhov R.A., Fedichev P.O., Vinnik A.A., Testa J.R., Favorova O.O.https://creativecommons.org/licenses/by/4.0https://actanaturae.ru/2075-8251/article/view/10676

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.

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