DRUG REGULATION OF GENE ACTIVITY

Issue: 
9
Year: 
2016

V.I. Kiselev
Dr.Sc. (Med.), Emanuel Institute of Biochemical Physics of the Russian Academy of Sciences (Moscow)
E-mail: vkis10@mail.ru
I.N. Kuznetsov
Ph.D. (Biol.), A.I. Evdokimov Moscow State University of Medicine and Dentistry
E-mail: KuznetsovIN@ilmixgroup.ruV.M. Drukh
Ph.D. (Med.), Peoples' Friendship University of Russia (Moscow)
E-mail: DruhVM@ilmixgroup.ru
E.L. Muyzhnek
Ph.D. (Biol.), ZAO «MiraxBioPharma» (Moscow)
E-mail: MuyzhnekEL@ilmixgroup.ru

Today classic genocentric concept is radically overhauled, and new young scientific discipline of epigenetics, which studies the ability to reverse the direction of the flow of information on the function, under the influence of various external and internal factors, the corresponding gene is considered to be one of the most studied and perspective in biology. Epigenetic modification, also called epimutations, unlike true genetic mutations do not affect the structure of the DNA and are potentially reversible, i.e. can be regulated by factors internal and external environment. Especially actively examines the role of epigenetics in the initiation and progression of cancer, which led to the formation of a separate, independent scientific direction − epigenetics of cancer. The reversibility of abnormal epigenetic modifications makes enzymes that mediate the reversibility very attractive drug target in the development of targeted epigenetic drugs. Key targets are considered to be a DNA methyltransferase and histone deacetylase. In view of the foregoing, we developed drugs Indinol® Forto (active substance indole-3-carbinol) Epigallat® (active substance) and Cezarox® (diindolylmethane active substance in a liquid dosage form that has greater bioavailability). According to clinical trials conducted by us in conjunction with specialists from the leading medical institutions of the Russian Federation, high efficiency of these drugs has been proved as a means of mono- and combination therapy in the treatment of various benign and precancerous diseases of the female reproductive system. Thus, in patients of reproductive age with benign (HPV infection) and pre-cancerous (CIN 1-2) cervical disease after a 6-month course of therapy with Indinol® Forto and Epigallat®, there was normalization of the clinical signs and almost a 100% demethylation of significant gene suppressors of tumor growth. Similar results were obtained in another trial, during which we studied DNA demethylating activity of these two drugs in the treatment of patients with pathological processes of the endometrium.

Keywords: 
Key words: epigenetic; indole-3-carbinol; epigallocatechin-3-gallate; diindolylmethane; pre-cancerous diseases.