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EntreChem's kinase inhibitor shows potential for treatment of head and neck cancer

March 26th, 2012 - Oviedo (Spain)

•  The PI3K/Akt/PTEN molecular pathway is frequently mutated in this type of tumor, where activation of the Akt kinase is a poor prognosis factor, according to researchers at CIEMAT.

EC-70124, a kinase inhibitor under development at EntreChem SL, has shown efficacy in a murine model of Head & Neck cancer that expresses a permanently active form of the Akt1 kinase together with loss of Trp53.

The results of a public-private collaborative research from EntreChem SL (Oviedo) and CIEMAT (Research Center for Energy, Environment and Technology, in Madrid) focused on searching for a new strategy for Head and Neck Squamous Cell Carcinoma, one of the 10 most common cancers worldwide, has been presented in a poster in the Cold Spring Harbor Symposium "PTEN Pathways and Targets" held on March 13th-16th in New York.

The research, directed by Dr. Jesús Paramio, Head of the Molecular Oncology Unit at CIEMAT, makes use of a HNSCC mouse model, myrAkt;Trp53Epi, which expresses a permanently active form of the Akt1 kinase together with loss of Trp53 expression in the basal layer of stratified epithelia. Oral tumors in these animals have a high incidence and they are phenotipycally similar to human HNSCC.

EC-70124 reduces oral keratinocyte cell viability in a dose-dependent manner, and it specifically affects myrAkt;Trp53Epi protumoral cells, both in vitro and in vivo. EC-70124 regulates PI3K/Akt/PTEN pathway in myrAkt;Trp53Epi oral keratinocytes. The molecule EC-70124, a selective kinase inhibitor, reduces myrAkt;Trp53Epi tumor growth in immunodeficient mice administered intraperitoneally at doses well below toxic levels in mice.

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The inhibitor EC-70124, is currently undergoing preclinical development by EntreChem SL (therefore not yet available for human assays). EC-70124 is a hybrid natural product obtained from genetically modified bacteria by combinatorial biosynthesis.

EntreChem SL is a spin off company created from research developed in the University of Oviedo, and its shareholders include, aside from the original co-founders, local industry companies such as Industrial Química del Nalón, Alvargonzález SA and Alimerka. Private financing is complemented by regional, national and european public programs like NEOTEC program (MICINN), Genome Spain Foundation, FICYT, IDEPA, SRP and 7FP from the European Union.

More information:

Dr. Jesús M. Paramio:
+34 914 962 517

Dr. Francisco Morís Varas:
+34 985 259 021

and also:

(basic research, epithelial biomedicine)

EntreChem SL: