Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes
| Autor: | Miguel Carda, Santiago Díaz-Oltra, Eva Falomir, J. Alberto Marco, Juan Murga, Concepción Vilanova |
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| Rok vydání: | 2015 |
| Předmět: |
Vascular Endothelial Growth Factor A
Telomerase Antiangiogenesis VEGF receptors Clinical Biochemistry Genes myc Pharmaceutical Science Gene Expression Angiogenesis Inhibitors Biochemistry chemistry.chemical_compound Drug Discovery medicine Colchicine Humans Telomerase reverse transcriptase Pironetin Molecular Biology Gene Hybrid biology Organic Chemistry Cancer medicine.disease Molecular biology Hybrid molecules Vascular endothelial growth factor Enzyme Activation chemistry Pyrones biology.protein Molecular Medicine HT29 Cells |
| Zdroj: | Bioorganicmedicinal chemistry letters. 25(16) |
| ISSN: | 1464-3405 |
| Popis: | A small group of hybrid molecules composed of a colchicine moiety and a pironetin analogue fragment have been investigated for their ability to inhibit the expression of the VEGF, hTERT and c-Myc genes. The VEGF gene is involved in the generation of the vascular endothelial growth factor (VEGF) and thus in the angiogenic process whereas the two latter ones are related to the activation of telomerase. All three genes therefore may be of paramount importance in the cancer generation process. It has been found that colchicine and some of its derivatives display a measurable ability to inhibit the expression of the VEGF and the two other telomerase-related genes. In the case of some of the hybrids, the available data point to the colchicine fragment being responsible for the observed biological activities. It is the first time that the last biological feature has been reported for colchicine or derivatives thereof. We thank the Spanish Government (MINECO, Ministerio de Economía y Competitividad, research grants CTQ2008-02800 and CTQ2011-27560), by the Consellería d’Empresa, Universitat i Ciencia de la Generalitat Valenciana (research grants PROMETEO/2013/027, ACOMP09/113 and ACOMP/2014/272) and by the Universitat Jaume I (research grants P1-1B-2008-14 and PI-1B-2011-37) for financial support. C.V. further thanks the MINECO for a predoctoral fellowship of the FPI program. The authors thank Prof. C. M. Cerda García-Rojas, from the Departamento de Química, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Mexico, for the kind sending of pironetin samples. |
| Databáze: | OpenAIRE |
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