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Volume 2, Issue 3(Suppl) Oncol Cancer Case Rep
ISSN: 2471-8556 an open access journal
Page 27
Notes:
Cancer Therapy & Biomarkers 2016
December 05-07, 2016
conferenceseries.com
CANCER THERAPY,
BIOMARKERS & CLINICAL RESEARCH
15th World Congress on
December 05-07, 2016 Philadelphia, USA
From multi-drug treatment to a single multitarget drug: A new path in the treatment of cancer
José Guadalupe Trujillo Ferrara and Erik Andrade Jorge
Escuela Superior de Medicina, Instituto Politécnico Nacional, México
Drug discovery and development is a resource-intensive endeavor that does not always end in success. One of the particu-
larly illustrative examples of this challenge is the development of drugs for cancer treatment. Cancer is one of the leading
causes of death worldwide and currently used chemotherapy causes several serious side effects. Hence it is advantageous to
combine traditional methodology with new computer-assisted technology to increase the success and lower the investment in-
volved in drug research. The aim of the present work was to develop new compounds with an epigenetic approach for treating
cancer cells. This means generating a compound that could inhibit HDAC and ODC while depleting the high level of thiol-con-
taining compounds existing in cancer cells. Overall, the objective is to have an extended conformation of DNA because this
tends to silence proliferative genes and activate anti-cancer genes. Additionally, the greater oxidative stress has been shown to
lead to death by apoptosis in mitochondrial cells. In silico results allow us to predict that α,β-unsaturated compounds will react
with thiol-containing compounds in a selective way by a Michael type 1,4-addition reaction. Moreover, molecular docking
clearly demonstrates that one moiety of the ligand recognizes the catalytic site of HDAC while the other one recognizes ODC, a
theoretical result that has been corroborated by in vitro studies. Cell viability did not decrease in noncancerous cells (epithelial
cells, HaCaT, THLE-3), it did indeed do so in human cancer cells (HuH7, HepG2, Hela), it was found an inhibition constant of
1.5µM estimated for ODC and HDAC. Finally, the administration of one or more of these compounds in an in vivo model was
able to extend the life of mice in survival experiments, reaching up to double the time found in the control. This is a preliminary
contribution to pave the way for clinical testing of this kind of molecule.
Biography
Pioneering in Mexico in the field of medicinal chemistry, Dr. Trujillo has focused on rational drug design based on the physicochemical properties of ligands and
receptors, by using new technology. His different research lines include cancer, obesity, adrenoceptors, Parkinson’s, diabetes, and many others. Dr. Trujillo has
authored more than 125 publications and has more than 876 citations. He has been the advisor for 72 students to obtain a university degree. He is a member of
the National System of Researchers, level III, and is currently in charge of the Ministry of Research and Graduate Studies of the Instituto Politecnico Nacional.
José Guadalupe Trujillo Ferrara et al., Oncol Cancer Case Rep 2016,2:3(Suppl)