In vitro and in vivo synergistic antitumor effect of thapsigargin and a penicillin derivative in murine melanoma cells

BELLIZZI YANINA; CORNIER P.G.; DELPICCOLO CM; CAYROL MF; CREMASCHI GA; BOGGIAN D; MATA E.G.; BLANK VC; ROGUIN LP

Mar del Plata

Congreso; LXIV Reunión Anual de la Sociedad Argentina de Investigación Clínica, LI Reunión Anual de la Asociación Argentina de Farmacología Experimental, XXI Reunión Anual de la Sociedad Argentina de Biología, XXXI Reunión Anual de la Sociedad Argentina de Parasit; 2019

SAIC, SAI, SAFE

The triazolyl peptidyl penicillins (TAPs) are novel hybrids compounds having in their structure a penicillanic core linked to a peptide portion via a triazole group. In a previous study, we showed that the derivative containing the dipeptide Leu-Phe (TAP7f) activates an endoplamic reticulum (ER) stress response and induces apoptosis of murine B16-F0 melanoma cells. In this work, we first demonstrated the contribution of ER stress to the antitumor effect of TAP7f. When cell viability was determined after pre-incubating cells with a specific siRNA for CHOP, a protein involved in ER stress signaling, cell growth increased from 25 ± 2% to 40 ± 1% (p