Ammazzalorso Alessandra, De Lellis Laura, Florio Rosalba, Bruno Isabella, De Filippis Barbara, Fantacuzzi Marialuigia, Giampietro Letizia, Maccallini Cristina, Perconti Silvia, Verginelli Fabio, Cama Alessandro, Amoroso Rosa
Unità di Chimica Farmaceutica, Dipartimento di Farmacia, Università "G. d'Annunzio", Chieti, Italy.
Unità di Patologia Generale, Dipartimento di Farmacia, Università "G. d'Annunzio", Chieti, Italy.
Chem Biol Drug Des. 2017 Nov;90(5):1029-1035. doi: 10.1111/cbdd.13026. Epub 2017 Jul 19.
Recent studies report an interesting role of peroxisome proliferator-activated receptor (PPAR) antagonists in different tumor models, being these compounds able to perturb metabolism and viability in cancer cells. In this work, the identification of a novel PPAR antagonist, showing inhibitory activity on PPARα and a weaker antagonism on PPARγ, is described. The activity of this compound and of a series of chemical analogues was investigated in selected tumor cell lines, expressing both PPARα and PPARγ. Data obtained show a dose-dependent cytotoxic effect of the novel PPAR antagonist in colorectal and pancreatic cancer models.
近期研究报道了过氧化物酶体增殖物激活受体(PPAR)拮抗剂在不同肿瘤模型中的有趣作用,这些化合物能够扰乱癌细胞的代谢和活力。在本研究中,描述了一种新型PPAR拮抗剂的鉴定,该拮抗剂对PPARα具有抑制活性,对PPARγ的拮抗作用较弱。在同时表达PPARα和PPARγ的选定肿瘤细胞系中研究了该化合物及一系列化学类似物的活性。所获得的数据表明,新型PPAR拮抗剂在结直肠癌和胰腺癌模型中具有剂量依赖性细胞毒性作用。