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过氧化物酶体增殖物激活受体拮抗剂的抗癌潜力。

The Anticancer Potential of Peroxisome Proliferator-Activated Receptor Antagonists.

机构信息

Department of Pharmacy, University of Chieti, Via dei Vestini 31, 66100, Chieti, Italy.

Unit of General Pathology, CeSI-MeT, University of Chieti, Chieti, Italy.

出版信息

ChemMedChem. 2018 Feb 6;13(3):209-219. doi: 10.1002/cmdc.201700703. Epub 2018 Jan 10.

Abstract

The effects on cancer-cell proliferation and differentiation mediated by peroxisome proliferator-activated receptors (PPARs) have been widely studied, and pleiotropic outcomes in different cancer models and under different experimental conditions have been obtained. Interestingly, few studies report and little preclinical evidence supports the potential antitumor activity of PPAR antagonists. This review focuses on recent findings on the antitumor in vitro and in vivo effects observed for compounds able to inhibit the three PPAR subtypes in different tumor models, providing a rationale for the use of PPAR antagonists in the treatment of tumors expressing the corresponding receptors.

摘要

过氧化物酶体增殖物激活受体 (PPARs) 介导的对癌细胞增殖和分化的影响已得到广泛研究,并在不同的癌症模型和不同的实验条件下获得了多种结果。有趣的是,很少有研究报道,也几乎没有临床前证据支持 PPAR 拮抗剂的潜在抗肿瘤活性。本综述重点介绍了最近在不同肿瘤模型中观察到的能够抑制三种 PPAR 亚型的化合物的抗肿瘤体内外作用的发现,为使用 PPAR 拮抗剂治疗表达相应受体的肿瘤提供了依据。

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