Cytotoxic effect of a family of peroxisome proliferator-activated receptor antagonists in colorectal and pancreatic cancer cell lines

被引：19
作者：
Ammazzalorso, Alessandra [1 ]
De Lellis, Laura [2 ,3 ]
Florio, Rosalba [2 ,3 ]
Bruno, Isabella [1 ]
De Filippis, Barbara [1 ]
Fantacuzzi, Marialuigia [1 ]
Giampietro, Letizia [1 ]
Maccallini, Cristina [1 ]
Perconti, Silvia [3 ]
Verginelli, Fabio [2 ,3 ]
Cama, Alessandro [2 ,3 ]
Amoroso, Rosa [1 ]
机构：
[1] Univ G DAnnunzio, Unita Chim Farmaceut, Dipartimento Farm, Chieti, Italy
[2] Univ G DAnnunzio, Unita Patol Gen, Dipartimento Farm, Chieti, Italy
[3] Univ G DAnnunzio, Aging Res Ctr Ce SI, Chieti, Italy
来源：
CHEMICAL BIOLOGY & DRUG DESIGN | 2017年 / 90卷 / 05期
关键词：
antitumor agents; CPT1A expression; cytotoxicity; PPAR antagonist; sulfonamides; PPAR-GAMMA AGONISTS; ALPHA; DELTA; METABOLISM; MECHANISMS;
D O I：
10.1111/cbdd.13026
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 PPAR and a weaker antagonism on PPAR, is described. The activity of this compound and of a series of chemical analogues was investigated in selected tumor cell lines, expressing both PPAR and PPAR. Data obtained show a dose-dependent cytotoxic effect of the novel PPAR antagonist in colorectal and pancreatic cancer models.
引用
收藏
页码：1029 / 1035
页数：7
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