Journal of Nippon Medical School
Online ISSN : 1347-3409
Print ISSN : 1345-4676
ISSN-L : 1345-4676
Original
Evaluation of Teneligliptin Effects on Transcriptional Activity of PPARγ in Cell-Based Assays
Yasuhiro TakenakaIkuo InoueTakanari NakanoMasaaki IkedaYoshihiko KakinumaYuichi IkegamiAkira ShimadaMitsuhiko Noda
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2018 Volume 85 Issue 2 Pages 95-101

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Abstract

Background: The antidiabetic drug teneligliptin is a novel dipeptidyl peptidase-4 (DPP-4) inhibitor with a thiazolidine-specific structure. This study aimed to investigate whether teneligliptin can activate PPARγ directly and/or indirectly in cell-based assays. Methods: Promoter assays using the reporter construct driven under the control of the SV40 promoter and the PPAR response element (PPRE) were performed. Luciferase activity was measured after a 3-day incubation of vector-transduced cells with various concentrations of teneligliptin. Results: Treatment of the cells with 50 μM teneligliptin significantly transactivated a reporter gene. The presence of the PPARγ antagonist, GW9662, did not affect the activation of PPRE-reporter expression by teneligliptin. Conclusion: We found that teneligliptin could increase PPARγ activity in cell-based assays irrespective of the PPARγ ligand-binding domain.

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© 2018 by the Medical Association of Nippon Medical School
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