| Title : Evaluation of Teneligliptin Effects on Transcriptional Activity of PPARgamma in Cell-Based Assays - Takenaka_2018_J.Nippon.Med.Sch_85_95 |
| Author(s) : Takenaka Y , Inoue I , Nakano T , Ikeda M , Kakinuma Y , Ikegami Y , Shimada A , Noda M |
| Ref : J Nippon Med Sch , 85 :95 , 2018 |
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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 PPARgamma 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 muM teneligliptin significantly transactivated a reporter gene. The presence of the PPARgamma antagonist, GW9662, did not affect the activation of PPRE-reporter expression by teneligliptin. CONCLUSION: We found that teneligliptin could increase PPARgamma activity in cell-based assays irrespective of the PPARgamma ligand-binding domain. |
| PubMedSearch : Takenaka_2018_J.Nippon.Med.Sch_85_95 |
| PubMedID: 29731503 |
Takenaka Y, Inoue I, Nakano T, Ikeda M, Kakinuma Y, Ikegami Y, Shimada A, Noda M (2018)
Evaluation of Teneligliptin Effects on Transcriptional Activity of PPARgamma in Cell-Based Assays
J Nippon Med Sch
85 :95
Takenaka Y, Inoue I, Nakano T, Ikeda M, Kakinuma Y, Ikegami Y, Shimada A, Noda M (2018)
J Nippon Med Sch
85 :95