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Two Thiophenes Compounds Are Partial Peroxisome Proliferator-Activated Receptor α/γ Dual Agonists

Overview of attention for article published in Biological and Pharmaceutical Bulletin, January 2011
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Title
Two Thiophenes Compounds Are Partial Peroxisome Proliferator-Activated Receptor α/γ Dual Agonists
Published in
Biological and Pharmaceutical Bulletin, January 2011
DOI 10.1248/bpb.34.1631
Pubmed ID
Authors

Zhihui Zheng, Yi Yang, Huayi Shao, Zongying Liu, Xinhua Lu, Yanni Xu, Xiaobo He, Wei Jiang, Qin Jiang, Baohua Zhao, Hua Zhang, Zhuorong Li, Shuyi Si

Abstract

In our previous study, two synthetic thiophenes such as IMB-05 and IMB-15 were found as peroxisome proliferator-activated receptor gamma (PPARγ) agonists and exhibited beneficial effects on glucose tolerance of diabetic mice in vivo. In the present study, their effect on the transactivity of other nuclear receptors was further investigated. IMB-05 and IMB-15 could not only activated PPARγ but also efficiently activate PPARα in GAL4-hPPARα/γ (ligand binding domain (LBD)) chimeric receptor assay and PPAR response element (PPRE)-luc reporter gene assay with EC(50) values of 1.8-5.2 µM, whereas no activity was observed in other nuclear receptor assays. In addition, the maximal efficacy of IMB-05 and IMB-15 in activating PPARα/γ was approximately 30% of that observed with Wy14643 and rosiglitazone. These data indicate that the two thiophene derivatives are novel class of partial PPARα/γ dual agonists, which may be the mechanism underlying their regulatory effects on glucose homeostasis.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 8 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Japan 1 13%
Unknown 7 88%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 4 50%
Researcher 2 25%
Student > Postgraduate 1 13%
Unknown 1 13%
Readers by discipline Count As %
Medicine and Dentistry 2 25%
Agricultural and Biological Sciences 1 13%
Physics and Astronomy 1 13%
Immunology and Microbiology 1 13%
Chemistry 1 13%
Other 1 13%
Unknown 1 13%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 05 October 2011.
All research outputs
#20,147,309
of 22,653,392 outputs
Outputs from Biological and Pharmaceutical Bulletin
#2,568
of 2,942 outputs
Outputs of similar age
#169,783
of 180,249 outputs
Outputs of similar age from Biological and Pharmaceutical Bulletin
#92
of 96 outputs
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