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    Article

    TGR5 agonist inhibits intestinal epithelial cell apoptosis via cAMP/PKA/c-FLIP/JNK signaling pathway and ameliorates dextran sulfate sodium-induced ulcerative colitis

    Excessive apoptosis of intestinal epithelial cell (IEC) is a crucial cause of disrupted epithelium homeostasis, leading to the pathogenesis of ulcerative colitis (UC). The regulation of Takeda G protein-couple...

    Wen-ji Yang, Fang-hui Han, Yi-pei Gu, Hui Qu, Jia Liu in Acta Pharmacologica Sinica (2023)

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    Article

    Coronarin A modulated hepatic glycogen synthesis and gluconeogenesis via inhibiting mTORC1/S6K1 signaling and ameliorated glucose homeostasis of diabetic mice

    Promotion of hepatic glycogen synthesis and inhibition of hepatic glucose production are effective strategies for controlling hyperglycemia in type 2 diabetes mellitus (T2DM), but agents with both properties w...

    Su-ling Huang, Wei **e, Yang-liang Ye, Jia Liu, Hui Qu in Acta Pharmacologica Sinica (2023)

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    Article

    SL010110, a lead compound, inhibits gluconeogenesis via SIRT2-p300-mediated PEPCK1 degradation and improves glucose homeostasis in diabetic mice

    Suppression of excessive hepatic gluconeogenesis is an effective strategy for controlling hyperglycemia in type 2 diabetes (T2D). In the present study, we screened our compounds library to discover the active ...

    Yu-ran Ren, Yang-liang Ye, Ying Feng, Ti-fei Xu, Yu Shen in Acta Pharmacologica Sinica (2021)

  4. Article

    OL3, a novel low-absorbed TGR5 agonist with reduced side effects, lowered blood glucose via dual actions on TGR5 activation and DPP-4 inhibition

    TGR5 agonists stimulate intestinal glucagon-like peptide-1 (GLP-1) release, but systemic exposure causes unwanted side effects, such as gallbladder filling. In the present study, linagliptin, a DPP-4 inhibitor...

    Shan-yao Ma, Meng-meng Ning, Qing-an Zou, Ying Feng in Acta Pharmacologica Sinica (2016)

  5. Article

    Identification of DW532 as a novel anti-tumor agent targeting both kinases and tubulin

    7,8-Dihydroxy-4-(3-hydroxy-4-methoxyphenyl)-2H-chromen-2-one (DW532) is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities....

    Ting Peng, Jian-rui Wu, Lin-jiang Tong, Meng-yuan Li in Acta Pharmacologica Sinica (2014)

  6. Article

    Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11β-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro

    To design and synthese a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors, featuring the (phenylsulfonamido-methyl)pyridine and (phenylsulfonamido-methyl)thiazole framework.

    Xu Zhang, Yang Zhou, Yu Shen, Li-li Du, Jun-hua Chen in Acta Pharmacologica Sinica (2009)