scholarly journals Gαi2Enhances Insulin Signaling via Suppression of Protein-tyrosine Phosphatase 1B

2001 ◽  
Vol 276 (43) ◽  
pp. 39705-39712 ◽  
Author(s):  
Jiangchuan Tao ◽  
Craig C. Malbon ◽  
Hsien-yu Wang
Biomolecules ◽  
2019 ◽  
Vol 9 (12) ◽  
pp. 859 ◽  
Author(s):  
Phi Hung Nguyen ◽  
Huynh Nhu Tuan ◽  
Duc Thuan Hoang ◽  
Quoc Trung Vu ◽  
Minh Quan Pham ◽  
...  

Seven pimarane diterpenes (1–7) were isolated from Orthosiphon stamineus Benth. by assay-guided isolation. All of the isolates possessed a 2-deoxy-2-((7-nitro-2,1,3-benzoxadiazol-4-yl)amino)-d-glucose uptake effect in 3T3-L1 adipocytes at concentrations of 5 and 10 μM. Most of them showed potent inhibition against protein tyrosine phosphatase 1B with IC50 values ranging from 0.33 to 9.84 μM. In the kinetic study, all inhibition types were exposed for the examined potencies, including mixed-competitive (1), non-competitives (3 and 5), competitive (6), and uncompetitive (7). The results suggested that O. stamineus and its pimarane diterpenes might exert the hypoglycemic effect via the insulin signaling pathway targeting inhibition of protein tyrosine phosphatase 1B (PTP1B) activity.


2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Makoto Ito ◽  
Sumiaki Fukuda ◽  
Shohei Sakata ◽  
Hisayo Morinaga ◽  
Takeshi Ohta

Protein tyrosine phosphatase 1B (PTP1B) is a negative regulator of leptin signaling as well as insulin signaling. JTT-551 is a new PTP1B inhibitor, which is reported to improve glucose metabolism by enhancement of insulin signaling. We have evaluated an antiobesity effect of JTT-551 using diet-induced obesity (DIO) mice. A single administration of JTT-551 was provided to DIO mice with or without leptin, and DIO mice were given food containing JTT-551 for six weeks. A single administration of JTT-551 with leptin treatment enhanced the food inhibition and the signal transducer and activator of transcription 3 (STAT3) phosphorylation in hypothalamus. Moreover, chronic administration of JTT-551 showed an antiobesity effect and an improvement of glucose and lipid metabolism in DIO mice. JTT-551 shows an antiobesity effect possibly by enhancement of leptin signaling and could be useful in the treatment of type 2 diabetes and obesity.


2001 ◽  
Vol 276 (13) ◽  
pp. 10207-10211 ◽  
Author(s):  
Katsuya Egawa ◽  
Hiroshi Maegawa ◽  
Shinya Shimizu ◽  
Katsutaro Morino ◽  
Yoshihiko Nishio ◽  
...  

2014 ◽  
Vol 8 (3) ◽  
pp. 851-855 ◽  
Author(s):  
TAKATOSHI KITAZAWA ◽  
YUSUKE YOSHINO ◽  
SATOSHI SUZUKI ◽  
ICHIRO KOGA ◽  
YASUO OTA

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