scholarly journals Selective binding modes and allosteric inhibitory effects of lupane triterpenes on protein tyrosine phosphatase 1B

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Tiantian Jin ◽  
Haibo Yu ◽  
Xu-Feng Huang
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
Binding Modes ◽  
Inhibitory Effects ◽  
Selective Binding ◽  
Protein Tyrosine ◽  
Lupane Triterpenes

Pterocarpans with inhibitory effects on protein tyrosine phosphatase 1B from Erythrina lysistemon Hutch.

2009 ◽  
Vol 70 (17-18) ◽  
pp. 2053-2057 ◽  
Author(s):  
Trong Tuan Dao ◽  
Phi Hung Nguyen ◽  
Phuong Thien Thuong ◽  
Keon Wook Kang ◽  
MinKyun Na ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
Inhibitory Effects ◽  
Protein Tyrosine

scholarly journals Computational Insight into Protein Tyrosine Phosphatase 1B Inhibition: A Case Study of the Combined Ligand- and Structure-Based Approach

2017 ◽  
Vol 2017 ◽  
pp. 1-13 ◽  
Author(s):  
Xiangyu Zhang ◽  
Hailun Jiang ◽  
Wei Li ◽  
Jian Wang ◽  
Maosheng Cheng
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Active Sites ◽  
Tyrosine Phosphatase ◽  
Pharmacophore Model ◽  
Protein Tyrosine Phosphatase 1B ◽  
Binding Modes ◽  
Protein Tyrosine ◽  
R Region ◽  
Ptp1b Inhibitors ◽  
Autodock 4.0

Protein tyrosine phosphatase 1B (PTP1B) is an attractive target for treating cancer, obesity, and type 2 diabetes. In our work, the way of combined ligand- and structure-based approach was applied to analyze the characteristics of PTP1B enzyme and its interaction with competitive inhibitors. Firstly, the pharmacophore model of PTP1B inhibitors was built based on the common feature of sixteen compounds. It was found that the pharmacophore model consisted of five chemical features: one aromatic ring (R) region, two hydrophobic (H) groups, and two hydrogen bond acceptors (A). To further elucidate the binding modes of these inhibitors with PTP1B active sites, four docking programs (AutoDock 4.0, AutoDock Vina 1.0, standard precision (SP) Glide 9.7, and extra precision (XP) Glide 9.7) were used. The characteristics of the active sites were then described by the conformations of the docking results. In conclusion, a combination of various pharmacophore features and the integration information of structure activity relationship (SAR) can be used to design novel potent PTP1B inhibitors.

New 5-deoxyflavonoids and their inhibitory effects on protein tyrosine phosphatase 1B (PTP1B) activity

2011 ◽  
Vol 19 (11) ◽  
pp. 3378-3383 ◽  
Author(s):  
Phi Hung Nguyen ◽  
Trong Tuan Dao ◽  
Jayeon Kim ◽  
Do Tuan Phong ◽  
Derek Tantoh Ndinteh ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
Inhibitory Effects ◽  
Protein Tyrosine

Triterpenoids from the Leaves ofDiospyros kaki(Persimmon) and Their Inhibitory Effects on Protein Tyrosine Phosphatase 1B

2008 ◽  
Vol 71 (10) ◽  
pp. 1775-1778 ◽  
Author(s):  
Phuong Thien Thuong ◽  
Chul Ho Lee ◽  
Trong Tuan Dao ◽  
Phi Hung Nguyen ◽  
Wan Gi Kim ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
Inhibitory Effects ◽  
Protein Tyrosine

Oleanane hemiacetal glycosides from Gymnema latifolium and their inhibitory effects on protein tyrosine phosphatase 1B

2020 ◽  
Vol 170 ◽  
pp. 112181 ◽  
Author(s):  
Ha Thanh Tung Pham ◽  
Byeol Ryu ◽  
Hyo Moon Cho ◽  
Ba-Wool Lee ◽  
Woo Young Yang ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
Inhibitory Effects ◽  
Protein Tyrosine

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

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