Prospects for Inhibitors of Protein Tyrosine Phosphatase 1B as Antidiabetic Drugs

2004 ◽  
Vol 47 (17) ◽  
pp. 4142-4146 ◽  
Author(s):  
Rob Hooft van Huijsduijnen ◽  
Wolfgang H. B. Sauer ◽  
Agnes Bombrun ◽  
Dominique Swinnen
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Antidiabetic Drugs ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine

scholarly journals Natural α-Glucosidase and Protein Tyrosine Phosphatase 1B Inhibitors: A Source of Scaffold Molecules for Synthesis of New Multitarget Antidiabetic Drugs

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4818
Author(s):  
Massimo Genovese ◽  
Ilaria Nesi ◽  
Anna Caselli ◽  
Paolo Paoli
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Antidiabetic Drugs ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Lead Compounds ◽  
Limited Effectiveness ◽  
Biological Target ◽  
Dual Inhibitors

Diabetes mellitus (DM) represents a group of metabolic disorders that leads to acute and long-term serious complications and is considered a worldwide sanitary emergence. Type 2 diabetes (T2D) represents about 90% of all cases of diabetes, and even if several drugs are actually available for its treatment, in the long term, they show limited effectiveness. Most traditional drugs are designed to act on a specific biological target, but the complexity of the current pathologies has demonstrated that molecules hitting more than one target may be safer and more effective. The purpose of this review is to shed light on the natural compounds known as α-glucosidase and Protein Tyrosine Phosphatase 1B (PTP1B) dual-inhibitors that could be used as lead compounds to generate new multitarget antidiabetic drugs for treatment of T2D.

scholarly journals Prospects for Inhibitors of Protein Tyrosine Phosphatase 1B as Antidiabetic Drugs.

ChemInform ◽  
2004 ◽  
Vol 35 (43) ◽  
Author(s):  
Rob Hooft van Huijsduijnen ◽  
Wolfgang H. B. Sauer ◽  
Agnes Bombrun ◽  
Dominique Swinnen
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Antidiabetic Drugs ◽  
Protein Tyrosine Phosphatase 1B ◽  
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.

The Involvement of the Mammalian Target of Rapamycin, Protein Tyrosine Phosphatase 1b and Dipeptidase 4 Signaling Pathways in Cancer and Diabetes: A Narrative Review

2020 ◽  
Vol 20 ◽  
Author(s):  
Jiajia Zhang ◽  
Ning Wu ◽  
Dayong Shi
Keyword(s):  
Signaling Pathways ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Mammalian Target Of Rapamycin ◽  
Eukaryotic Cell ◽  
Target Of Rapamycin ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Transduction Mechanisms ◽  
Specific Proteins

Background: The mammalian target of rapamycin (mTOR), protein tyrosine phosphatase 1b (PTP1B) and dipeptidase 4 (DPP4) signaling pathways regulate eukaryotic cell proliferation and metabolism. Previous researches described different transduction mechanisms in the progression of cancer and diabetes. Methodology: We reviewed recent advances in the signal transduction pathways of mTOR, PTP1B and DPP4 regulation and determined the crosstalk and common pathway in diabetes and cancer. Results: We showed that according to numerous past studies, the proteins participate in the signaling networks for both diseases. Conclusion: There are common pathways and specific proteins involved in diabetes and cancer. This article demonstrates and explains the potential mechanisms of association and future prospects for targeting these proteins in pharmacological studies.

Sign in / Sign up

Export Citation Format

Share Document