Recent advances in the development of allosteric protein tyrosine phosphatase inhibitors for drug discovery

2021 ◽  
Author(s):  
Reham M. Elhassan ◽  
Xuben Hou ◽  
Hao Fang
Keyword(s):  
Drug Discovery ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Phosphatase Inhibitors ◽  
Protein Tyrosine ◽  
Recent Advances ◽  
Allosteric Protein

Design and Biological Evaluation of Novel Imidazolyl Flavonoids as Potent and Selective Protein Tyrosine Phosphatase Inhibitors

2020 ◽  
Vol 16 (4) ◽  
pp. 563-574 ◽  
Author(s):  
Rong Y. Han ◽  
Yu Ge ◽  
Ling Zhang ◽  
Qing M. Wang
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatases ◽  
Structural Features ◽  
Biological Evaluation ◽  
Cell Protein ◽  
Phosphatase Inhibitors ◽  
Protein Tyrosine ◽  
Therapeutic Development ◽  
Chemical Studies

Background: Protein tyrosine phosphatases 1B are considered to be a desirable validated target for therapeutic development of type II diabetes and obesity. Methods: A new series of imidazolyl flavonoids as potential protein tyrosine phosphatase inhibitors were synthesized and evaluated. Results: Bioactive results indicated that some synthesized compounds exhibited potent protein phosphatase 1B (PTP1B) inhibitory activities at the micromolar range. Especially, compound 8b showed the best inhibitory activity (IC50=1.0 µM) with 15-fold selectivity for PTP1B over the closely related T-cell protein tyrosine phosphatase (TCPTP). Cell viability assays indicated that 8b is cell permeable with lower cytotoxicity. Molecular modeling and dynamics studies revealed the reason for selectivity of PTP1B over TCPTP. Quantum chemical studies were carried out on these compounds to understand the structural features essential for activity. Conclusion: Compound 8b should be a potential selective PTP1B inhibitor.

Structure-Based Design and Discovery of Protein Tyrosine Phosphatase Inhibitors Incorporating Novel Isothiazolidinone Heterocyclic Phosphotyrosine Mimetics

2005 ◽  
Vol 48 (21) ◽  
pp. 6544-6548 ◽  
Author(s):  
Andrew P. Combs ◽  
Eddy W. Yue ◽  
Michael Bower ◽  
Paul J. Ala ◽  
Brian Wayland ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Phosphatase Inhibitors ◽  
Protein Tyrosine

scholarly journals Development of Molecular Probes for Second-Site Screening and Design of Protein Tyrosine Phosphatase Inhibitors

2007 ◽  
Vol 50 (9) ◽  
pp. 2137-2143 ◽  
Author(s):  
Jesus Vazquez ◽  
Lutz Tautz ◽  
Jennifer J. Ryan ◽  
Kristiina Vuori ◽  
Tomas Mustelin ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Molecular Probes ◽  
Phosphatase Inhibitors ◽  
Protein Tyrosine

scholarly journals Identification of Phomoxanthone A and B as Protein Tyrosine Phosphatase Inhibitors

ACS Omega ◽  
2020 ◽  
Vol 5 (40) ◽  
pp. 25927-25935
Author(s):  
Runlei Yang ◽  
Qian Dong ◽  
Huibin Xu ◽  
XueHui Gao ◽  
Ziyue Zhao ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Phosphatase Inhibitors ◽  
Protein Tyrosine

Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors

2005 ◽  
Vol 15 (18) ◽  
pp. 4037-4042 ◽  
Author(s):  
Kyeong Lee ◽  
Shanthaveerappa K. Boovanahalli ◽  
Ky-Youb Nam ◽  
Sang-Uk Kang ◽  
Mijeoung Lee ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Phosphatase Inhibitors ◽  
Protein Tyrosine
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