PHOSPHORAMIDATE DERIVATIVES OF 2′,5′-DIDEOXYADENOSINE AS POTENTIAL INHIBITORS OF THE EDHF PHENOMENON

2005 ◽  
Vol 24 (5-7) ◽  
pp. 553-555 ◽  
Author(s):  
F. Gavazza ◽  
F. Daverio ◽  
A. T. Chaytor ◽  
T. M. Griffith ◽  
C. McGuigan
Keyword(s):  
Potential Inhibitors ◽  
Derivatives Of

Phosphonate monoesters on a thiacalix[4]arene framework as potential inhibitors of protein tyrosine phosphatase 1B

2015 ◽  
Vol 13 (33) ◽  
pp. 8803-8806 ◽  
Author(s):  
Viacheslav V. Trush ◽  
Sergiy G. Kharchenko ◽  
Vsevolod Yu. Tanchuk ◽  
Vitaly I. Kalchenko ◽  
Andriy I. Vovk
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Methylphosphonic Acid ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Potential Inhibitors ◽  
Derivatives Of

Monoester derivatives of thiacalix[4]arene tetrakis(methylphosphonic) acid were found to be capable of inhibiting protein tyrosine phosphatase 1B. In addition, these compounds can strongly bind to human serum albumin.

Phosphonate derivatives of tetraazamacrocycles as new inhibitors of protein tyrosine phosphatases

2015 ◽  
Vol 13 (27) ◽  
pp. 7437-7444 ◽  
Author(s):  
Oleksandr L. Kobzar ◽  
Michael V. Shevchuk ◽  
Alesya N. Lyashenko ◽  
Vsevolod Yu. Tanchuk ◽  
Vadim D. Romanenko ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatases ◽  
Tyrosine Phosphatases ◽  
Protein Tyrosine ◽  
Potential Inhibitors ◽  
Derivatives Of

α,α-Difluoro-β-ketophosphonate derivatives of tetraazamacrocycles were synthesized and found to be potential inhibitors of protein tyrosine phosphatases.

Potential inhibitors of nucleotide biosynthesis. 2. Halomethyl ketone derivatives of pyrimidine nucleosides

1984 ◽  
Vol 27 (5) ◽  
pp. 680-684 ◽  
Author(s):  
John A. Montgomery ◽  
H. Jeanette Thomas ◽  
R. Wallace Brockman ◽  
Robert D. Elliott
Keyword(s):  
Nucleotide Biosynthesis ◽  
Pyrimidine Nucleosides ◽  
Potential Inhibitors ◽  
Derivatives Of

scholarly journals Sulfonyl-bridged Calix[4]arene as an Inhibitor of Protein Tyrosine Phosphatases

2017 ◽  
Vol 5 (2) ◽  
pp. 144-151 ◽  
Author(s):  
Vladyslav Buldenko ◽  
Oleksandr Kobzar ◽  
Viacheslav Trush ◽  
Andriy Drapailo ◽  
Vitaly Kalchenko ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatases ◽  
Tyrosine Phosphatases ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Potential Inhibitors ◽  
Derivatives Of ◽  
Active Site Region ◽  
Micromolar Range

Previously, phosphonic acid derivatives of calix[4]arene and thiacalix[4]arene were found to be potential inhibitors of protein tyrosine phosphatase 1B. In the present paper, the inhibitory activity of unsubstituted sulfonyl-bridget calix[4]arene towards some of the therapeutically important protein tyrosine phosphatases has been established. The obtained results showed that the sulfonylcalix[4]arene is able to inhibit protein tyrosine phosphatase MEG2 with IC50 value in the micromolar range. At the same time, the inhibitor demonstrated lower activity in case of other protein tyrosine phosphatases such as PTP1B, MEG1, TC-PTP, SHP2, and PTPβ. The performed molecular docking indicated that the inhibitor binds to the active site region of MEG2 and PTP1B with WPD-loop in the open conformation.

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