The Discovery of Novel Protein Tyrosine Phosphatase ε Inhibitors Using a High-throughput Screening Approach

2017 ◽  
Vol 38 (1) ◽  
pp. 44-53 ◽  
Author(s):  
Hye-Yeoung Yun ◽  
Bonsu Ku ◽  
Hye Seon Lee ◽  
Ho-Chul Shin ◽  
Jun-Beom Park ◽  
...  
Keyword(s):  
High Throughput ◽  
Protein Tyrosine Phosphatase ◽  
High Throughput Screening ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine ◽  
Screening Approach ◽  
Novel Protein

Molecular Docking and High-Throughput Screening for Novel Inhibitors of Protein Tyrosine Phosphatase-1B

2002 ◽  
Vol 45 (11) ◽  
pp. 2213-2221 ◽  
Author(s):  
Thompson N. Doman ◽  
Susan L. McGovern ◽  
Bryan J. Witherbee ◽  
Thomas P. Kasten ◽  
Ravi Kurumbail ◽  
...  
Keyword(s):  
Molecular Docking ◽  
High Throughput ◽  
Protein Tyrosine Phosphatase ◽  
High Throughput Screening ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine

scholarly journals Development of a Robust High-Throughput Screening Platform for Inhibitors of the Striatal-Enriched Tyrosine Phosphatase (STEP)

2021 ◽  
Vol 22 (9) ◽  
pp. 4417
Author(s):  
Lester J Lambert ◽  
Stefan Grotegut ◽  
Maria Celeridad ◽  
Palak Gosalia ◽  
Laurent JS De Backer ◽  
...  
Keyword(s):  
Drug Discovery ◽  
High Throughput ◽  
Tyrosine Kinases ◽  
High Throughput Screening ◽  
Kinase Inhibitors ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatases ◽  
Synaptic Function ◽  
Label Free ◽  
Protein Tyrosine

Many human diseases are the result of abnormal expression or activation of protein tyrosine kinases (PTKs) and protein tyrosine phosphatases (PTPs). Not surprisingly, more than 30 tyrosine kinase inhibitors (TKIs) are currently in clinical use and provide unique treatment options for many patients. PTPs on the other hand have long been regarded as “undruggable” and only recently have gained increased attention in drug discovery. Striatal-enriched tyrosine phosphatase (STEP) is a neuron-specific PTP that is overactive in Alzheimer’s disease (AD) and other neurodegenerative and neuropsychiatric disorders, including Parkinson’s disease, schizophrenia, and fragile X syndrome. An emergent model suggests that the increase in STEP activity interferes with synaptic function and contributes to the characteristic cognitive and behavioral deficits present in these diseases. Prior efforts to generate STEP inhibitors with properties that warrant clinical development have largely failed. To identify novel STEP inhibitor scaffolds, we developed a biophysical, label-free high-throughput screening (HTS) platform based on the protein thermal shift (PTS) technology. In contrast to conventional HTS using STEP enzymatic assays, we found the PTS platform highly robust and capable of identifying true hits with confirmed STEP inhibitory activity and selectivity. This new platform promises to greatly advance STEP drug discovery and should be applicable to other PTP targets.

Molecular Cloning, Chromosomal Mapping, and Developmental Expression of a Novel Protein Tyrosine Phosphatase-like Gene

Genomics ◽  
1999 ◽  
Vol 62 (3) ◽  
pp. 406-416 ◽  
Author(s):  
Dafe A. Uwanogho ◽  
Zoë Hardcastle ◽  
Piroska Balogh ◽  
Ghazala Mirza ◽  
Kent L. Thornburg ◽  
...  
Keyword(s):  
Molecular Cloning ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Chromosomal Mapping ◽  
Developmental Expression ◽  
Protein Tyrosine ◽  
Novel Protein

Molecular cloning of a novel protein-tyrosine phosphatase SH-PTP3 with sequence similarity to the src -homology region 2

FEBS Letters ◽  
1992 ◽  
Vol 314 (3) ◽  
pp. 335-339 ◽  
Author(s):  
Masaaki Adachi ◽  
Masuo Sekiya ◽  
Toshiki Miyachi ◽  
Keiki Matsuno ◽  
Yuji Hinoda ◽  
...  
Keyword(s):  
Molecular Cloning ◽  
Protein Tyrosine Phosphatase ◽  
Sequence Similarity ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine ◽  
Homology Region ◽  
Src Homology ◽  
Novel Protein
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