Evidence map›Paper›PMID 30289412›Full record

ArticleActa crystallographica. Section D, Structural biology2018

High-resolution crystal structures of the D1 and D2 domains of protein tyrosine phosphatase epsilon for structure-based drug design.

George T Lountos, Sreejith Raran-Kurussi, Bryan M Zhao, Beverly K Dyas, Terrence R Burke, Robert G Ulrich, David S Waugh

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Acta crystallographica. Section D, Structural biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

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0cells of the map it votes in
2citing papers in PubMed
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1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

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Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

2 citing papers in PubMed.

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4 · The record

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5 · Who and what money

Authors and funding

7 authors.

George T LountosBasic Science Program, Frederick National Laboratory for Cancer Research sponsored by the National Cancer Institute, Frederick, MD 21702, USA.
Sreejith Raran-KurussiMacromolecular Crystallography Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, USA.
Bryan M ZhaoThe Oak Ridge Institute for Science and Education, Oak Ridge, TN 37831, USA.
Beverly K DyasMolecular and Translational Sciences Division, US Army Medical Research Institute of Infectious Diseases, Frederick, MD 21702, USA.
Terrence R BurkeChemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, USA.
Robert G UlrichMolecular and Translational Sciences Division, US Army Medical Research Institute of Infectious Diseases, Frederick, MD 21702, USA.
David S WaughMacromolecular Crystallography Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, USA.

Funding

Inhibitors of Tyrosine Kinase-Dependent Signalling as Anti-Cancer AgentsZIABC006198 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI BURKE, TERRENCE · 2009 to 2025
$13.7M
CCR NIH HHS HHSN261200800001CNCI NIH HHS HHSN261200800001EU.S. Department of Energy, Office of Basic Energy Sciences W-31-109-Eng-38
6 · The paper itself

Abstract

Here, new crystal structures are presented of the isolated membrane-proximal D1 and distal D2 domains of protein tyrosine phosphatase epsilon (PTPℇ), a protein tyrosine phosphatase that has been shown to play a positive role in the survival of human breast cancer cells. A triple mutant of the PTPℇ D2 domain (A455N/V457Y/E597D) was also constructed to reconstitute the residues of the PTPℇ D1 catalytic domain that are important for phosphatase activity, resulting in only a slight increase in the phosphatase activity compared with the native D2 protein. The structures reported here are of sufficient resolution for structure-based drug design, and a microarray-based assay for high-throughput screening to identify small-molecule inhibitors of the PTPℇ D1 domain is also described.

Indexed as

Drug DesignCrystallography, X-RayHumansProtein Array AnalysisProtein DomainsProtein Structure, TertiaryReceptor-Like Protein Tyrosine Phosphatases, Class 4Small Molecule LibrariesReceptor-Like Protein Tyrosine Phosphatases, Class 4Small Molecule Librariesmicroarray assayprotein tyrosine phosphatasePTPreceptor-like protein tyrosine phosphataseRPTPstructure-based drug design

Identifiers

PMID30289412
PMCPMC6173050

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.