Evidence map›Paper›PMID 29116812›Full record

ArticleJournal of medicinal chemistry2017

X-ray Characterization and Structure-Based Optimization of Striatal-Enriched Protein Tyrosine Phosphatase Inhibitors.

Michael R Witten, Lisa Wissler, Melanie Snow, Stefan Geschwindner, Jon A Read, Nicholas J Brandon, Angus C Nairn, Paul J Lombroso, Helena Käck, Jonathan A Ellman

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
0.9field-weighted citation impact, top 26% of its field
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

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

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

14 citing papers in PubMed, 30 citations in OpenAlex.

  1. Phosphatase Signaling as a Therapeutic Strategy in Schizophrenia.International journal of molecular sciences · 2026
    Review
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  13. Conformational Analysis of Acyclic α-Fluoro Sulfur Motifs.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020
    Article
  14. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 4 institutions in 3 countries.

Michael R WittenDepartment of Chemistry, Yale University , New Haven, Connecticut 06520, United States.
Lisa WisslerDiscovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Gothenburg, Sweden.
Melanie SnowDiscovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Macclesfield SK10 4TG, United Kingdom.
Stefan GeschwindnerDiscovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Gothenburg, Sweden.ORCID 0000-0002-2154-8345
Jon A ReadDiscovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Cambridge CB4 0WG, United Kingdom.
Nicholas J BrandonNeuroscience, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Cambridge, Massachusetts 02139, United States.
Angus C NairnDepartment of Psychiatry, Yale University , New Haven, Connecticut 06520, United States.
Paul J LombrosoDepartment of Psychiatry, Yale University , New Haven, Connecticut 06520, United States.
Helena KäckDiscovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Gothenburg, Sweden.ORCID 0000-0002-5456-3269
Jonathan A EllmanDepartment of Chemistry, Yale University , New Haven, Connecticut 06520, United States.ORCID 0000-0001-9320-5512
Yale University · USAstraZeneca (Sweden) · SEAstraZeneca (United Kingdom) · GBAstraZeneca (United States) · US

Funding

Next-generation C-H functionalization methods for organic synthesis and their applications to biological inquiryR35GM122473 · NIGMS · YALE UNIVERSITY · PI JONATHAN A ELLMAN · 2017 to 2026
$7.6M
Redox-Regulated Inhibitors of the Striatal-Enriched Protein Tyrosine PhosphataseF32GM114880 · NIGMS · YALE UNIVERSITY · PI WITTEN, MICHAEL · 2015 to 2017
$156k
NIGMS NIH HHS F32 GM114880NIGMS NIH HHS R35 GM122473
6 · The paper itself

Abstract

Excessive activity of striatal-enriched protein tyrosine phosphatase (STEP) in the brain has been detected in numerous neuropsychiatric disorders including Alzheimer's disease. Notably, knockdown of STEP in an Alzheimer mouse model effected an increase in the phosphorylation levels of downstream STEP substrates and a significant reversal in the observed cognitive and memory deficits. These data point to the promising potential of STEP as a target for drug discovery in Alzheimer's treatment. We previously reported a substrate-based approach to the development of low molecular weight STEP inhibitors with K

Indexed as

Alzheimer DiseaseAnimalsCatalytic DomainCrystallography, X-RayDrug DiscoveryDrug StabilityDual-Specificity PhosphatasesMicrosomes, LiverOrganophosphonatesProtein Tyrosine Phosphatases, Non-ReceptorRatsSulfonamidesDual-Specificity Phosphatases(fluoro(2'-fluoro-3'-(2,4,5-trichlorobenzyl)-(1,1'-biphenyl)-4-yl)(morpholinosulfonyl)methyl)phosphonic acidOrganophosphonatesProtein Tyrosine Phosphatases, Non-ReceptorSulfonamides

Identifiers

PMID29116812
PMCPMC5758861
OpenAlexW2767592452

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

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.