Evidence map›Paper›PMID 24403103›Full record

ArticleChemMedChem2014

Covalent inhibition of the lymphoid tyrosine phosphatase.

Vanessa F Ahmed, Nunzio Bottini, Amy M Barrios

Open access · greenAbstract read
In one paragraph

Article in ChemMedChem, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.3field-weighted citation impact, top 41% 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

3 citing papers in PubMed, 6 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
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

3 authors at 2 institutions in 1 country.

Vanessa F AhmedDepartment of Medicinal Chemistry, University of Utah, 30 South 2000 East, Salt Lake City, UT 84112 (USA).
Nunzio Bottini
Amy M Barrios
University of Utah · USLa Jolla Institute for Immunology · US

Funding

Sanford-Burnham Center for Chemical GenomicsU54HG005033 · NHGRI · SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE · PI JACKSON, MICHAEL · 2008 to 2012
$72.5M
Fluorogenic Assays for Cell-based HTS of Tyrosine Phosphatase InhibitorsR01DK080165 · NIDDK · UNIVERSITY OF SOUTHERN CALIFORNIA · PI BOTTINI, NUNZIO · 2008 to 2012
$1.5M
Fluorogenic PTP Assay for Use in HTS of Novel LYP InhibitorsR21NS056945 · NINDS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI BOTTINI, NUNZIO · 2006 to 2008
$244k
NHGRI NIH HHS U54 HG005033NHGRI NIH HHS U54 HG005033-02NIDDK NIH HHS DK080165NIDDK NIH HHS R01 DK080165NINDS NIH HHS NS056945NINDS NIH HHS R21 NS056945
6 · The paper itself

Abstract

Covalent inhibitors of lymphoid tyrosine phosphatase (LYP) were identified from a screen of the NIH Molecular Libraries Small Molecules Repository (MLSMR). Both of the two lead compounds identified have phosphotyrosine-mimetic benzoic acid moieties as well as electrophilic acrylonitrile groups. Inhibition kinetics of both compounds are consistent with covalent modification of the enzyme, with nanomolar KI and reciprocal millisecond kinact values, representing the best efficiency ratios (kinact /KI ) among currently reported covalent LYP inhibitors. Covalent inhibitors can provide longer efficacy and better selectivity than more conventional noncovalent inhibitors, and these lead compounds are an important step toward the development of protein tyrosine phosphatase (PTP)-targeted covalent therapeutic compounds.

Indexed as

Enzyme InhibitorsHumansKineticsProtein Tyrosine Phosphatase, Non-Receptor Type 22Small Molecule LibrariesStructure-Activity RelationshipEnzyme InhibitorsProtein Tyrosine Phosphatase, Non-Receptor Type 22Small Molecule Librariesacrylonitrileselectrophilesirreversible inhibitorsLYPphosphatasesPTP

Identifiers

PMID24403103
PMCPMC4096870
OpenAlexW1993015895

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.