Evidence map›Paper›PMID 34905258›Full record

ArticleChembiochem : a European journal of chemical biology2022

Asymmetrically Substituted m-Terphenyl Phosphates Inhibit the Transcription Factor STAT5a.

Daniel Müller-Klieser, Thorsten Berg

Open access · hybridAbstract read
In one paragraph

Article in Chembiochem : a European journal of chemical biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.3field-weighted citation impact, top 40% 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

5 citing papers in PubMed, 6 citations in OpenAlex.

  1. Article
  2. Article
  3. Stafiba: A STAT5-Selective Small-Molecule Inhibitor.Chembiochem : a European journal of chemical biology · 2023
    Article
  4. Article
  5. Asymmetrically Substituted m-Terphenyl Phosphates Inhibit the Transcription Factor STAT5a.Chembiochem : a European journal of chemical biology · 2022
    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

2 authors at 1 institution in 1 country.

Daniel Müller-KlieserInstitute of Organic Chemistry, Leipzig University, Johannisallee 29, 04103, Leipzig, Germany.
Thorsten BergInstitute of Organic Chemistry, Leipzig University, Johannisallee 29, 04103, Leipzig, Germany.ORCID 0000-0003-3109-7696
Leipzig University · DE

Funding

Deutsche Forschungsgemeinschaft BE 4572/4-2
6 · The paper itself

Abstract

We recently presented Stafia-1 as the first chemical entity that inhibits the transcription factor STAT5a with selectivity over the highly homologous STAT5b. Stafia-1, which was identified from a series of symmetrically substituted m-terphenyl phosphates, binds to the interface between the SH2 domain and the linker domain of STAT5a. Here, we outline a synthetic strategy for the synthesis of asymmetrically substituted m-terphenyl phosphates, which can be tailored to address their asymmetric STAT5a binding site in a more specific manner. The asymmetrically substituted m-terphenyl phosphate with the highest activity against STAT5a was converted to a phosphatase-stable monofluoromethylene phosphonate. The synthetic methodology and activity analysis described here provide first insights into the structure-activity relationships of m-terphenyl phosphates for use as selective STAT5a inhibitors.

Indexed as

Dose-Response Relationship, DrugHumansModels, MolecularMolecular StructureOrganophosphorus CompoundsSTAT5 Transcription FactorStructure-Activity RelationshipTumor Suppressor ProteinsOrganophosphorus CompoundsSTAT5A protein, humanSTAT5 Transcription FactorTumor Suppressor Proteinscross couplinginhibitorsprotein-protein interactionsSH2 domainstranscription factors

Identifiers

PMID34905258
PMCPMC9303812
OpenAlexW4200549148

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.