Evidence map›Paper›PMID 32657203›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2020

Synthesis and structure-activity relationships of cerebroside analogues as substrates of cerebroside sulphotransferase and discovery of a competitive inhibitor.

Wenjin Li, Joren Guillaume, Younis Baqi, Isabell Wachsmann, Volkmar Gieselmann, Serge Van Calenbergh, Christa E Müller

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2020. 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
0.4field-weighted citation impact, top 44% 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, 8 citations in OpenAlex.

  1. Article
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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

7 authors at 2 institutions in 2 countries.

Wenjin LiDepartment of Pharmaceutical & Medicinal Chemistry, PharmaCenter Bonn, Pharmaceutical Institute, University of Bonn, Bonn, Germany.
Joren GuillaumeLaboratory for Medicinal Chemistry, Gent, Belgium.
Younis BaqiDepartment of Chemistry, College of Science, Sultan Qaboos University, Muscat, Oman.ORCID https://orcid.org/0000-0002-9659-8419
Isabell WachsmannInstitut für Biochemie und Molekularbiologie, University of Bonn, Bonn, Germany.
Volkmar GieselmannInstitut für Biochemie und Molekularbiologie, University of Bonn, Bonn, Germany.
Serge Van CalenberghLaboratory for Medicinal Chemistry, Gent, Belgium.ORCID https://orcid.org/0000-0002-4201-1264
Christa E MüllerDepartment of Pharmaceutical & Medicinal Chemistry, PharmaCenter Bonn, Pharmaceutical Institute, University of Bonn, Bonn, Germany.ORCID https://orcid.org/0000-0002-0013-6624
University of Bonn · DESultan Qaboos University · OM

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Metachromatic leukodystrophy (MLD) is a rare genetic disease characterised by a dysfunction of the enzyme arylsulphatase A leading to the lysosomal accumulation of cerebroside sulphate (sulphatide) causing subsequent demyelination in patients. The enzyme galactosylceramide (cerebroside) sulphotransferase (CST) catalyses the transfer of a sulphate group from 3'-phosphoadenosine-5'-phosphosulphate (PAPS) to cerebrosides producing sulphatides. Substrate reduction therapy for arylsulphatase A by inhibition of CST was proposed as a promising therapeutic approach. To identify competitive CST inhibitors, we synthesised and investigated analogues of the substrate galactosylceramide with variations at the anomeric position, the acyl substituent and the carbohydrate moiety, and investigated their structure-activity relationships. While most of the compounds behaved as substrates, α-galactosylceramide

Indexed as

Drug DiscoveryCerebrosidesDose-Response Relationship, DrugHumansLeukodystrophy, MetachromaticMolecular StructureStructure-Activity RelationshipSubstrate SpecificitySulfotransferasesCerebrosidesgalactosylceramide sulfotransferaseSulfotransferasesCapillary electrophoresis (CE)competitative inhibitorenzyme assaygalactosyl ceramide analoguesgalactosylceramide sulphotransferase (CST)metachromatic leukodystrophy (MLD)

Identifiers

PMID32657203
PMCPMC7470129
OpenAlexW3042526892

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.