Evidence map›Paper›PMID 38879664›Full record

ArticlePurinergic signalling2025

Exploring novel dilazep derivatives as hENT1 inhibitors and potentially covalent molecular tools.

Majlen A Dilweg, Marina Gorostiola González, Martijn D de Ruiter, Nadine J Meijboom, Jacobus P D van Veldhoven, Rongfang Liu, Willem Jespers, Gerard J P van Westen, Laura H Heitman, Adriaan P IJzerman and 1 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Purinergic signalling, 2025. 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
–field-weighted citation impact
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.

  1. Article
  2. Review
  3. 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

11 authors.

Majlen A DilwegDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.ORCID http://orcid.org/0000-0002-4455-3737
Marina Gorostiola GonzálezDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.ORCID http://orcid.org/0000-0003-1568-0881
Martijn D de RuiterDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.
Nadine J MeijboomDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.
Jacobus P D van VeldhovenDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.
Rongfang LiuDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.ORCID http://orcid.org/0000-0003-0136-8811
Willem JespersDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.ORCID http://orcid.org/0000-0002-4951-9220
Gerard J P van WestenDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.ORCID http://orcid.org/0000-0003-0717-1817
Laura H HeitmanDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.ORCID http://orcid.org/0000-0002-1381-8464
Adriaan P IJzermanDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands.ORCID http://orcid.org/0000-0002-1182-2259
Daan van der EsDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, PO Box 9502, Leiden, The Netherlands. d.van.der.es@lacdr.leidenuniv.nl.ORCID http://orcid.org/0000-0003-3662-8177

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The human equilibrative nucleoside transporter 1 (SLC29A1, hENT1) is a solute carrier that modulates the passive transport of nucleosides and nucleobases, such as adenosine. This nucleoside regulates various physiological processes, such as vasodilation and -constriction, neurotransmission and immune defense. Marketed drugs such as dilazep and dipyridamole have proven useful in cardiovascular afflictions, but the application of hENT1 inhibitors can be beneficial in a number of other diseases. In this study, 39 derivatives of dilazep's close analogue ST7092 were designed, synthesized and subsequently assessed using [

Indexed as

DilazepEquilibrative Nucleoside Transporter 1HumansMolecular Docking SimulationDilazepEquilibrative Nucleoside Transporter 1SLC29A1 protein, humanCovalent inhibitorDilazepHuman equilibrative nucleoside transporter 1Solute carrierStructure–activity relationship

Identifiers

PMID38879664
PMCPMC12061832

What Socratic 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 Socratic graph.