Evidence map›Paper›PMID 39916550›Full record

ArticleJournal of medicinal chemistry2025

Discovery of New Nanomolar Selective IRAP Inhibitors.

Ben He, Nour Bou Karroum, Ronan Gealageas, François-Xavier Mauvais, Sandrine Warenghem, Matthieu Roignant, Nicolas Kraupner, Bao Vy Lam, Nathalie Azaroual, Vincent Ultré and 7 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

17 authors.

Ben HeUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.ORCID 0009-0000-8530-8618
Nour Bou KarroumUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.
Ronan GealageasUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.
François-Xavier MauvaisInstitut Necker Enfants Malades, Université Paris Cité, INSERM, CNRS, Paris F-75015, France.
Sandrine WarenghemUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.
Matthieu RoignantUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.
Nicolas KraupnerUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.
Bao Vy LamUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.ORCID 0000-0002-5713-4507
Nathalie AzaroualUniversity Lille, CHU Lille, ULR 7365─GRITA─Groupe de Recherche Sur Les Formes Injectables Et Les Technologies Associées, Lille F-59000, France.
Vincent UltréUniversity Lille, Plateau RMN Pharmacie, UFR3S-Pharmacie, Lille F-59000, France.
Alexandre RechUniversity Lille, Plateau RMN Pharmacie, UFR3S-Pharmacie, Lille F-59000, France.
Laetitia LesireUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.
Cyril CouturierUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.
Florence LerouxUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.
Peter van EndertInstitut Necker Enfants Malades, Université Paris Cité, INSERM, CNRS, Paris F-75015, France.
Benoit DeprezUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.ORCID 0000-0002-2777-4538
Rebecca Deprez-PoulainUniv. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000 Lille, France.ORCID 0000-0002-3318-5297

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Among the M1 family of oxytocinase aminopeptidases, insulin-regulated aminopeptidase IRAP, is an emerging drug target implicated in various biological pathways and particularly in MHC-I antigen presentation through amino-terminal trimming of exogenous cross-presented peptides. A few series of inhibitors inspired either by angiotensin IV, one of IRAP substrates, or by bestatin a pan aminopeptidase inhibitor, have been disclosed. However, the variety and number of chemotypes remains relatively limited. Here we disclose the design and optimization of a series of hydroxamic acids IRAP inhibitors bearing a 5-substituted indole. Docking studies of the best compound

Indexed as

Cystinyl AminopeptidaseAnimalsDrug DiscoveryEnzyme InhibitorsHumansHydroxamic AcidsIndolesModels, MolecularMolecular Docking SimulationStructure-Activity RelationshipCystinyl AminopeptidaseEnzyme InhibitorsHydroxamic AcidsIndolesleucyl-cystinyl aminopeptidase

Identifiers

PMID39916550
PMCPMC11874008

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.