Evidence map›Paper›PMID 39011823›Full record

ReviewJournal of medicinal chemistry2024

ERAP Inhibitors in Autoimmunity and Immuno-Oncology: Medicinal Chemistry Insights.

Vasileios Fougiaxis, Ben He, Tuhina Khan, Rodolphe Vatinel, Nikoletta M Koutroumpa, Antreas Afantitis, Laetitia Lesire, Pierre Sierocki, Benoit Deprez, Rebecca Deprez-Poulain

Abstract readReview
In one paragraph

Review in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing 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

6 citing papers in PubMed.

  1. Review
  2. Exploring the Involvement ofLife (Basel, Switzerland) · 2026
    Review
  3. Article
  4. Discovery of New Nanomolar Selective IRAP Inhibitors.Journal of medicinal chemistry · 2025
    Article
  5. Review
  6. 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

10 authors.

Vasileios FougiaxisU1177 - Drugs and Molecules for Living Systems, Univ. Lille, Inserm, Institut Pasteur de Lille, F-59000 Lille, France.ORCID 0009-0002-4917-9163
Ben HeU1177 - Drugs and Molecules for Living Systems, Univ. Lille, Inserm, Institut Pasteur de Lille, F-59000 Lille, France.
Tuhina KhanU1177 - Drugs and Molecules for Living Systems, Univ. Lille, Inserm, Institut Pasteur de Lille, F-59000 Lille, France.ORCID 0000-0002-4260-4852
Rodolphe VatinelU1177 - Drugs and Molecules for Living Systems, Univ. Lille, Inserm, Institut Pasteur de Lille, F-59000 Lille, France.
Nikoletta M KoutroumpaNovamechanics Ltd., Nicosia 1516, Cyprus.
Antreas AfantitisNovamechanics Ltd., Nicosia 1516, Cyprus.ORCID 0000-0002-0977-8180
Laetitia LesireU1177 - Drugs and Molecules for Living Systems, Univ. Lille, Inserm, Institut Pasteur de Lille, F-59000 Lille, France.
Pierre SierockiU1177 - Drugs and Molecules for Living Systems, Univ. Lille, Inserm, Institut Pasteur de Lille, F-59000 Lille, France.
Benoit DeprezU1177 - Drugs and Molecules for Living Systems, Univ. Lille, Inserm, Institut Pasteur de Lille, F-59000 Lille, France.ORCID 0000-0002-2777-4538
Rebecca Deprez-PoulainU1177 - Drugs and Molecules for Living Systems, Univ. Lille, Inserm, Institut Pasteur de Lille, F-59000 Lille, France.ORCID 0000-0002-3318-5297

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Endoplasmic reticulum aminopeptidases ERAP1 and 2 are intracellular aminopeptidases that trim antigenic precursors and generate antigens presented by major histocompatibility complex class I (MHC-I) molecules. They thus modulate the antigenic repertoire and drive the adaptive immune response. ERAPs are considered as emerging targets for precision immuno-oncology or for the treatment of autoimmune diseases, in particular MHC-I-opathies. This perspective covers the structural and biological characterization of ERAP, their relevance to these diseases and the ongoing research on small-molecule inhibitors. We describe the chemical and pharmacological space explored by medicinal chemists to exploit the potential of these targets given their localization, biological functions, and family depth. Specific emphasis is put on the binding mode, potency, selectivity, and physchem properties of inhibitors featuring diverse scaffolds. The discussion provides valuable insights for the future development of ERAP inhibitors and analysis of persisting challenges for the translation for clinical applications.

Indexed as

AminopeptidasesMinor Histocompatibility AntigensAnimalsAutoimmune DiseasesAutoimmunityChemistry, PharmaceuticalHistocompatibility Antigens Class IHumansProtease InhibitorsAminopeptidasesERAP1 protein, humanERAP2 protein, humanHistocompatibility Antigens Class IMinor Histocompatibility AntigensProtease Inhibitors

Identifiers

PMID39011823
PMCPMC11284793

What OpenQuestion holds

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LicenceCC BY-NC-ND
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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.