Evidence map›Paper›PMID 31841350›Full record

ArticleJournal of medicinal chemistry2020

Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1.

Zachary Maben, Richa Arya, Digamber Rane, W Frank An, Shailesh Metkar, Marc Hickey, Samantha Bender, Akbar Ali, Tina T Nguyen, Irini Evnouchidou and 4 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.

0numbers the graph read from it
0cells of the map it votes in
26citing papers in PubMed
1.8field-weighted citation impact, top 14% 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

26 citing papers in PubMed, 52 citations in OpenAlex.

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  12. Determination of Ligand-Binding Affinity (Journal of medicinal chemistry · 2023
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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

14 authors at 4 institutions in 2 countries.

Zachary Maben
Richa Arya
Digamber RaneKansas University Specialized Chemistry Center , Lawrence , Kansas 66047 , United States.
W Frank AnBroad Institute of MIT and Harvard , Cambridge , Massachusetts 02142 , United States.
Shailesh MetkarBroad Institute of MIT and Harvard , Cambridge , Massachusetts 02142 , United States.
Marc HickeyBroad Institute of MIT and Harvard , Cambridge , Massachusetts 02142 , United States.
Samantha BenderBroad Institute of MIT and Harvard , Cambridge , Massachusetts 02142 , United States.
Tina T Nguyen
Irini EvnouchidouNational Centre for Scientific Research Demokritos , Agia Paraskevi, Athens 15341 , Greece.
Roger SchillingBroad Institute of MIT and Harvard , Cambridge , Massachusetts 02142 , United States.
Efstratios StratikosNational Centre for Scientific Research Demokritos , Agia Paraskevi, Athens 15341 , Greece.ORCID 0000-0002-3566-2309
Jennifer GoldenKansas University Specialized Chemistry Center , Lawrence , Kansas 66047 , United States.ORCID 0000-0002-6813-3710
University of Massachusetts Chan Medical School · USBroad Institute · USUniversity of Kansas · USNational Centre of Scientific Research "Demokritos" · GR

Funding

ER-aminopeptidases: Conformational regulation and antigen presentation functionR01AI153828 · NIAID · UNIV OF MASSACHUSETTS MED SCH WORCESTER · PI STERN, LAWRENCE J. · 2020 to 2023
$2.0M
Structure and Function of Class II MHC ProteinsR01AI038996 · NIAID · UNIV OF MASSACHUSETTS MED SCH WORCESTER · PI STERN, LAWRENCE J · 1996 to 2006
$1.6M
Small molecule probes of ERAP-1R03MH097543 · NIMH · UNIV OF MASSACHUSETTS MED SCH WORCESTER · PI STERN, LAWRENCE J. · 2012 to 2013
$82k
NIAID NIH HHS R01 AI038996NIAID NIH HHS R01 AI153828NIMH NIH HHS R03 MH097543
6 · The paper itself

Abstract

ERAP1 is an endoplasmic reticulum-resident zinc aminopeptidase that plays an important role in the immune system by trimming peptides for loading onto major histocompatibility complex proteins. Here, we report discovery of the first inhibitors selective for ERAP1 over its paralogues ERAP2 and IRAP. Compound

Indexed as

AminopeptidasesCatalytic DomainDrug DiscoveryHeLa CellsHumansMinor Histocompatibility AntigensMolecular Docking SimulationMolecular StructurePhenylurea CompoundsPolymorphism, Single NucleotideProtease InhibitorsProtein BindingStructure-Activity RelationshipSulfonamidesTryptaminesAminopeptidasesERAP1 protein, humanMinor Histocompatibility AntigensPhenylurea CompoundsProtease InhibitorsSulfonamidesTryptamines

Identifiers

PMID31841350
PMCPMC8218592
OpenAlexW2995298549

What OpenQuestion holds

Textmetadata
LicenceTDM
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.