Evidence map›Paper›PMID 32154052›Full record

ArticleChemistryOpen2020

Synthesis, Evaluation and Proposed Binding Pose of Substituted Spiro-Oxindole Dihydroquinazolinones as IRAP Inhibitors.

Karin Engen, Sudarsana Reddy Vanga, Thomas Lundbäck, Faith Agalo, Vivek Konda, Annika Jenmalm Jensen, Johan Åqvist, Hugo Gutiérrez-de-Terán, Mathias Hallberg, Mats Larhed and 1 more

Open access · goldAbstract read
In one paragraph

Article in ChemistryOpen, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
0.5field-weighted citation impact, top 38% 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

9 citing papers in PubMed, 15 citations in OpenAlex.

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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

11 authors at 2 institutions in 2 countries.

Karin EngenDepartment of Medicinal Chemistry Uppsala University SE-751 23 Uppsala SWEDEN.
Sudarsana Reddy VangaDepartment of Cell and Molecular Biology Uppsala University SE-751 23 Uppsala SWEDEN.
Thomas LundbäckChemical Biology Consortium Sweden, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics Karolinska Institutet SE-171 65 Solna SWEDEN.ORCID 0000-0002-8145-7808
Faith AgaloDepartment of Medicinal Chemistry Uppsala University SE-751 23 Uppsala SWEDEN.
Vivek KondaDepartment of Medicinal Chemistry Uppsala University SE-751 23 Uppsala SWEDEN.
Annika Jenmalm JensenChemical Biology Consortium Sweden, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics Karolinska Institutet SE-171 65 Solna SWEDEN.
Johan ÅqvistDepartment of Cell and Molecular Biology Uppsala University SE-751 23 Uppsala SWEDEN.
Hugo Gutiérrez-de-TeránScience for Life Laboratory, Department of Cell and Molecular Biology Uppsala University SE-751 23 Uppsala SWEDEN.
Mathias HallbergThe Beijer Laboratory, Department of Pharmaceutical Biosciences Uppsala University SE-751 23 Uppsala SWEDEN.
Mats LarhedScience for Life Laboratory, Department of Medicinal Chemistry Uppsala University SE-751 23 Uppsala SWEDEN.ORCID 0000-0001-6258-0635
Ulrika RosenströmDepartment of Medicinal Chemistry Uppsala University SE-751 23 Uppsala SWEDEN.ORCID 0000-0002-0817-8140
Uppsala University · SEScience for Life Laboratory · SE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Insulin-regulated aminopeptidase (IRAP) is a new potential macromolecular target for drugs aimed for treatment of cognitive disorders. Inhibition of IRAP by angiotensin IV (Ang IV) improves the memory and learning in rats. The majority of the known IRAP inhibitors are peptidic in character and suffer from poor pharmacokinetic properties. Herein, we present a series of small non-peptide IRAP inhibitors derived from a spiro-oxindole dihydroquinazolinone screening hit (pIC

Indexed as

AnimalsBinding SitesCystinyl AminopeptidaseDrug Evaluation, PreclinicalHumansModels, MolecularOxindolesProtease InhibitorsProtein BindingProtein ConformationQuinazolinonesRatsReceptors, AngiotensinSolubilityStructure-Activity RelationshipCystinyl Aminopeptidaseleucyl-cystinyl aminopeptidaseOxindolesProtease InhibitorsQuinazolinonesReceptors, Angiotensinenzymesinhibitorsinsulin-regulated aminopeptidasespreclinical profilingspiro compounds

Identifiers

PMID32154052
PMCPMC7050655
OpenAlexW2985409475

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.