Evidence map›Paper›PMID 29428527›Full record

ArticleBioorganic & medicinal chemistry2018

Discovery of chromenes as inhibitors of macrophage migration inhibitory factor.

Tjie Kok, Hannah Wapenaar, Kan Wang, Constantinos G Neochoritis, Tryfon Zarganes-Tzitzikas, Giordano Proietti, Nikolaos Eleftheriadis, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Robbert H Cool and 3 more

Open access · bronzeAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2018. 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
0.2field-weighted citation impact, top 44% 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

6 citing papers in PubMed, 18 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

13 authors at 3 institutions in 3 countries.

Tjie KokDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Groningen, The Netherlands; Faculty of Biotechnology, University of Surabaya, Jalan Raya Kalirungkut, Surabaya 60292, Indonesia.
Hannah WapenaarDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Groningen, The Netherlands.
Kan WangDepartment of Drug Design, University of Groningen, Groningen, The Netherlands.
Constantinos G NeochoritisDepartment of Drug Design, University of Groningen, Groningen, The Netherlands.
Tryfon Zarganes-TzitzikasDepartment of Drug Design, University of Groningen, Groningen, The Netherlands.
Giordano ProiettiDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Groningen, The Netherlands.
Nikolaos EleftheriadisDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Groningen, The Netherlands; Molecular Microscopy Research Group, Zernike Institute for Advanced Materials, University of Groningen, Groningen, The Netherlands.
Katarzyna KurpiewskaFaculty of Chemistry, Jagiellonian University, 3 Ingardena Street, 30-060 Kraków, Poland.
Justyna Kalinowska-TłuścikFaculty of Chemistry, Jagiellonian University, 3 Ingardena Street, 30-060 Kraków, Poland.
Robbert H CoolDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Groningen, The Netherlands.
Gerrit J PoelarendsDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Groningen, The Netherlands.
Alexander DömlingDepartment of Drug Design, University of Groningen, Groningen, The Netherlands.
Frank J DekkerDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Groningen, The Netherlands. Electronic address: f.j.dekker@rug.nl.
University of Groningen · NLJagiellonian University · PLUniversity of Surabaya · ID

Funding

Real-time discovery of inhibitors among billion compounds for preview and downloadR01GM097082 · NIGMS · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI CAMACHO, CARLOS J. · 2011 to 2020
$2.5M
European Research Council 309782NIGMS NIH HHS R01 GM097082
6 · The paper itself

Abstract

Macrophage migration inhibitory factor (MIF) is an essential signaling cytokine with a key role in the immune system. Binding of MIF to its molecular targets such as, among others, the cluster of differentiation 74 (CD74) receptor plays a key role in inflammatory diseases and cancer. Therefore, the identification of MIF binding compounds gained importance in drug discovery. In this study, we aimed to discover novel MIF binding compounds by screening of a focused compound collection for inhibition of its tautomerase enzyme activity. Inspired by the known chromen-4-one inhibitor Orita-13, a focused collection of compounds with a chromene scaffold was screened for MIF binding. The library was synthesized using versatile cyanoacetamide chemistry to provide diversely substituted chromenes. The screening provided inhibitors with IC

Indexed as

BenzopyransBinding SitesCrystallography, X-RayHumansInhibitory Concentration 50Intramolecular OxidoreductasesKineticsMacrophage Migration-Inhibitory FactorsMolecular ConformationMolecular Dynamics SimulationProtein BindingStructure-Activity RelationshipBenzopyransIntramolecular OxidoreductasesMacrophage Migration-Inhibitory FactorsMIF protein, humanChromenesEnzyme kineticsInhibitorMacrophage migration inhibitory factor

Identifiers

PMID29428527
PMCPMC6323139
OpenAlexW2777392268

What OpenQuestion holds

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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.