Evidence map›Paper›PMID 32316498›Full record

ArticleInternational journal of molecular sciences2020

Antimigraine Drug Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor That Induces CYP1A1 in Hepatic and Intestinal Cells.

Barbora Vyhlídalová, Kristýna Krasulová, Petra Pečinková, Karolína Poulíková, Radim Vrzal, Zdeněk Andrysík, Aneesh Chandran, Sridhar Mani, Zdenek Dvorak

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.5field-weighted citation impact, top 37% 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

0 citing papers in PubMed, 9 citations in OpenAlex.

No citing paper in PubMed yet.

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

9 authors at 4 institutions in 2 countries.

Barbora VyhlídalováDepartment of Cell Biology and Genetics, Faculty of Science, Palacky University, Slechtitelu 27, 783 71 Olomouc, Czech Republic.
Kristýna KrasulováDepartment of Cell Biology and Genetics, Faculty of Science, Palacky University, Slechtitelu 27, 783 71 Olomouc, Czech Republic.
Petra PečinkováDepartment of Cell Biology and Genetics, Faculty of Science, Palacky University, Slechtitelu 27, 783 71 Olomouc, Czech Republic.
Karolína PoulíkováDepartment of Cell Biology and Genetics, Faculty of Science, Palacky University, Slechtitelu 27, 783 71 Olomouc, Czech Republic.
Radim VrzalDepartment of Cell Biology and Genetics, Faculty of Science, Palacky University, Slechtitelu 27, 783 71 Olomouc, Czech Republic.
Zdeněk AndrysíkDepartment of Pharmacology, University of Colorado School of Medicine, Aurora, CO 80045, USA.
Aneesh ChandranDepartment of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109-1065, USA.
Sridhar ManiDepartment of Genetics and Department of Medicine, Albert Einstein College of Medicine, Bronx, NY 10461, USA.
Zdenek DvorakDepartment of Cell Biology and Genetics, Faculty of Science, Palacky University, Slechtitelu 27, 783 71 Olomouc, Czech Republic.
Palacký University Olomouc · CZAlbert Einstein College of Medicine · USUniversity of Colorado Denver · USUniversity of Michigan · US

Funding

Agentura Pro Zdravotnický Výzkum České Republiky NV19-05-00220
6 · The paper itself

Abstract

The efforts for therapeutic targeting of the aryl hydrocarbon receptor (AhR) have emerged in recent years. We investigated the effects of available antimigraine triptan drugs, having an indole core in their structure, on AhR signaling in human hepatic and intestinal cells. Activation of AhR in reporter gene assays was observed for Avitriptan and to a lesser extent for Donitriptan, while other triptans were very weak or no activators of AhR. Using competitive binding assay and by homology docking, we identified Avitriptan as a low-affinity ligand of AhR. Avitriptan triggered nuclear translocation of AhR and increased binding of AhR in CYP1A1 promotor DNA, as revealed by immune-fluorescence microscopy and chromatin immune-precipitation assay, respectively. Strong induction of

Indexed as

Basic Helix-Loop-Helix ProteinsCells, CulturedCytochrome P-450 CYP1A1Drug RepositioningEnzyme ActivationHepatocytesHumansIntestinal MucosaLigandsModels, MolecularMolecular Docking SimulationOrgan SpecificityPromoter Regions, GeneticReceptors, Aryl HydrocarbonSulfonamidesTryptaminesAHR protein, humanavitriptanBasic Helix-Loop-Helix ProteinsCYP1A1 protein, humanCytochrome P-450 CYP1A1LigandsReceptors, Aryl HydrocarbonSulfonamidesTryptaminesAntimigraine drugsAryl Hydrocarbon ReceptorrepurposingTriptans

Identifiers

PMID32316498
PMCPMC7216230
OpenAlexW3016842020

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.