Evidence map›Paper›PMID 32631520›Full record

ArticleBioorganic & medicinal chemistry letters2020

Discovery of phenanthridine analogues as novel chemical probes disrupting the binding of DNA to ΔFosB homodimers and ΔFosB/JunD heterodimers.

Yi Li, Zhiqing Liu, Galina Aglyamova, Jianping Chen, Haiying Chen, Mukund Bhandari, Mark A White, Gabrielle Rudenko, Jia Zhou

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

Article in Bioorganic & medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.4field-weighted citation impact, top 40% 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

1 citing paper in PubMed, 7 citations in OpenAlex.

  1. 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

9 authors at 1 institution in 1 country.

Yi LiDepartment of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
Zhiqing LiuDepartment of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
Galina AglyamovaDepartment of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
Jianping ChenDepartment of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
Haiying ChenDepartment of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
Mukund BhandariDepartment of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
Mark A WhiteDepartment of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, TX 77555, United States; Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch, Galveston, TX 77555, United States.
Gabrielle RudenkoDepartment of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States; Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch, Galveston, TX 77555, United States. Electronic address: garudenk@utmb.edu.
Jia ZhouDepartment of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States; Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch, Galveston, TX 77555, United States. Electronic address: jizhou@utmb.edu.
The University of Texas Medical Branch at Galveston · US

Funding

Small molecule modulators of ΔFosB FunctionR01DA040621 · NIDA · UNIVERSITY OF TEXAS MED BR GALVESTON · PI NESTLER, ERIC J., ROBISON, ALFRED J · 2016 to 2025
$7.1M
NIDA NIH HHS R01 DA040621
6 · The paper itself

Abstract

The transcription factor ΔFosB accumulates in response to chronic insults such as drugs of abuse, L-3,4-dihydroxyphenylalanine (l-DOPA) or stress in specific regions of the brain, triggering long lasting neural and behavioral changes that underlie aspects of drug addiction, dyskinesia, and depression. Thus, small molecule chemical probes are urgently needed to investigate biological functions of ΔFosB. Herein we describe the identification of a novel phenanthridine analogue ZL0220 (27) as an active and promising ΔFosB chemical probe with micromolar inhibitory activities against ΔFosB homodimers and ΔFosB/JunD heterodimers.

Indexed as

Drug DiscoveryBinding SitesDNADose-Response Relationship, DrugHumansMolecular Docking SimulationMolecular StructurePhenanthridinesProto-Oncogene Proteins c-fosProto-Oncogene Proteins c-junStructure-Activity RelationshipDNAJunD protein, humanPhenanthridinesProto-Oncogene Proteins c-fosProto-Oncogene Proteins c-junChemical probesFluorescence polarization assayHigh-throughput screeningΔFosB homodimerΔFosB/JunD heterodimer

Identifiers

PMID32631520
PMCPMC7376976
OpenAlexW3033818658

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.