Evidence map›Paper›PMID 39945195›Full record

ArticleJournal of medicinal chemistry2025

BRF110, an Orally Active Nurr1-RXRα-Selective Rexinoid, Enhances BDNF Expression without Elevating Triglycerides.

Xenophon Asvos, Mohamed A El Mubarak, Theodoros Karampelas, Theodoros Rampias, Constantin Tamvakopoulos, Gregory B Sivolapenko, Athanasios Papakyriakou, Stavros Topouzis, Demetrios K Vassilatis, Demosthenes Fokas

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In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
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

2 citing papers in PubMed.

  1. Article
  2. Review
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

10 authors.

Xenophon AsvosDepartment of Materials Science and Engineering, University of Ioannina, Ioannina 45110, Greece.
Mohamed A El MubarakDepartment of Pharmacy, University of Patras, Patras 26504, Greece.
Theodoros KarampelasCenter for Clinical Research, Experimental Surgery, and Translational Research, Biomedical Research Foundation of the Academy of Athens, Athens 11527, Greece.
Theodoros RampiasCenter for Clinical Research, Experimental Surgery, and Translational Research, Biomedical Research Foundation of the Academy of Athens, Athens 11527, Greece.
Constantin TamvakopoulosCenter for Clinical Research, Experimental Surgery, and Translational Research, Biomedical Research Foundation of the Academy of Athens, Athens 11527, Greece.ORCID 0000-0001-9627-4812
Gregory B SivolapenkoDepartment of Pharmacy, University of Patras, Patras 26504, Greece.
Athanasios PapakyriakouInstitute of Biosciences and Applications, National Centre for Scientific Research "Demokritos", Athens 15341, Greece.ORCID 0000-0003-3931-6232
Stavros TopouzisDepartment of Pharmacy, University of Patras, Patras 26504, Greece.
Demetrios K VassilatisCenter for Clinical Research, Experimental Surgery, and Translational Research, Biomedical Research Foundation of the Academy of Athens, Athens 11527, Greece.
Demosthenes FokasDepartment of Materials Science and Engineering, University of Ioannina, Ioannina 45110, Greece.ORCID 0009-0004-6039-5048

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

We report the discovery of a Nurr1-RXRα heterodimer-selective rexinoid which emerged from the structural modification of aminopyrimidine XCT0135908. Although XCT0135908 demonstrated high selectivity for the Nurr1-RXRα heterodimer over other RXRα dimerization partners, its poor in vivo stability and limited brain penetration hindered its utility. Structure-activity relationship (SAR) studies alongside bioactivity evaluations of a diverse series of substituted pyrimidines led to BRF110, a brain-penetrant compound retaining the selective activation of the Nurr1-RXRα heterodimer. BRF110, as XCT0135908, protects dopaminergic cells against the Parkinson's disease-related toxin MPP

Indexed as

Brain-Derived Neurotrophic FactorNuclear Receptor Subfamily 4, Group A, Member 2Retinoid X Receptor alphaAdministration, OralAnimalsDopaminergic NeuronsHumansMaleMiceMice, Inbred C57BLNeuroprotective AgentsPyrimidinesStructure-Activity RelationshipTriglyceridesBrain-Derived Neurotrophic FactorNeuroprotective AgentsNuclear Receptor Subfamily 4, Group A, Member 2PyrimidinesRetinoid X Receptor alphaTriglycerides

Identifiers

PMID39945195
PMCPMC11874024

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Registered trials

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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.