Evidence map›Paper›PMID 31768440›Full record

ArticleHeliyon2019

Identification and characterization of a phenyl-thiazolyl-benzoic acid derivative as a novel RAR/RXR agonist.

Chie Koshiishi, Takanori Kanazawa, Eric Vangrevelinghe, Toshiyuki Honda, Shinji Hatakeyama

Open access · goldAbstract read
In one paragraph

Article in Heliyon, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.3field-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

4 citing papers in PubMed, 8 citations in OpenAlex.

  1. Review
  2. Exploring the nexus of nuclear receptors in hematological malignancies.Cellular and molecular life sciences : CMLS · 2024
    Review
  3. Article
  4. iTRAQ-derived quantitative proteomics uncovers the neuroprotective property of bexarotene in a mice model of cerebral ischemia-reperfusion injury.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2022
    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

5 authors at 3 institutions in 3 countries.

Chie KoshiishiNovartis Institutes for BioMedical Research, Novartis Pharma K.K, Tsukuba, Ibaraki, Japan.
Takanori KanazawaNovartis Institutes for BioMedical Research, Novartis Pharma K.K, Tsukuba, Ibaraki, Japan.
Eric VangrevelingheNovartis Institutes for BioMedical Research, Novartis Pharma AG, Basel, Switzerland.
Toshiyuki HondaNovartis Institutes for BioMedical Research, Inc., Cambridge, MA, USA.
Shinji HatakeyamaNovartis Institutes for BioMedical Research, Novartis Pharma AG, Basel, Switzerland.
Novartis (Japan) · JPNovartis (Switzerland) · CHNovartis (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

objectiveTo identify an agonist of RXRα and RARα with reduced undesired profiles of all-trans retinoic acid for differentiation-inducing therapy of acute promyelocytic leukemia (APL), such as its susceptibility to P450 enzyme, induction of P450 enzyme, increased sequestration by cellular retinoic acid binding protein and increased expression of P-glycoprotein, a virtual screening was performed. RESULTS AND

conclusionIn this study, a phenyl-thiazolyl-benzoic acid derivative (PTB) was identified as a potent agonist of RXRα and RARα. PTB was characterized in nuclear receptor binding, reporter gene, cell differentiation and cell growth assays. PTB bound directly to RXRα and RARα, but not to PPARα, δ(β) or γ. PTB fully activated reporter genes with enhancer elements for RXRα/RXRα, and partially activated reporter genes with enhancer elements for RARα/RXRα, PPARδ(β) and PPARγ. Furthermore, PTB induced differentiation and inhibited the growth of human APL cells. Thus, PTB is a novel dual agonist of RXRα and RARα and works as both a differentiation inducer and a proliferation inhibitor to leukemic cells.

Indexed as

Acute promyelocytic leukemiaBiochemistryCancer researchDose-response relationshipDrug bindingHematological systemMolecular biologyOncologyRetinoic acidVirtual screening

Identifiers

PMID31768440
PMCPMC6872757
OpenAlexW2990246655

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.