Evidence mapPaperPMID 34067839Full record

ArticleMolecules (Basel, Switzerland)2021

Identification of Binding Regions of Bilirubin in the Ligand-Binding Pocket of the Peroxisome Proliferator-Activated Receptor-A (PPARalpha).

Darren M Gordon, Stephen H Hong, Zachary A Kipp, Terry D Hinds

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.

0numbers the graph read from it
0cells of the map it votes in
39citing papers in PubMed
2.4field-weighted citation impact, top 10% 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

39 citing papers in PubMed, 47 citations in OpenAlex.

  1. Article
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  8. Article
  9. Bilirubin Targeting WNK1 to Alleviate NLRP3-Mediated Neuroinflammation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025
    Article
  10. Review
  11. Bilirubin metabolism and its application in disease prevention: mechanisms and research advances.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2025
    Review
  12. Article
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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

4 authors at 2 institutions in 1 country.

Darren M GordonDepartment of Neurosciences, University of Toledo College of Medicine and Life Sciences, Toledo, OH 43614, USA.
Stephen H HongDepartment of Neurosciences, University of Toledo College of Medicine and Life Sciences, Toledo, OH 43614, USA.ORCID 0000-0002-9273-2465
Zachary A KippDepartment of Pharmacology and Nutritional Sciences, University of Kentucky College of Medicine, 760 Press Avenue, Healthy Kentucky Research Building, Lexington, KY 40508, USA.
Terry D HindsDepartment of Pharmacology and Nutritional Sciences, University of Kentucky College of Medicine, 760 Press Avenue, Healthy Kentucky Research Building, Lexington, KY 40508, USA.
University of Kentucky · USUniversity of Toledo · US

Funding

NIDDK NIH HHS 1R01DK121797NIDDK NIH HHS R01 DK121797
6 · The paper itself

Abstract

Recent work has shown that bilirubin has a hormonal function by binding to the peroxisome proliferator-activated receptor-α (PPARα), a nuclear receptor that drives the transcription of genes to control adiposity. Our previous in silico work predicted three potential amino acids that bilirubin may interact with by hydrogen bonding in the PPARα ligand-binding domain (LBD), which could be responsible for the ligand-induced function. To further reveal the amino acids that bilirubin interacts with in the PPARα LBD, we harnessed bilirubin's known fluorescent properties when bound to proteins such as albumin. Our work here revealed that bilirubin interacts with threonine 283 (T283) and alanine 333 (A333) for ligand binding. Mutational analysis of T283 and A333 showed significantly reduced bilirubin binding, reductions of 11.4% and 17.0%, respectively. Fenofibrate competitive binding studies for the PPARα LBD showed that bilirubin and fenofibrate possibly interact with different amino acid residues. Furthermore, bilirubin showed no interaction with PPARγ. This is the first study to reveal the amino acids responsible for bilirubin binding in the ligand-binding pocket of PPARα. Our work offers new insight into the mechanistic actions of a well-known molecule, bilirubin, and new fronts into its mechanisms.

Indexed as

BilirubinBinding, CompetitiveHEK293 CellsHumansLigandsPPAR alphaProtein BindingBilirubinLigandsPPAR alphaalbuminautofluorescencebilirubinbiliverdin reductaseBVRAheme oxygenaseHO-1mutagenesis analysisnuclear receptorPPAR

Identifiers

PMID34067839
PMCPMC8157031
OpenAlexW3160481258

What Socratic holds

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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 Socratic graph.