Evidence map›Paper›PMID 27518621›Full record

ArticleMethods in molecular biology (Clifton, N.J.)2016

Quantitative High-Throughput Luciferase Screening in Identifying CAR Modulators.

Caitlin Lynch, Jinghua Zhao, Hongbing Wang, Menghang Xia

Abstract read
In one paragraph

Article in Methods in molecular biology (Clifton, N.J.), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
9.5field-weighted citation impact, top 2% 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

5 citing papers in PubMed, 9 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Identification of Modulators That Activate the Constitutive Androstane Receptor From the Tox21 10K Compound Library.Toxicological sciences : an official journal of the Society of Toxicology · 2019
    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

4 authors at 2 institutions in 1 country.

Caitlin LynchNational Center for Advancing Translational Sciences, National Institutes of Health, Building C, MSC: 3375, 9800 Medical Center Drive, Bethesda, MD, 20892, USA.
Jinghua ZhaoNational Center for Advancing Translational Sciences, National Institutes of Health, Building C, MSC: 3375, 9800 Medical Center Drive, Bethesda, MD, 20892, USA.
Hongbing WangDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, USA.
Menghang XiaNational Center for Advancing Translational Sciences, National Institutes of Health, Building C, MSC: 3375, 9800 Medical Center Drive, Bethesda, MD, 20892, USA. mxia@mail.nih.gov.
National Center for Advancing Translational Sciences · USUniversity of Maryland, Baltimore · US

Funding

Small molecule screening programZ01HG200319 · NHGRI · NATIONAL HUMAN GENOME RESEARCH INSTITUTE · PI AUSTIN, CHRISTOPHER P · 2004 to 2008
$32.3M
Toxicology in the 21st Century Program (Tox21) - Systems ToxicologyZIATR000038 · NCATS · NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES · PI XIA, MENGHANG · 2015 to 2025
$5.7M
Regulation of CYP2B6 in Human LIverR01DK061652 · NIDDK · UNIVERSITY OF NORTH CAROLINA CHAPEL HILL · PI WANG, HONGBING · 2003 to 2015
$3.7M
Intramural NIH HHS Z01 HG200319Intramural NIH HHS ZIA TR000038NIDDK NIH HHS R01 DK061652
6 · The paper itself

Abstract

The constitutive androstane receptor (CAR, NR1I3) is responsible for the transcription of multiple drug metabolizing enzymes and transporters. There are two possible methods of activation for CAR, direct ligand binding and a ligand-independent method, which makes this a unique nuclear receptor. Both of these mechanisms require translocation of CAR from the cytoplasm into the nucleus. Interestingly, CAR is constitutively active in immortalized cell lines due to the basal nuclear location of this receptor. This creates an important challenge in most in vitro assay models because immortalized cells cannot be used without inhibiting the high basal activity. In this book chapter, we go into detail of how to perform quantitative high-throughput screens to identify hCAR1 modulators through the employment of a double stable cell line. Using this line, we are able to identify activators, as well as deactivators, of the challenging nuclear receptor, CAR.

Indexed as

Founder EffectHigh-Throughput Screening AssaysActive Transport, Cell NucleusAntineoplastic AgentsCell LineCell NucleusCell SurvivalConstitutive Androstane ReceptorCytochrome P-450 CYP2B6CytoplasmGene Expression RegulationHep G2 CellsHumansIsoquinolinesLuciferasesOximes6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oximeAntineoplastic AgentsConstitutive Androstane ReceptorCYP2B6 protein, humanCytochrome P-450 CYP2B6IsoquinolinesLuciferasesNR1I3 protein, humanOximesPK 11195Receptors, Cytoplasmic and NuclearThiazolesConstitutive Androstane Receptor (CAR)Cytochrome P450 2B6 (CYP2B6)LuciferaseQuantitative high-throughput screening (qHTS)

Identifiers

PMID27518621
PMCPMC5341601
OpenAlexW2515794083

What OpenQuestion holds

Textmetadata
LicenceTDM
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.