Evidence map›Paper›PMID 31247375›Full record

ArticleEuropean journal of medicinal chemistry2019

Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies.

Dongdong Liang, Linhao Li, Caitlin Lynch, Bryan Mackowiak, William D Hedrich, Yong Ai, Yue Yin, Scott Heyward, Menghang Xia, Hongbing Wang and 1 more

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

Article in European journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.0field-weighted citation impact, top 23% 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

3 citing papers in PubMed, 14 citations in OpenAlex.

  1. Article
  2. Article
  3. 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

11 authors at 2 institutions in 1 country.

Dongdong LiangDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, United States.
Linhao LiDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, United States.
Caitlin Lynch9800 Medical Center Drive, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD, 20892, United States.
Bryan MackowiakDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, United States.
William D HedrichDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, United States.
Yong AiDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, United States.
Yue YinDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, United States.
Scott HeywardBioIVT, 1450 S Rolling Rd, Halethorpe, MD, 21227, United States.
Menghang Xia9800 Medical Center Drive, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD, 20892, United States.
Hongbing WangDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, United States. Electronic address: hongbing.wang@rx.umaryland.edu.
Fengtian XueDepartment of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, United States. Electronic address: fxue@rx.umaryland.edu.
University of Maryland, Baltimore · USNational Institutes of Health · US

Funding

Function and Regulation of SLC13A5 in the LiverR01GM121550 · NIGMS · UNIVERSITY OF MARYLAND BALTIMORE · PI WANG, HONGBING · 2018 to 2021
$1.3M
Role of constitutive androstane receptor in cyclophosphamide-based chemotherapyR01GM107058 · NIGMS · UNIVERSITY OF MARYLAND BALTIMORE · PI WANG, HONGBING · 2013 to 2016
$1.2M
NIGMS NIH HHS R01 GM107058NIGMS NIH HHS R01 GM121550
6 · The paper itself

Abstract

The DNA alkylating prodrug cyclophosphamide (CPA), alone or in combination with other agents, is one of the most commonly used anti-cancer agents. As a prodrug, CPA is activated by cytochrome P450 2B6 (CYP2B6), which is transcriptionally regulated by the human constitutive androstane receptor (hCAR). Therefore, hCAR agonists represent novel sensitizers for CPA-based therapies. Among known hCAR agonists, compound 6-(4-chlorophenyl)imidazo-[2,1-b]thiazole-5-carbaldehyde-O-(3,4-dichlorobenzyl)oxime (CITCO) is the most potent and broadly utilized in biological studies. Through structural modification of CITCO, we have developed a novel compound DL5016 (32), which has an EC

Indexed as

Antineoplastic AgentsCell ProliferationCell SurvivalConstitutive Androstane ReceptorCyclophosphamideDose-Response Relationship, DrugDrug Screening Assays, AntitumorHep G2 CellsHumansLymphoma, Non-HodgkinMolecular StructureProdrugsReceptors, Cytoplasmic and NuclearStructure-Activity RelationshipTumor Cells, CulturedAntineoplastic AgentsConstitutive Androstane ReceptorCyclophosphamideProdrugsReceptors, Cytoplasmic and NuclearChemotherapyCo-cultureCyclophosphamideHuman constitutive androstane receptorStructure-activity relationship

Identifiers

PMID31247375
PMCPMC6718324
OpenAlexW2952639377

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.