Evidence map›Paper›PMID 24767852›Full record

ArticleBioorganic & medicinal chemistry letters2014

Bis-aryloxadiazoles as effective activators of the aryl hydrocarbon receptor.

Kaitlin J Basham, Vasudev R Bhonde, Collin Kieffer, James B C Mack, Matthew Hess, Bryan E Welm, Ryan E Looper

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2014. 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. 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

7 authors.

Kaitlin J BashamDepartment of Oncological Sciences, Huntsman Cancer Institute, University of Utah, Salt Lake City, UT 84112, USA.
Vasudev R BhondeDepartment of Chemistry, University of Utah, Salt Lake City, UT 84112, USA.
Collin KiefferDepartment of Oncological Sciences, Huntsman Cancer Institute, University of Utah, Salt Lake City, UT 84112, USA.
James B C MackDepartment of Chemistry, University of Utah, Salt Lake City, UT 84112, USA.
Matthew HessDepartment of Chemistry, University of Utah, Salt Lake City, UT 84112, USA.
Bryan E WelmDepartment of Oncological Sciences, Huntsman Cancer Institute, University of Utah, Salt Lake City, UT 84112, USA; Department of Surgery, University of Utah, Salt Lake City, UT 84112, USA.
Ryan E LooperDepartment of Chemistry, University of Utah, Salt Lake City, UT 84112, USA. Electronic address: r.looper@utah.edu.

Funding

DEVELOPMENTAL BIOLOGY TRAINING PROGRAMT32HD007491 · NICHD · UTAH STATE HIGHER EDUCATION SYSTEM--UNIVERSITY OF UTAH · PI James Alan Gagnon, Kristen M Kwan · 1995 to 2026
$8.0M
Synthetic and biological investigations of 2-aminoimidazole derived natural products.R01GM090082 · NIGMS · UNIVERSITY OF UTAH · PI LOOPER, RYAN EDWARD · 2010 to 2019
$2.6M
Identification of Novel Cancer Selective Compounds in 3D Tumor Organoid AssaysR01CA140296 · NCI · UNIVERSITY OF UTAH · PI SIGMAN, MATTHEW S · 2009 to 2013
$1.5M
Analysis of the Cellular Origins of Breast CancerR01CA143815 · NCI · UNIVERSITY OF UTAH · PI WELM, BRYAN E. · 2010 to 2014
$1.5M
NCI NIH HHS R01 CA140296NCI NIH HHS R01-CA140296NCI NIH HHS R01 CA143815NCI NIH HHS R01-CA143815NICHD NIH HHS T32 HD007491NIGMS NIH HHS R01 GM090082NIGMS NIH HHS R01-GM090082
6 · The paper itself

Abstract

Bis-aryloxadiazoles are common scaffolds in medicinal chemistry due to their wide range of biological activities. Previously, we identified a 1,2,4-bis-aryloxadiazole that blocks mammary branching morphogenesis through activation of the aryl hydrocarbon receptor (AHR). In addition to defects in mammary differentiation, AHR stimulation induces toxicity in many other tissues. We performed a structure activity relationship (SAR) study of 1,2,4-bis-aryloxadiazole to determine which moieties of the molecule are critical for AHR activation. We validated our results with a functional biological assay, using desmosome formation during mammary morphogenesis to indicate AHR activity. These findings will aid the design of oxadiazole derivative therapeutics with reduced off-target toxicity profiles.

Indexed as

Dose-Response Relationship, DrugHumansModels, MolecularMolecular StructureOxadiazolesReceptors, Aryl HydrocarbonStructure-Activity RelationshipOxadiazolesReceptors, Aryl HydrocarbonAryl hydrocarbon receptorBranching morphogenesisDioxinMammary glandOxadiazole

Identifiers

PMID24767852
PMCPMC4086406

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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.