Evidence map›Paper›PMID 30409702›Full record

ArticleBioorganic & medicinal chemistry2018

Design, synthesis, and ex vivo evaluation of a selective inhibitor for retinaldehyde dehydrogenase enzymes.

Angelica R Harper, Anh T Le, Timothy Mather, Anthony Burgett, William Berry, Jody A Summers

Open access · hybridAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.5field-weighted citation impact, top 36% 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

7 citing papers in PubMed, 13 citations in OpenAlex.

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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

6 authors at 3 institutions in 1 country.

Angelica R HarperDepartment of Cell Biology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, United States.
Anh T LeDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, OK 73019, United States.
Timothy MatherOklahoma Medical Research Foundation, Oklahoma City, OK 73104, United States.
Anthony BurgettDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, OK 73019, United States.
William BerryDepartment of Cell Biology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, United States.
Jody A SummersDepartment of Cell Biology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73104, United States. Electronic address: jody-summers@ouhsc.edu.
University of Oklahoma Health Sciences Center · USUniversity of Oklahoma · USOklahoma Medical Research Foundation · US

Funding

Structure-Function Studies of MsvR, a Methanogen-Specific Transcriptional RegulaP20GM103640 · NIGMS · UNIVERSITY OF OKLAHOMA · PI WEST, ANN H · 2012 to 2021
$20.4M
Regulation of Scleral Growth and Remodelling in MyopiaR01EY009391 · NEI · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI SUMMERS, JODY A · 1992 to 2021
$6.5M
Identifying the Role of RALDH2 Mediated Retinoic Acid Synthesis in Visually Guided Eye GrowthF31EY025168 · NEI · UNIVERSITY OF OKLAHOMA HLTH SCIENCES CTR · PI HARPER, ANGELICA R · 2015 to 2016
$58k
NEI NIH HHS F31 EY025168NEI NIH HHS R01 EY009391NIGMS NIH HHS P20 GM103640
6 · The paper itself

Abstract

The retinaldehyde dehydrogenase (RALDH) enzymes, RALDH1, RALDH2, and RALDH3, catalyze the irreversible oxidation of retinaldehyde to all-trans-retinoic acid (ATRA). Despite the importance of the RALDH enzymes in embryonic development, postnatal growth and differentiation, and in several disease states, there are no commercially available inhibitors that specifically target these isozymes. We report here the development and characterization of a small molecule inhibitor dichloro-all-trans-retinone (DAR) (Summers et al., 2017) that is an irreversible inhibitor of RALDH1, 2, and 3 that effectively inhibits RALDH1, 2, and 3 in the nanomolar range but has no inhibitory activity against mitochondrial ALDH2. These results provide support for the development of DAR as a specific ATRA synthesis inhibitor for a variety of experimental and clinical applications.

Indexed as

Drug DesignAldehyde DehydrogenaseAldehyde Dehydrogenase 1 FamilyAldehyde OxidoreductasesAnimalsCells, CulturedChickensDose-Response Relationship, DrugEnzyme InhibitorsHEK293 CellsHumansKineticsMaleModels, MolecularMolecular StructureRetinal DehydrogenaseAldehyde DehydrogenaseAldehyde Dehydrogenase 1 Familyaldehyde dehydrogenase (NAD(P)+)Aldehyde OxidoreductasesALDH1A1 protein, humanALDH1A2 protein, humanEnzyme InhibitorsRetinal Dehydrogenase

Identifiers

PMID30409702
PMCPMC6331054
OpenAlexW2898386358

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.