Evidence map›Paper›PMID 37154197›Full record

ArticleArchiv der Pharmazie2023

Investigation of selective retinoic acid receptor alpha antagonist ER-50891 and related analogs for male contraception.

Jillian L Kyzer, Md Abdullah Al Noman, Rebecca A D Cuellar, Sanny S W Chung, Soma Maitra, Tahmina Naqvi, Jon E Hawkinson, Debra J Wolgemuth, Gunda I Georg

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

Article in Archiv der Pharmazie, 2023. 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
2.0field-weighted citation impact, top 14% 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

9 authors at 2 institutions in 1 country.

Jillian L KyzerDepartment of Medicinal Chemistry, Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA.
Md Abdullah Al NomanDepartment of Medicinal Chemistry, Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA.
Rebecca A D CuellarDepartment of Medicinal Chemistry, Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA.
Sanny S W ChungDepartment of Genetics and Development, Columbia University Medical Center, New York, New York, USA.
Soma MaitraDepartment of Medicinal Chemistry, Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA.
Tahmina NaqviDepartment of Medicinal Chemistry, Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA.
Jon E HawkinsonDepartment of Medicinal Chemistry, Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA.
Debra J WolgemuthDepartment of Genetics and Development, Columbia University Medical Center, New York, New York, USA.
Gunda I GeorgDepartment of Medicinal Chemistry, Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA.ORCID http://orcid.org/0000-0002-8900-9460
University of Minnesota · USColumbia University Irving Medical Center · US

Funding

Drug Discovery & Synthesis of Contraceptive AgentsU01HD076542 · NICHD · UNIVERSITY OF MINNESOTA · PI GEORG, GUNDA I. · 2012 to 2016
$5.0M
Understanding Behavioral Patterns in Contraceptive UseU54HD093540 · NICHD · UNIVERSITY OF MINNESOTA · PI BARBER, JENNIFER S. · 2017 to 2018
$4.4M
Chemistry-Biology Interface Training GrantT32GM008700 · NIGMS · UNIVERSITY OF MINNESOTA TWIN CITIES · PI DISTEFANO, MARK D · 1999 to 2018
$4.0M
Understanding Behavioral Patterns in Contraceptive UseP50HD093540 · NICHD · UNIVERSITY OF MINNESOTA · PI BARBER, JENNIFER S. · 2019 to 2020
$3.9M
NICHD NIH HHS HHSN275201300017CNICHD NIH HHS P50 HD093540NICHD NIH HHS U01 HD076542NICHD NIH HHS U54 HD093540NIGMS NIH HHS GM008700NIGMS NIH HHS T32 GM008700
6 · The paper itself

Abstract

Retinoic acid receptor alpha (RARα) antagonist ER-50891 and 15 analogs were prepared and tested in vitro for potency and selectivity at RARα, RARβ, and RARγ using transactivation assays. Minor modifications to the parent molecule such as the introduction of a C4 tolyl group in place of the C4 phenyl group on the quinoline moiety slightly increased the RARα selectivity but larger substituents significantly decreased the potency. Replacement of the pyrrole moiety of ER-50891 with triazole, amides, or a double bond produced inactive compounds. ER-50891 was found to be stable in male mouse liver microsomes and was tested in male mice to assess its effects on spermatogenesis. Characteristic, albeit modest and transient, effects on spermatogenesis were observed.

Indexed as

ContraceptionAnimalsMaleMiceRetinoic Acid Receptor alphaStructure-Activity RelationshipRetinoic Acid Receptor alphainhibitionretinoic acid receptor alphaselectivityspermatogenesistransactivation assays

Identifiers

PMID37154197
PMCPMC13243132
OpenAlexW4375863054

What OpenQuestion holds

Textmetadata
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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.