Evidence map›Paper›PMID 37421886›Full record

ArticleEuropean journal of medicinal chemistry2023

Development and pharmacological evaluation of a new chemical series of potent pan-ERR agonists, identification of SLU-PP-915.

Carissa S Hampton, Sadichha Sitaula, Cyrielle Billon, Keith Haynes, Amer Avdagic, Udayanga Wanninayake, Christiana M Adeyemi, Arindam Chatterjee, Kristine Griffett, Subhashis Banerjee and 7 more

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
3.1field-weighted citation impact, top 8% 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

9 citing papers in PubMed, 10 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

17 authors at 3 institutions in 1 country.

Carissa S HamptonDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Sadichha SitaulaCenter for Clinical Pharmacology, St. Louis College of Pharmacy, Saint Louis, Missouri, 63110, United States.
Cyrielle BillonCenter for Clinical Pharmacology, St. Louis College of Pharmacy, Saint Louis, Missouri, 63110, United States.
Keith HaynesDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Amer AvdagicDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Udayanga WanninayakeDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Christiana M AdeyemiDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Arindam ChatterjeeDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Kristine GriffettCenter for Clinical Pharmacology, St. Louis College of Pharmacy, Saint Louis, Missouri, 63110, United States.
Subhashis BanerjeeDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Sheryl L BurrisCenter for Clinical Pharmacology, St. Louis College of Pharmacy, Saint Louis, Missouri, 63110, United States.
Emmalie SchoepkeDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Terri BoehmDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Alex BessDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Ian Mitchelle S de VeraDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States.
Thomas P BurrisUniversity of Florida Genetics Institute, Gainesville, FL, 32310, USA.
John K WalkerDepartment of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri, 63104, United States; Institute for Translational Neuroscience, Saint Louis University, St. Louis MO, 63110, United States. Electronic address: john.walker@health.slu.edu.
Saint Louis University · USUniversity of Health Sciences and Pharmacy · USUniversity of Florida · US

Funding

Exercise Mimetics for Dementia and Alzheimer's DiseaseRF1AG077160 · NIA · UNIVERSITY OF FLORIDA · PI BURRIS, THOMAS P, ELGENDY, BAHAA · 2023 to 2023
$2.3M
ERRgamma Agonists to Treat Muscular DystrophyR01AR069280 · NIAMS · ST. LOUIS COLLEGE OF PHARMACY · PI BURRIS, THOMAS P, WALKER, JOHN K. · 2016 to 2018
$1.7M
NIAMS NIH HHS R01 AR069280NIA NIH HHS RF1 AG077160
6 · The paper itself

Abstract

Estrogen-related receptors (ERR) are an orphan nuclear receptor sub-family that play a critical role in regulating gene transcription for several physiological processes including mitochondrial function, cellular energy utilization and homeostasis. They have also been implicated to play a role in several pathological conditions. Herein, we report the identification, synthesis, structure-activity relationships and pharmacological evaluation of a new chemical series of potent pan-ERR agonists. This template was designed for ERRγ starting from the known acyl hydrazide template and compounds such as agonist GSK-4716 employing a structure-based drug design approach. This led to the preparation of a series of 2,5-disubstituted thiophenes from which several were found to be potent agonists of ERRγ in cell-based co-transfection assays. Additionally, direct binding to ERRγ was established through

Indexed as

EstrogensProtein IsoformsEstrogensProtein Isoforms2 5-disubstituted thiophenesBoronic acidEstrogen-related receptorNuclear receptorPan-agonist

Identifiers

PMID37421886
PMCPMC10399613
OpenAlexW4381952723

What OpenQuestion holds

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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.