Evidence map›Paper›PMID 34676039›Full record

ArticleACS medicinal chemistry letters2021

Potent Anti-Inflammatory, Arylpyrazole-Based Glucocorticoid Receptor Agonists That Do Not Impair Insulin Secretion.

Brandon J Kennedy, Ashley M Lato, Alexander R Fisch, Susan J Burke, Justin K Kirkland, Carson W Prevatte, Lee E Dunlap, Russell T Smith, Konstantinos D Vogiatzis, J Jason Collier and 1 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2021. 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
0.5field-weighted citation impact, top 29% 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

2 citing papers in PubMed, 4 citations in OpenAlex.

  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

11 authors at 2 institutions in 1 country.

Brandon J KennedyDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.ORCID https://orcid.org/0000-0003-1892-8926
Ashley M LatoDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.ORCID https://orcid.org/0000-0003-4076-9714
Alexander R FischDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.
Susan J BurkePennington Biomedical Research Center, Baton Rouge, Louisiana 70808, United States.
Justin K KirklandDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.
Carson W PrevatteDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.
Lee E DunlapDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.
Russell T SmithDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.
Konstantinos D VogiatzisDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.ORCID https://orcid.org/0000-0002-7439-3850
J Jason CollierPennington Biomedical Research Center, Baton Rouge, Louisiana 70808, United States.ORCID https://orcid.org/0000-0003-2817-4152
Shawn R CampagnaDepartment of Chemistry, University of Tennessee, Knoxville, Tennessee 37996, United States.ORCID https://orcid.org/0000-0001-6809-3862
University of Tennessee at Knoxville · USPennington Biomedical Research Center · US

Funding

Tracking & Evaluation CoreU54GM104940 · NIGMS · LSU PENNINGTON BIOMEDICAL RESEARCH CTR · PI Leigh Lamonica · 2012 to 2026
$69.1M
SGK1 is a regulator of islet beta cell mass and secretory functionR01DK123183 · NIDDK · LSU PENNINGTON BIOMEDICAL RESEARCH CTR · PI COLLIER, JAMES JASON · 2020 to 2024
$1.8M
A Unique Receptor Agonist Approach for Type 1 Diabetes PreventionR21AI138136 · NIAID · LSU PENNINGTON BIOMEDICAL RESEARCH CTR · PI COLLIER, JAMES JASON · 2018 to 2019
$436k
NIAID NIH HHS R21 AI138136NIDDK NIH HHS R01 DK123183NIGMS NIH HHS U54 GM104940
6 · The paper itself

Abstract

Glucocorticoids (GCs) are widely used in medicine for their role in the treatment of autoimmune-mediated conditions, certain cancers, and organ transplantation. The transcriptional activities GCs elicit include transrepression, postulated to be responsible for the anti-inflammatory activity, and transactivation, proposed to underlie the undesirable side effects associated with long-term use. A GC analogue that could elicit only transrepression and beneficial transactivation properties would be of great medicinal value and is highly sought after. In this study, a series of 1-(4-substituted phenyl)pyrazole-based GC analogues were synthesized, biologically screened, and evaluated for SARs leading to the desired activity. Activity observed in compounds bearing an electron deficient arylpyrazole moiety showed promise toward a dissociated steroid, displaying transrepression while having limited transactivation activity. In addition, compounds

Identifiers

PMID34676039
PMCPMC8521651
OpenAlexW3200284037

What OpenQuestion holds

Textmetadata
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.