Evidence map›Paper›PMID 39240657›Full record

ArticleJournal of medicinal chemistry2024

Merging Natural Product Structures with Pharmaceutical Leads: Unnatural Enantiomers of Estranes as Glucocorticoid Receptor Modulators That Suppress TNF-α and IL-6 Release.

Joshua M Nicholson, Dexi Yang, Thomas Koelblen, Eric L Hu, Christopher C Coss, Thomas P Burris, Xiao Hu, Glenn C Micalizio

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. Review
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

8 authors.

Joshua M Nicholson6128 Burke Laboratory, Department of Chemistry, Dartmouth College, Hanover, New Hampshire 03755, United States.
Dexi YangDepartment of Chemistry, The Scripps Research Institute, Scripps Florida, Jupiter, Florida 33458, United States.
Thomas KoelblenUniversity of Florida Genetics Institute, Gainesville, Florida 32610, United States.
Eric L HuComputational Biology Undergraduate Concentration, Brown University, 69 Brown Street, Mail no. 4277, Providence, Rhode Island 02912, United States.
Christopher C CossDivision of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.ORCID 0000-0002-8184-9190
Thomas P BurrisUniversity of Florida Genetics Institute, Gainesville, Florida 32610, United States.ORCID 0000-0003-2922-4449
Xiao HuAccunet LLC BioPharma Consulting, 1805 Olive Green Street, Chula Vista, California 91913, United States.
Glenn C Micalizio6128 Burke Laboratory, Department of Chemistry, Dartmouth College, Hanover, New Hampshire 03755, United States.ORCID 0000-0002-3408-5570

Funding

Metallacycle-mediated coupling in stereoselective synthesisR35GM134725 · NIGMS · DARTMOUTH COLLEGE · PI MICALIZIO, GLENN C · 2020 to 2024
$2.6M
NIGMS NIH HHS R35 GM134725
6 · The paper itself

Abstract

Natural products are widely recognized as valuable starting points for the development of therapeutics, with synthetic tetracyclic triterpenoids (e.g., steroids) being the most well represented among the drugs approved by the Food and Drug Administration. Here, recently developed synthetic tools for concise, asymmetric, and convergent construction of steroidal systems are leveraged to drive a program aimed at identifying novel glucocorticoid receptor (GR) modulators. While glucocorticoids have been extensively used as anti-inflammatory agents, they are plagued by severe side effects that include bone loss, muscle wasting, and metabolic disease. Ultimately, a program targeting the unnatural enantiomers of estranes (

Indexed as

Biological ProductsInterleukin-6Interleukin-6 InhibitorsReceptors, GlucocorticoidTumor Necrosis Factor-alphaAnimalsAnti-Inflammatory AgentsHumansMiceStereoisomerismStructure-Activity RelationshipAnti-Inflammatory AgentsBiological ProductsInterleukin-6Interleukin-6 InhibitorsReceptors, GlucocorticoidTumor Necrosis Factor-alpha

Identifiers

PMID39240657
PMCPMC11609614

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.