Evidence map›Paper›PMID 34855388›Full record

ArticleJournal of medicinal chemistry2021

Indole-Containing Amidinohydrazones as Nonpeptide, Dual RXFP3/4 Agonists: Synthesis, Structure-Activity Relationship, and Molecular Modeling Studies.

Dongliang Guan, Md Toufiqur Rahman, Elaine A Gay, Vineetha Vasukuttan, Kelly M Mathews, Ann M Decker, Alexander H Williams, Chang-Guo Zhan, Chunyang Jin

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.2field-weighted citation impact, top 20% 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

6 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Staying Ahead of the Game: How SARS-CoV-2 has Accelerated the Application of Machine Learning in Pandemic Management.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy · 2023
    Review
  5. Article
  6. 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

9 authors at 2 institutions in 1 country.

Dongliang GuanCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.ORCID 0000-0002-7814-1116
Md Toufiqur RahmanCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.ORCID 0000-0003-2752-6822
Elaine A GayCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Vineetha VasukuttanCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Kelly M MathewsCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Ann M DeckerCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.ORCID 0000-0003-1899-6558
Alexander H WilliamsDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536, United States.
Chang-Guo ZhanDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536, United States.
Chunyang JinCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.ORCID 0000-0001-6733-3094
RTI International · USUniversity of Kentucky · US

Funding

Kentucky Center for Clinical and Translational ScienceUL1TR001998 · NCATS · UNIVERSITY OF KENTUCKY · PI HARTMANN, KATHERINE E, KERN, PHILIP A · 2016 to 2025
$34.2M
Understanding the role of anti-apolipoprotein A-I antibodies in atherosclerotic cardiovascular diseaseP20GM130456 · NIGMS · UNIVERSITY OF KENTUCKY · PI M. Ashfaqul Alam · 2020 to 2026
$18.7M
Training in Drug Abuse Related Research.T32DA016176 · NIDA · UNIVERSITY OF KENTUCKY · PI DWOSKIN, LINDA P · 2004 to 2020
$4.0M
Synthetic Cannabinoid Toxicity: Role of BiotransformationR01DA039143 · NIDA · UNIV OF ARKANSAS FOR MED SCIS · PI PRATHER, PAUL L · 2016 to 2020
$2.9M
Small molecule antagonist probes for the relaxin-3/RXFP3 systemR01AA028255 · NIAAA · RESEARCH TRIANGLE INSTITUTE · PI BESHEER, JOYCE, JIN, CHUNYANG · 2020 to 2022
$1.9M
NCATS NIH HHS UL1 TR001998NIAAA NIH HHS R01 AA028255NIDA NIH HHS R01 DA039143NIDA NIH HHS T32 DA016176NIGMS NIH HHS P20 GM130456
6 · The paper itself

Abstract

The central relaxin-3/RXFP3 system plays important roles in stress responses, feeding, and motivation for reward. However, exploration of its therapeutic applications has been hampered by the lack of small molecule ligands and the cross-activation of RXFP1 in the brain and RXFP4 in the periphery. Herein, we report the first structure-activity relationship studies of a series of novel nonpeptide amidinohydrazone-based agonists, which were characterized by RXFP3 functional and radioligand binding assays. Several potent and efficacious RXFP3 agonists (e.g.,

Indexed as

HumansHydrazonesIndolesModels, MolecularRadioligand AssayReceptors, G-Protein-CoupledReceptors, PeptideStructure-Activity RelationshipHydrazonesIndolesReceptors, G-Protein-CoupledReceptors, PeptideRXFP3 protein, humanRXFP4 protein, human

Identifiers

PMID34855388
PMCPMC8758203
OpenAlexW3215654177

What OpenQuestion holds

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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.