Evidence map›Paper›PMID 34046601›Full record

ArticleRSC medicinal chemistry2021

Pharmacophore-based screening of diamidine small molecule inhibitors for protein arginine methyltransferases.

Kun Qian, Chunli Yan, Hairui Su, Tran Dang, Bo Zhou, Zhenyu Wang, Xinyang Zhao, Ivaylo Ivanov, Meng-Chiao Ho, Y George Zheng

Open access · bronzeAbstract read
In one paragraph

Article in RSC medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.3field-weighted citation impact, top 45% 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

4 citing papers in PubMed, 12 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. 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

10 authors at 4 institutions in 2 countries.

Kun QianDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia Athens Georgia 30602 USA yzheng@uga.edu +(706) 542 0277.ORCID https://orcid.org/0000-0003-1132-2374
Chunli YanDepartment of Chemistry and Center for Diagnostics and Therapeutics, Georgia State University Atlanta Georgia 30302 USA.
Hairui SuDepartment of Biochemistry and Molecular Genetics, The University of Alabama at Birmingham Birmingham Alabama 35294 USA.
Tran DangDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia Athens Georgia 30602 USA yzheng@uga.edu +(706) 542 0277.
Bo ZhouDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia Athens Georgia 30602 USA yzheng@uga.edu +(706) 542 0277.
Zhenyu WangDepartment of Chemistry and Center for Diagnostics and Therapeutics, Georgia State University Atlanta Georgia 30302 USA.
Xinyang ZhaoDepartment of Biochemistry and Molecular Genetics, The University of Alabama at Birmingham Birmingham Alabama 35294 USA.
Ivaylo IvanovDepartment of Chemistry and Center for Diagnostics and Therapeutics, Georgia State University Atlanta Georgia 30302 USA.
Meng-Chiao HoInstitute of Biological Chemistry, Academia Sinica Nankang Taipei Taiwan.
Y George ZhengDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia Athens Georgia 30602 USA yzheng@uga.edu +(706) 542 0277.ORCID https://orcid.org/0000-0001-7116-3067
University of Georgia · USGeorgia State University · USUniversity of Alabama at Birmingham · USInstitute of Biological Chemistry, Academia Sinica · TW

Funding

Integrative modeling of PCNA assemblies engaged in genome duplication and repairR01GM110387 · NIGMS · GEORGIA STATE UNIVERSITY · PI IVANOV, IVAYLO NIKOLAEV · 2015 to 2019
$1.7M
Mechanism and Inhibition of Protein Arginine MethylationR01GM126154 · NIGMS · UNIVERSITY OF GEORGIA · PI ZHENG, Y. GEORGE · 2018 to 2021
$1.2M
The Functions of antisense RNA AS-RBM15 in hematopoiesisR01DK110574 · NIDDK · UNIVERSITY OF ALABAMA AT BIRMINGHAM · PI ZHAO, XINYANG · 2017 to 2019
$668k
PRMT1-mediated metabolic reprogramming in leukemia progressionR21CA202390 · NCI · UNIVERSITY OF ALABAMA AT BIRMINGHAM · PI KLUG, CHRISTOPHER, ZHAO, XINYANG · 2016 to 2017
$352k
NCI NIH HHS R21 CA202390NIDDK NIH HHS R01 DK110574NIGMS NIH HHS R01 GM110387NIGMS NIH HHS R01 GM126154
6 · The paper itself

Abstract

Protein arginine methyltransferases (PRMTs) are essential epigenetic and post-translational regulators in eukaryotic organisms. Dysregulation of PRMTs is intimately related to multiple types of human diseases, particularly cancer. Based on the previously reported PRMT1 inhibitors bearing the diamidine pharmacophore, we performed virtual screening to identify additional amidine-associated structural analogs. Subsequent enzymatic tests and characterization led to the discovery of a top lead K313 (2-(4-((4-carbamimidoylphenyl)amino)phenyl)-1

Identifiers

PMID34046601
PMCPMC8130551
OpenAlexW3090114053

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.