Evidence map›Paper›PMID 36389181›Full record

ArticleMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents2022

Synthesis of 2-Oxoquinoline Derivatives as Dual Pim and mTORC Protein Kinase Inhibitors.

Giri R Gnawali, Koichi Okumura, Karolina Perez, Rosa Gallagher, Julia Wulfkuhle, Emanuel F Petricoin, Sathish Kumar Reddy Padi, Jeremiah Bearss, Zhiyong He, Wei Wang and 1 more

Open access · greenAbstract read
In one paragraph

Article in Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, 2022. 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
0.4field-weighted citation impact, top 39% 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, 5 citations in OpenAlex.

  1. Review
  2. 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

11 authors at 3 institutions in 1 country.

Giri R GnawaliR. Ken Coit College of Pharmacy, University of Arizona, Department of Pharmacology and Toxicology, 1295 N. Martin Ave, Tucson, AZ, 85721 USA.
Koichi OkumuraUniversity of Arizona College of Medicine, Department of Physiology, 1501 N. Campbell, Tucson, AZ 85724 USA.
Karolina PerezUniversity of Arizona Cancer Center, Department of Medicine, 1515 N. Campbell Ave., Tucson, AZ 85724 USA.
Rosa GallagherCenter for Applied Proteomics and Molecular Medicine, George Mason University, Manassas, Virginia.
Julia WulfkuhleCenter for Applied Proteomics and Molecular Medicine, George Mason University, Manassas, Virginia.
Emanuel F PetricoinCenter for Applied Proteomics and Molecular Medicine, George Mason University, Manassas, Virginia.
Sathish Kumar Reddy PadiDepartment of Molecular Biology and Biophysics, UConn Health, 263 Farmington Ave., Farmington, CT 06030.
Jeremiah BearssUniversity of Arizona Cancer Center, Department of Medicine, 1515 N. Campbell Ave., Tucson, AZ 85724 USA.
Zhiyong HeR. Ken Coit College of Pharmacy, University of Arizona, Department of Pharmacology and Toxicology, 1295 N. Martin Ave, Tucson, AZ, 85721 USA.
Wei WangR. Ken Coit College of Pharmacy, University of Arizona, Department of Pharmacology and Toxicology, 1295 N. Martin Ave, Tucson, AZ, 85721 USA.
Andrew S KraftUniversity of Arizona Cancer Center, Department of Medicine, 1515 N. Campbell Ave., Tucson, AZ 85724 USA.
University of Arizona · USGeorge Mason University · USUConn Health · US

Funding

VITAMIN AP30CA023074 · NCI · UNIVERSITY OF ARIZONA · PI Teri L Bankhead · 1985 to 2026
$110.2M
Design of Fe2+ and H2O2 Induced Proximity Functionalized Imaging Probes for the Control of Cellular FunctionsR01GM130772 · NIGMS · UNIVERSITY OF ARIZONA · PI WANG, WEI · 2019 to 2022
$1.3M
Regulation of P-Body Formation and mRNA Decapping in Cancer: Control by AKT and Pim Kinase Phosphorylation of EDC3R21CA241010 · NCI · UNIVERSITY OF ARIZONA · PI OKUMURA, KOICHI · 2020 to 2020
$395k
NCI NIH HHS P30 CA023074NCI NIH HHS R21 CA241010NIGMS NIH HHS R01 GM130772
6 · The paper itself

Abstract

Compound VBT-5445 was identified as an inhibitor to block the association of Pim and the protein Enhancer of Decapping 3 (EDC3), a Pim substrate, which normally functions to enhance the decapping of messenger RNA (mRNA). It was also shown to inhibit both the Pim and mTORC protein kinases. The activity of this compound class can be fine-tuned by structural modification. A series of VBT analogs were designed, synthesized, and evaluated. These compounds decrease the growth of multiple cancer types, including pancreas, prostate, breast, lung, and leukemia. Notably, 6-methyl (GRG-1-31,

Indexed as

antitumor activitymTORCPim kinaseQuinoline derivatives

Identifiers

PMID36389181
PMCPMC9648566
OpenAlexW4281555172

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.