Evidence map›Paper›PMID 25350970›Full record

ArticleOncotarget2014

A novel drug discovery strategy: mechanistic investigation of an enantiomeric antitumor agent targeting dual p53 and NF-κB pathways.

Chunlin Zhuang, Chunquan Sheng, Woo Shik Shin, Yuelin Wu, Jin Li, Jianzhong Yao, Guoqiang Dong, Wen Zhang, Yuk Yin Sham, Zhenyuan Miao and 1 more

Open access · diamondAbstract read
In one paragraph

Article in Oncotarget, 2014. 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
1.1field-weighted citation impact, top 24% 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, 12 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Chemical Variations on the p53 Reactivation Theme.Pharmaceuticals (Basel, Switzerland) · 2016
    Review
  5. Article
  6. 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 2 countries.

Chunlin ZhuangDepartment of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China. Research Center for Marine Drugs, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Chunquan ShengDepartment of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Woo Shik ShinCenter for Drug Design, Academic Health Center, University of Minnesota, Minneapolis, 55455, Minnesota.
Yuelin WuDepartment of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Jin LiDepartment of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Jianzhong YaoDepartment of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Guoqiang DongDepartment of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Wen ZhangResearch Center for Marine Drugs, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Yuk Yin ShamCenter for Drug Design, Academic Health Center, University of Minnesota, Minneapolis, 55455, Minnesota.
Zhenyuan MiaoDepartment of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Wannian ZhangDepartment of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China.
Second Military Medical University · CNUniversity of Minnesota · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The p53 and nuclear factor κB (NF-κB) pathways play crucial roles in human cancer development. Simultaneous targeting of both pathways is an attractive therapeutic strategy against cancer. In this study, we report an antitumor molecule that bears a pyrrolo[3,4-c]pyrazole scaffold and functions as an enantiomeric inhibitor against both the p53-MDM2 interaction and the NF-κB activation. It is a first-in-class enantiomeric inhibitor with dual efficacy for cancer therapy. Synergistic effect was observed in vitro and in vivo. Docking and molecular dynamics simulation studies further provided insights into the nature of stereoselectivity.

Indexed as

Drug DiscoveryAnimalsAntineoplastic AgentsApoptosisBlotting, WesternCell ProliferationDrug Screening Assays, AntitumorFlow CytometryHumansMaleMiceMice, Inbred BALB CMice, NudeModels, MolecularMolecular Dynamics SimulationMolecular Structure5-(3-(1H-imidazol-1-yl)propyl)-4-(4-bromophenyl)-1-(4-fluorobenzyl)-3-phenyl-4,5-dihydropyrrolo(3,4-c)pyrazol-6(1H)-oneAntineoplastic AgentsNF-kappa BProto-Oncogene Proteins c-mdm2pyrazolePyrazolesPyrrolidinonesTumor Suppressor Protein p53

Identifiers

PMID25350970
PMCPMC4279413
OpenAlexW1582393024

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.