Evidence map›Paper›PMID 32440103›Full record

ArticleDrug design, development and therapy2020

Virtual Screening and Optimization of Novel mTOR Inhibitors for Radiosensitization of Hepatocellular Carcinoma.

Ying-Qi Feng, Shuang-Xi Gu, Yong-Shou Chen, Xu-Dong Gao, Yi-Xin Ren, Jian-Chao Chen, Yin-Ying Lu, Heng Zhang, Shuang Cao

Open access · goldAbstract read
In one paragraph

Article in Drug design, development and therapy, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed, 1 pooled it
1.2field-weighted citation impact, top 23% 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

13 citing papers in PubMed, 1 synthesis or guideline pooled it, 20 citations in OpenAlex.

  1. Pooled it
  2. Review
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  5. Article
  6. The Role of PI3K/AKT/mTOR Signaling in Hepatocellular Carcinoma Metabolism.International journal of molecular sciences · 2023
    Review
  7. Article
  8. Article
  9. Article
  10. Review
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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 4 institutions in 1 country.

Ying-Qi Feng *Key Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430072, People's Republic of China.
Shuang-Xi Gu *Key Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430072, People's Republic of China.ORCID 0000-0003-0159-4616
Yong-Shou Chen *Key Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430072, People's Republic of China.
Xu-Dong GaoComprehensive Liver Cancer Department, The Fifth Medical Center, Chinese PLA General Hospital, Beijing 100039, People's Republic of China.
Yi-Xin RenKey Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430072, People's Republic of China.
Jian-Chao ChenKey Laboratory of Structure-Based Drug Design and Discovery, Shenyang Pharmaceutical University, Ministry of Education, Shenyang 110016, People's Republic of China.ORCID 0000-0002-8144-939X
Yin-Ying LuComprehensive Liver Cancer Department, The Fifth Medical Center, Chinese PLA General Hospital, Beijing 100039, People's Republic of China.
Heng ZhangKey Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430072, People's Republic of China.
Shuang CaoKey Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430072, People's Republic of China.ORCID 0000-0002-1855-3426
Wuhan Institute of Technology · CNChinese PLA General Hospital · CNNational Institutes for Food and Drug Control · CNShenyang Pharmaceutical University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundRadiotherapy has an ameliorative effect on a wide variety of tumors, but hepatocellular carcinoma (HCC) is insensitive to this treatment. Overactivated mammalian target of rapamycin (mTOR) plays an important part in the resistance of HCC to radiotherapy; thus, mTOR inhibitors have potential as novel radiosensitizers to enhance the efficacy of radiotherapy for HCC.

methodsA lead compound was found based on pharmacophore modeling and molecular docking, and optimized according to the differences between the ATP-binding pockets of mTOR and PI3K. The radiosensitizing effect of the optimized compound (

resultsThe key amino acid residues in mTOR were identified, and a precise virtual screening model was constructed. Compound

conclusionA new class of selective mTOR inhibitors was developed and their radiosensitization effects were confirmed. This study also provides a basis for developing mTOR-specific inhibitors for use as radiosensitizers for HCC radiotherapy.

Indexed as

Carcinoma, HepatocellularCell Line, TumorCell SurvivalDose-Response Relationship, DrugDrug Evaluation, PreclinicalHumansLiver NeoplasmsModels, MolecularMolecular StructurePyrimidinonesRadiation-Sensitizing AgentsStructure-Activity RelationshipTOR Serine-Threonine KinasesMTOR protein, humanPyrimidinonesRadiation-Sensitizing AgentsTOR Serine-Threonine KinasesHCCkinase inhibitormTORradiosensitizervirtual docking

Identifiers

PMID32440103
PMCPMC7220363
OpenAlexW3021873403

What Socratic holds

Textmetadata
LicenceCC BY-NC
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 Socratic graph.