Evidence map›Paper›PMID 36759818›Full record

ArticleCancer cell international2023

In vitro and in vivo analyses on anti-NSCLC activity of apatinib: rediscovery of a new drug target V600E mutation.

Jiani Chen, Jingwen Zhai, Mingming Li, Shiyi Liu, Xiaobin Gong, Hongyu Yu, Hua Wei, Wansheng Chen

Open access · goldAbstract read
In one paragraph

Article in Cancer cell international, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
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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

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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

0 citing papers in PubMed, 0 citations in OpenAlex.

No citing paper in PubMed yet.

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

8 authors at 1 institution in 1 country.

Jiani Chen *Medical Guarantee Center, Second Affiliated Hospital of Naval Medical University, Shanghai, 200003, China.
Jingwen Zhai *Medical Guarantee Center, Second Affiliated Hospital of Naval Medical University, Shanghai, 200003, China.
Mingming Li *Medical Guarantee Center, Second Affiliated Hospital of Naval Medical University, Shanghai, 200003, China.
Shiyi LiuMedical Guarantee Center, Second Affiliated Hospital of Naval Medical University, Shanghai, 200003, China.
Xiaobin GongMedical Guarantee Center, Second Affiliated Hospital of Naval Medical University, Shanghai, 200003, China.
Hongyu YuDepartment of Pathology, Second Affiliated Hospital of Naval Medical University, Shanghai, 200003, China. yuhongyu795@hotmail.com.
Hua WeiMedical Guarantee Center, Second Affiliated Hospital of Naval Medical University, Shanghai, 200003, China. weihua@smmu.edu.cn.
Wansheng ChenMedical Guarantee Center, Second Affiliated Hospital of Naval Medical University, Shanghai, 200003, China. chenwanshengchzh@126.com.
Second Military Medical University · CN

Funding

Clinical Science and Technology Innovation Project of Shanghai Shenkang Hospital Development Center of China SHDC12015120International Scientific and Technological Cooperation Project of China 2015DFA31810National Major Scientific Research Project of China 2015CB931803Shanghai Science and Technology Commission Research Project of China 13DZ1930602
6 · The paper itself

Abstract

backgroundApatinib (YN968D1) is the first small-molecule-targeting drug with anti-tumor activity created in China for the treatment of advanced gastric cancer (GC) and hepatocellular carcinoma (HCC). It showed significant variation in the efficacy for treating cancers, including advanced non-squamous non-small-cell lung cancer (NSCLC). Whether its efficacy could be optimized by subgrouping patients with certain genetic variation remains elusive.

methodsHere, we firstly used kinase screening to identify any possible target of apatinib against 138 kinases. The effects of apatinib on proliferation rates, cell cycle, cell apoptosis, and cell migration on cancer cell lines were analyzed; the in vitro potential pathways of apatinib on cancer cell lines were screened. The effect of apatinib on mouse cancer models in vivo was also analyzed.

resultsBased on HCC364 cells with BRAF V600E mutation, we have shown that apatinib could inhibit their growth, migration, cell cycle, and induce their apoptosis. Based on mice with transplanted HCC364 cells, we have also shown that apatinib could inhibit the tumor growth. Based on immunohistochemistry, we have demonstrated that apatinib could suppress the phosphorylation of mitogen-activated protein kinase/extracellular signal-regulated kinase and extracellular regulated protein kinases. This may account at least part of the apatinib's inhibitory effect on HCC364 cancer cells.

conclusionsBRAF V600E protein kinase is a target of apatinib by kinase screening. We have demonstrated that apatinib can effectively inhibit tumor cells with BRAF V600E mutation by in vitro and in vivo experiments. Our results have demonstrated that targeting BRAF V600E mutation, apatinib appears to be effective and safe for treating NSCLC and possibly other cancers with the same mutation.

Indexed as

ApatinibBRAF V600ECYP2D6CYP3A4HPLC-MS/MSNon-small-cell lung cancer (NSCLC)P-gp

Identifiers

PMID36759818
PMCPMC9909954
OpenAlexW4319742882

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Registered trials

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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.