Evidence map›Paper›PMID 28570563›Full record

ArticlePloS one2017

A natural product-like JAK2/STAT3 inhibitor induces apoptosis of malignant melanoma cells.

Ke-Jia Wu, Jie-Min Huang, Hai-Jing Zhong, Zhen-Zhen Dong, Kasipandi Vellaisamy, Jin-Jian Lu, Xiu-Ping Chen, Pauline Chiu, Daniel W J Kwong, Quan-Bin Han and 2 more

Open access · goldAbstract read
In one paragraph

Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed
3.3field-weighted citation impact, top 6% 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

22 citing papers in PubMed, 48 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Article
  5. Review
  6. Review
  7. Natural Nrf2 Inhibitors: A Review of Their Potential for Cancer Treatment.International journal of biological sciences · 2023
    Review
  8. Article
  9. Article
  10. Review
  11. Article
  12. Article
  13. Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. Article
  19. Article
  20. 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

12 authors at 3 institutions in 3 countries.

Ke-Jia WuState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.
Jie-Min HuangState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.
Hai-Jing ZhongState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.
Zhen-Zhen DongDepartment of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China.
Kasipandi VellaisamyDepartment of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China.
Jin-Jian LuState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.
Xiu-Ping ChenState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.
Pauline ChiuDepartment of Chemistry, The University of Hong Kong, Hong Kong, China.
Daniel W J KwongDepartment of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China.
Quan-Bin HanSchool of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China.
Dik-Lung MaDepartment of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China.
Chung-Hang LeungState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.ORCID http://orcid.org/0000-0003-2988-3786
University of Macau · MOHong Kong Baptist University · HKState Key Laboratory of Synthetic Chemistry · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The JAK2/STAT3 signaling pathway plays a critical role in tumorigenesis, and has been suggested as a potential molecular target for anti-melanoma therapeutics. However, few JAK2 inhibitors were being tested for melanoma therapy. In this study, eight amentoflavone analogues were evaluated for their activity against human malignant melanoma cells. The most potent analogue, compound 1, inhibited the phosphorylation of JAK2 and STAT3 in human melanoma cells, but had no discernible effect on total JAK2 and STAT3 levels. A cellular thermal shift assay was performed to identify that JAK2 is engaged by 1 in cell lysates. Moreover, compound 1 showed higher antiproliferative activity against human melanoma A375 cells compared to a panel of cancer and normal cell lines. Compound 1 also activated caspase-3 and cleaved PARP, which are markers of apoptosis, and suppressed the anti-apoptotic Bcl-2 level. Finally, compound 1 induced apoptosis in 80% of treated melanoma cells. To our knowledge, compound 1 is the first amentoflavone-based JAK2 inhibitor to be investigated for use as an anti-melanoma agent.

Indexed as

ApoptosisBiological ProductsCell Line, TumorHumansJanus Kinase 2MelanomaSTAT3 Transcription FactorBiological ProductsJAK2 protein, humanJanus Kinase 2STAT3 protein, humanSTAT3 Transcription Factor

Identifiers

PMID28570563
PMCPMC5453690
OpenAlexW2621086963

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.