Evidence map›Paper›PMID 31289306›Full record

ArticleScientific reports2019

Identification of ryuvidine as a KDM5A inhibitor.

Eishin Mitsui, Shogo Yoshida, Yui Shinoda, Yasumasa Matsumori, Hiroshi Tsujii, Mie Tsuchida, Shuichi Wada, Makoto Hasegawa, Akihiro Ito, Koshiki Mino and 4 more

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
1.4field-weighted citation impact, top 19% 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

19 citing papers in PubMed, 30 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
  4. Article
  5. Article
  6. Review
  7. Lysine and arginine methylation of transcription factors.Cellular and molecular life sciences : CMLS · 2024
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  8. Epigenetics-targeted drugs: current paradigms and future challenges.Signal transduction and targeted therapy · 2024
    Review
  9. Article
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  11. Article
  12. Article
  13. Review
  14. Article
  15. JMJD family proteins in cancer and inflammation.Signal transduction and targeted therapy · 2022
    Review
  16. Article
  17. Article
  18. The emerging role of KDM5A in human cancer.Journal of hematology & oncology · 2021
    Review
  19. 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

14 authors at 3 institutions in 1 country.

Eishin MitsuiNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.ORCID http://orcid.org/0000-0003-0948-3152
Shogo YoshidaNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Yui ShinodaNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Yasumasa MatsumoriNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Hiroshi TsujiiNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Mie TsuchidaNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Shuichi WadaNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Makoto HasegawaNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Akihiro ItoSch. of Life Sci., Tokyo Univ. of Pharm. & Life Sci., 1432-1 Horinouchi, Hachioji, Tokyo, 192-0392, Japan.
Koshiki MinoNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Tetsuo OnukiDrug Discov. Seed Cpds. Explorat. Unit, RIKEN CSRS, 2-1 Hirosawa, Wako, Saitama, 351-0198, Japan.
Minoru YoshidaChem. Genomics, RIKEN CSRS, 2-1 Hirosawa, Wako, Saitama, 351-0198, Japan.ORCID http://orcid.org/0000-0002-4376-5674
Ryuzo SasakiNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan.
Tamio MizukamiNagahama Inst. Bio-Sci. & Tech., 1266 Tamura, Nagahama, Shiga, 526-0829, Japan. mizukami@nagahama-i-bio.ac.jp.
Nagahama Institute of Bio-Science and Technology · JPRIKEN · JPTokyo University of Pharmacy and Life Sciences · JP

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

KDM5 family members (A, B, C and D) that demethylate H3K4me3 have been shown to be involved in human cancers. Here we performed screening for KDM5A inhibitors from chemical libraries using the AlphaScreen method and identified a battery of screening hits that inhibited recombinant KDM5A. These compounds were further subjected to cell-based screening using a reporter gene that responded to KDM5A inhibition and 6 compounds were obtained as candidate inhibitors. When further confirmation of their inhibition activity on cellular KDM5A was made by immunostaining H3K4me3 in KDM5A-overexpressing cells, ryuvidine clearly repressed H3K4me3 demethylation. Ryuvidine prevented generation of gefitinib-tolerant human small-cell lung cancer PC9 cells and also inhibited the growth of the drug-tolerant cells at concentrations that did not affect the growth of parental PC9 cells. Ryuvidine inhibited not only KDM5A but also recombinant KDM5B and C; KDM5B was the most sensitive to the inhibitor. These results warrant that ryuvidine may serve as a lead compound for KDM5 targeted therapeutics.

Indexed as

Antineoplastic AgentsCarcinoma, Non-Small-Cell LungEnzyme InhibitorsHigh-Throughput Screening AssaysHumansLung NeoplasmsRetinoblastoma-Binding Protein 2Small Molecule LibrariesTumor Cells, CulturedAntineoplastic AgentsEnzyme InhibitorsKDM5A protein, humanRetinoblastoma-Binding Protein 2Small Molecule Libraries

Identifiers

PMID31289306
PMCPMC6616564
OpenAlexW2960931117

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.