Evidence map›Paper›PMID 24131029›Full record

ArticleJournal of medicinal chemistry2013

Triazole-dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration.

Yi-Chao Zheng, Ying-Chao Duan, Jin-Lian Ma, Rui-Min Xu, Xiaolin Zi, Wen-Lei Lv, Meng-Meng Wang, Xian-Wei Ye, Shun Zhu, David Mobley and 6 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 73 papers.

0numbers the graph read from it
0cells of the map it votes in
73citing papers in PubMed
7.9field-weighted citation impact, top 2% 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

73 citing papers in PubMed, 217 citations in OpenAlex.

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  18. Discovery of novel sulphonamide hybrids that inhibit LSD1 against bladder cancer cells.Journal of enzyme inhibition and medicinal chemistry · 2022
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13 more citing papers are in PubMed but not listed here.

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

16 authors at 2 institutions in 2 countries.

Yi-Chao Zheng *School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Ying-Chao Duan *School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Jin-Lian MaSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Rui-Min XuSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Xiaolin ZiDepartments of Urology, Pharmacology and Pharmaceutical Sciences, University of California, Irvine, Orange, USA.
Wen-Lei LvSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Meng-Meng WangSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Xian-Wei YeSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Shun ZhuDepartment of Pharmaceutical Sciences, University of California, Irvine, USA.
David MobleyDepartment of Pharmaceutical Sciences, University of California, Irvine, USA.
Yan-Yan ZhuThe College of Chemistry and Molecular Engineering, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Jun-Wei WangSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Jin-Feng LiSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Zhi-Ru WangSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Wen ZhaoSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Hong-Min LiuSchool of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China; New Drug Research & Development Center, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Zhengzhou University · CNUniversity of California, Irvine · US

Funding

Chemoprevention of urinary bladder carcinogenesis by flavokawain AR01CA122558 · NCI · UNIVERSITY OF CALIFORNIA-IRVINE · PI ZI, XIAOLIN · 2008 to 2012
$1.7M
NCI NIH HHS R01 CA122558
6 · The paper itself

Abstract

Lysine specific demethylase 1 (LSD1), the first identified histone demethylase, plays an important role in epigenetic regulation of gene activation and repression. The up-regulated LSD1's expression has been reported in several malignant tumors. In the current study, we designed and synthesized five series of 1,2,3-triazole-dithiocarbamate hybrids and screened their inhibitory activity toward LSD1. We found that some of these compounds, especially compound 26, exhibited the most specific and robust inhibition of LSD1. Interestingly, compound 26 also showed potent and selective cytotoxicity against LSD1 overexpressing gastric cancer cell lines MGC-803 and HGC-27, as well as marked inhibition of cell migration and invasion, compared to 2-PCPA. Furthermore, compound 26 effectively reduced the tumor growth bared by human gastric cancer cells in vivo with no signs of adverse side effects. These findings suggested that compound 26 deserves further investigation as a lead compound in the treatment of LSD1 overexpressing gastric cancer.

Indexed as

AnimalsAntineoplastic AgentsApoptosisCell Line, TumorCell MovementCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorEnzyme InhibitorsHistone DemethylasesHumansMiceMice, Inbred BALB CModels, MolecularMolecular Dynamics SimulationMolecular StructureAntineoplastic AgentsEnzyme InhibitorsHistone DemethylasesKDM1A protein, humanThiocarbamatesTriazoles

Identifiers

PMID24131029
PMCPMC3881423
OpenAlexW2396035051

What OpenQuestion holds

Textmetadata
LicenceTDM
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.