Evidence map›Paper›PMID 30237400›Full record

ArticleExperimental & molecular medicine2018

HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis.

Han-Hee Park, Se-Yeon Park, Shinmee Mah, Jung-Hee Park, Soon-Sun Hong, Sungwoo Hong, You-Sun Kim

Open access · goldAbstract read
In one paragraph

Article in Experimental & molecular medicine, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.

0numbers the graph read from it
0cells of the map it votes in
33citing papers in PubMed
6.2field-weighted citation impact, top 3% 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

33 citing papers in PubMed, 103 citations in OpenAlex.

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  15. Role of Necroptosis in Intervertebral Disc Degeneration.International journal of molecular sciences · 2023
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  19. Necroptosis: A Pathogenic Negotiator in Human Diseases.International journal of molecular sciences · 2022
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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

7 authors at 5 institutions in 1 country.

Han-Hee Park *Department of Biochemistry, Ajou University School of Medicine, Suwon, Korea.
Se-Yeon Park *Department of Biochemistry, Ajou University School of Medicine, Suwon, Korea.
Shinmee MahCenter for Catalytic Hydrocarbon Functionalizations, Institute for Basic Science (IBS), Daejeon, 34141, Korea.
Jung-Hee ParkDepartment of Biomedical Sciences, College of Medicine, Inha University, Incheon, 22332, Korea.
Soon-Sun HongDepartment of Biomedical Sciences, College of Medicine, Inha University, Incheon, 22332, Korea. hongs@inha.ac.kr.
Sungwoo HongCenter for Catalytic Hydrocarbon Functionalizations, Institute for Basic Science (IBS), Daejeon, 34141, Korea. hongorg@kaist.ac.kr.
You-Sun KimDepartment of Biochemistry, Ajou University School of Medicine, Suwon, Korea. yousunkim@ajou.ac.kr.
Ajou University · KRInha University · KRInstitute for Basic Science · KRKorea Advanced Institute of Science and Technology · KRUniversity of Suwon · KR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Necroptosis is a type of programmed cell death that usually occurs under apoptosis-deficient conditions. Receptor-interacting protein kinase-3 (RIP3, or RIPK3) is a central player in necroptosis, and its kinase activity is essential for downstream necroptotic signaling events. Since RIP3 kinase activity has been associated with various diseases, the development of specific RIP3 inhibitors is an attractive strategy for therapeutic application. In this study, we identified a potent RIP3 inhibitor, HS-1371, by the extensive screening of chemical libraries focused on kinases. HS-1371 directly binds to RIP3 in an ATP-competitive and time-independent manner, providing a mechanism of action. Moreover, the compound inhibited TNF-induced necroptosis but did not inhibit TNF-induced apoptosis, indicating that this novel inhibitor has a specific inhibitory effect on RIP3-mediated necroptosis via the suppression of RIP3 kinase activity. Our results suggest that HS-1371 could serve as a potential preventive or therapeutic agent for diseases involving RIP3 hyperactivation.

Indexed as

AnimalsApoptosisCell LineCytoprotectionHumansMiceNecrosisPhosphorylationPhosphoserinePiperidinesProtein Kinase InhibitorsPyrazolesQuinolinesReceptor-Interacting Protein Serine-Threonine KinasesTumor Necrosis Factor-alphaPhosphoserinePiperidinesProtein Kinase InhibitorsPyrazolesQuinolinesReceptor-Interacting Protein Serine-Threonine KinasesRIPK3 protein, humanTumor Necrosis Factor-alpha

Identifiers

PMID30237400
PMCPMC6148246
OpenAlexW2885340691

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.