Evidence map›Paper›PMID 38687638›Full record

ArticleJournal of medicinal chemistry2024

Discovery of LLC0424 as a Potent and Selective

Lianchao Liu, Abhijit Parolia, Yihan Liu, Caiyun Hou, Tongchen He, Yuanyuan Qiao, Sanjana Eyunni, Jie Luo, Chungen Li, Yongxing Wang and 6 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
–field-weighted citation impact
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

8 citing papers in PubMed.

  1. Review
  2. Article
  3. Review
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  8. Review
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.

Lianchao LiuState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, no. 345 Lingling Road., Shanghai 200032, People's Republic of China.
Abhijit ParoliaMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Yihan LiuMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Caiyun HouInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou 511400, People's Republic of China.
Tongchen HeMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Yuanyuan QiaoMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Sanjana EyunniMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Jie LuoMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Chungen LiState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, no. 345 Lingling Road., Shanghai 200032, People's Republic of China.
Yongxing WangLivzon Research Institute, Livzon Pharmaceutical Group Inc., no. 38 Chuangye North Road, Jinwan District, Zhuhai 519000, China.
Fengtao ZhouInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou 511400, People's Republic of China.ORCID 0000-0003-2518-7855
Weixue HuangState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, no. 345 Lingling Road., Shanghai 200032, People's Republic of China.
Xiaomei RenState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, no. 345 Lingling Road., Shanghai 200032, People's Republic of China.
Zhen WangState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, no. 345 Lingling Road., Shanghai 200032, People's Republic of China.ORCID 0000-0001-8762-6089
Arul M ChinnaiyanMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Ke DingState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, no. 345 Lingling Road., Shanghai 200032, People's Republic of China.ORCID 0000-0001-9016-812X

Funding

Exploring Precision Oncology: From Gene Fusions to lncRNAsR35CA231996 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI CHINNAIYAN, ARUL M · 2018 to 2024
$6.4M
Howard Hughes Medical InstituteNCI NIH HHS R35 CA231996
6 · The paper itself

Abstract

Nuclear receptor-binding SET domain-containing 2 (NSD2), a methyltransferase that primarily installs the dimethyl mark on lysine 36 of histone 3 (H3K36me2), has been recognized as a promising therapeutic target against cancer. However, existing NSD2 inhibitors suffer from low activity or inferior selectivity, and none of them can simultaneously remove the methyltransferase activity and chromatin binding function of NSD2. Herein we report the discovery of a novel NSD2 degrader

Indexed as

Histone-Lysine N-MethyltransferaseProteolysisAdaptor Proteins, Signal TransducingAnimalsAntineoplastic AgentsCell Line, TumorCell ProliferationDrug DiscoveryHistonesHumansMiceProteasome Endopeptidase ComplexRepressor ProteinsStructure-Activity RelationshipUbiquitin-Protein LigasesAdaptor Proteins, Signal TransducingAntineoplastic AgentsCRBN protein, humanHistone-Lysine N-MethyltransferaseHistonesNSD2 protein, humanProteasome Endopeptidase ComplexRepressor ProteinsUbiquitin-Protein Ligases

Identifiers

PMID38687638
PMCPMC11094793

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.