Evidence map›Paper›PMID 38746900›Full record

ArticleACS medicinal chemistry letters2024

Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders.

Jian Chen, Wentao Zhu, Wenqian Zhang, Yichen Tong, Fang Xu, Jiyan Pang

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS medicinal chemistry letters, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

6 authors.

Jian ChenSchool of Chemistry, Sun Yat-sen University, Guangzhou 510275, China.
Wentao ZhuSchool of Chemistry, Sun Yat-sen University, Guangzhou 510275, China.ORCID https://orcid.org/0000-0003-0433-5935
Wenqian ZhangSchool of Chemistry, Sun Yat-sen University, Guangzhou 510275, China.
Yichen TongSchool of Chemistry, Sun Yat-sen University, Guangzhou 510275, China.ORCID https://orcid.org/0000-0001-8561-0526
Fang XuInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization & Innovative Drug Development of Chinese Ministry of Education (MOE) and Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, Guangzhou 510632, China.ORCID https://orcid.org/0000-0002-0895-3071
Jiyan PangSchool of Chemistry, Sun Yat-sen University, Guangzhou 510275, China.ORCID https://orcid.org/0000-0003-0330-2808

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) has been identified as a promising oncogenic driver of several types of cancer and is considered to be a critical cancer therapeutic target. Several inhibitors of DYRK2 have been reported, but no degraders have been found yet. In this work, we designed and synthesized the first series of proteolysis-targeting chimeras (PROTACs) using curcumin and its analogs as warheads to target and degrade DYRK2. The results of degradation assays showed that the compound

Identifiers

PMID38746900
PMCPMC11089551

What OpenQuestion holds

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Registered trials

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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.