Evidence map›Paper›PMID 31330105›Full record

ArticleJournal of medicinal chemistry2019

Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders.

Shang Su, Zimo Yang, Hongying Gao, Haiyan Yang, Songbiao Zhu, Zixuan An, Juanjuan Wang, Qing Li, Sarat Chandarlapaty, Haiteng Deng and 2 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 89 papers.

0numbers the graph read from it
0cells of the map it votes in
89citing papers in PubMed
9.8field-weighted citation impact, top 1% 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

89 citing papers in PubMed, 186 citations in OpenAlex.

  1. Next-generation CDK inhibitors in HR+/HER2- breast cancer.The Journal of clinical investigation · 2026
    Review
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  12. FDA-approved kinase inhibitors in PROTAC design, development and synthesis.Journal of enzyme inhibition and medicinal chemistry · 2025
    Review
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  14. Article
  15. Review
  16. Article
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  18. Article
  19. Review
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29 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

12 authors at 2 institutions in 2 countries.

Shang SuMOE Key Laboratory of Protein Sciences, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.ORCID 0000-0003-0228-5380
Zimo YangMOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology , Tsinghua University , Beijing 100084 , P. R. China.
Hongying GaoMOE Key Laboratory of Protein Sciences, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.
Haiyan YangMOE Key Laboratory of Protein Sciences, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.
Songbiao ZhuMOE Key Laboratory of Bioinformatics, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.
Zixuan AnMOE Key Laboratory of Protein Sciences, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.
Juanjuan WangMOE Key Laboratory of Protein Sciences, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.
Qing LiHuman Oncology and Pathogenesis Program , Memorial Sloan Kettering Cancer Center (MSKCC) , New York , New York 10065 , United States.
Sarat ChandarlapatyHuman Oncology and Pathogenesis Program , Memorial Sloan Kettering Cancer Center (MSKCC) , New York , New York 10065 , United States.
Haiteng DengMOE Key Laboratory of Bioinformatics, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.
Wei WuMOE Key Laboratory of Protein Sciences, School of Life Sciences , Tsinghua University , Beijing 100084 , P. R. China.
Yu RaoMOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology , Tsinghua University , Beijing 100084 , P. R. China.ORCID 0000-0002-4356-8531
Tsinghua University · CNMemorial Sloan Kettering Cancer Center · US

Funding

X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI Nicholas D Socci · 1985 to 2026
$347.4M
NCI NIH HHS P30 CA008748
6 · The paper itself

Abstract

A focused PROTAC library hijacking cancer therapeutic target CDK6 was developed. A design principle as "match/mismatch" was proposed for understanding the degradation profile differences in these PROTACs. Notably, potent PROTACs with specific and remarkable CDK6 degradation potential were generated by linking CDK6 inhibitor palbociclib and E3 ligase CRBN recruiter pomalidomide. The PROTAC strongly inhibited proliferation of hematopoietic cancer cells including multiple myeloma and robustly degraded copy-amplified/mutated forms of CDK6, indicating future potential clinical applications.

Indexed as

Angiogenesis InhibitorsCell Line, TumorCell ProliferationCyclin-Dependent Kinase 6Hematologic NeoplasmsHL-60 CellsHumansMolecular StructurePiperazinesProtein Kinase InhibitorsProteolysisPyridinesSmall Molecule LibrariesThalidomideTHP-1 CellsUbiquitin-Protein LigasesAngiogenesis InhibitorsCDK6 protein, humanCyclin-Dependent Kinase 6palbociclibPiperazinespomalidomideProtein Kinase InhibitorsPyridinesSmall Molecule LibrariesThalidomideUbiquitin-Protein Ligases

Identifiers

PMID31330105
PMCPMC6790125
OpenAlexW2963581652

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.