Evidence map›Paper›PMID 39388374›Full record

ArticleJournal of medicinal chemistry2024

Discovery of ZLC491 as a Potent, Selective, and Orally Bioavailable CDK12/13 PROTAC Degrader.

Licheng Zhou, Kaijie Zhou, Yu Chang, Jianzhang Yang, Bohai Fan, Yuhan Su, Zilu Li, Rahul Mannan, Somnath Mahapatra, Ming Ding and 9 more

Abstract read
PubMed Full text at PMC Publisher
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. CDK12 and CDK13 in oncology: from RNA regulation to therapeutic targeting.Cellular oncology (Dordrecht, Netherlands) · 2026
    Review
  3. Review
  4. Review
  5. Review
  6. Article
  7. Discovery ofJournal of medicinal chemistry · 2025
    Article
  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

19 authors.

Licheng 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, China.
Kaijie ZhouState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Yu ChangMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Jianzhang YangInternational 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, China.
Bohai FanState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Yuhan SuState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Zilu LiState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Rahul MannanMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Somnath MahapatraMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Ming DingSchool of Life Science and Technology, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, 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, China.ORCID 0000-0003-2518-7855
Weixue HuangState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Xiaomei RenState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Jian XuLivzon Research Institute, Livzon Pharmaceutical Group Inc., No. 38, Chuangye North Road, Jinwan District, Zhuhai 519000, China.
George Xiaoju WangMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Jinwei ZhangState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Zhen WangState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.ORCID 0000-0001-8762-6089
Arul M ChinnaiyanMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Ke DingInternational 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, China.ORCID 0000-0001-9016-812X

Funding

Tissue/InformaticsP50CA186786 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI Ganesh S Palapattu · 2014 to 2026
$27.6M
Exploring Precision Oncology: From Gene Fusions to lncRNAsR35CA231996 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI CHINNAIYAN, ARUL M · 2018 to 2024
$6.4M
NCI NIH HHS P50 CA186786NCI NIH HHS R35 CA231996
6 · The paper itself

Abstract

Selective degradation of cyclin-dependent kinases 12 and 13 (CDK12/13) emerges as a new potential therapeutic approach for triple-negative breast cancer (TNBC) and other human cancers. While several proteolysis-targeting chimera (PROTAC) degraders of CDK12/13 were reported, none are orally bioavailable. Here, we report the discovery of

Indexed as

Antineoplastic AgentsBiological AvailabilityCyclin-Dependent KinasesProteolysisAdministration, OralAnimalsCDC2 Protein KinaseCell Line, TumorCell ProliferationDrug DiscoveryFemaleHumansMiceMice, NudeRatsRats, Sprague-DawleyAntineoplastic AgentsCDC2 Protein KinaseCDK12 protein, humanCDK13 protein, humanCyclin-Dependent Kinases

Identifiers

PMID39388374
PMCPMC11513923

What OpenQuestion holds

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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.