Evidence map›Paper›PMID 32840532›Full record

ArticleChemical communications (Cambridge, England)2020

Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs.

Yufeng Xiao, Jia Wang, Lisa Y Zhao, Xinyi Chen, Guangrong Zheng, Xuan Zhang, Daiqing Liao

Abstract read
In one paragraph

Article in Chemical communications (Cambridge, England), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.

0numbers the graph read from it
0cells of the map it votes in
53citing 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

53 citing papers in PubMed.

  1. PROTACs in cancer therapy: targeted degradation of GPX4, PARP and epigenetic regulators.Journal of enzyme inhibition and medicinal chemistry · 2026
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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.

Yufeng XiaoDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, 1333 Center Drive, Gainesville, FL 32610, USA. xuan.zhang@cop.ufl.edu.ORCID http://orcid.org/0000-0002-2679-0800
Jia WangDepartment of Anatomy & Cell Biology, College of Medicine, UF Health Cancer Center, University of Florida, 2033 Mowry Road, Gainesville, FL 32610, USA. dliao@ufl.edu and Affiliated Dongzhimen Hospital, Beijing University of Chinses Medicine, Beijing, China and Department of Integrated Traditional and Western Medicine, Affiliated Cancer Hospital of Zhengzhou University, Henan Cancer Hospital, Zhengzhou, China.
Lisa Y ZhaoDepartment of Anatomy & Cell Biology, College of Medicine, UF Health Cancer Center, University of Florida, 2033 Mowry Road, Gainesville, FL 32610, USA. dliao@ufl.edu.
Xinyi ChenAffiliated Dongzhimen Hospital, Beijing University of Chinses Medicine, Beijing, China.
Guangrong ZhengDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, 1333 Center Drive, Gainesville, FL 32610, USA. xuan.zhang@cop.ufl.edu.ORCID http://orcid.org/0000-0002-8106-6663
Xuan ZhangDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, 1333 Center Drive, Gainesville, FL 32610, USA. xuan.zhang@cop.ufl.edu.ORCID http://orcid.org/0000-0001-6062-6708
Daiqing LiaoDepartment of Anatomy & Cell Biology, College of Medicine, UF Health Cancer Center, University of Florida, 2033 Mowry Road, Gainesville, FL 32610, USA. dliao@ufl.edu.ORCID http://orcid.org/0000-0002-2948-2694

Funding

Acquisition of a Q Exactive HF Hybrid Quadrupole-OrbitrapS10OD021758 · OD · UNIVERSITY OF FLORIDA · PI BASSO, KARI B · 2017 to 2017
$600k
NIH HHS S10 OD021758
6 · The paper itself

Abstract

Histone deacetylases (HDACs) are validated drug targets for cancer treatment. Increased HDAC isozyme selectivity and novel strategies to inhibit HDAC activity could lead to safer and more effective drug candidates. Nonetheless, it is quite challenging to develop isozyme-specific HDACi due to the highly conserved catalytic domain. We discovered XZ9002, a first-in-class HDAC3-specific PROTAC that potently degraded HDAC3. Importantly, XZ9002 is more effective to inhibit cancer cell proliferation than its proteolysis-inactive counterpart, suggesting HDAC3 degradation is a novel and promising anticancer approach.

Indexed as

ProteolysisBenzamidesCatalytic DomainCell Line, TumorCell ProliferationHistone Deacetylase 3Histone Deacetylase InhibitorsHistone DeacetylasesHumansProteasome Endopeptidase ComplexUbiquitinUbiquitin-Protein LigasesbenzamideBenzamidesHistone Deacetylase 3Histone Deacetylase InhibitorsHistone DeacetylasesProteasome Endopeptidase ComplexUbiquitinUbiquitin-Protein Ligases

Identifiers

PMID32840532
PMCPMC7654701

What OpenQuestion holds

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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.