Evidence map›Paper›PMID 32475992›Full record

ReviewOncogene2020

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics.

Sajid Khan, Yonghan He, Xuan Zhang, Yaxia Yuan, Shaoyan Pu, Qingpeng Kong, Guangrong Zheng, Daohong Zhou

Open access · greenAbstract readReview
In one paragraph

Review in Oncogene, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 108 papers.

0numbers the graph read from it
0cells of the map it votes in
108citing papers in PubMed
12.5field-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

108 citing papers in PubMed, 232 citations in OpenAlex.

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  20. F-box in breast cancer: mechanism of action and therapeutic potential.American journal of translational research · 2025
    Review

48 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

8 authors at 2 institutions in 2 countries.

Sajid Khan *Department of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, FL, USA.ORCID http://orcid.org/0000-0003-1331-8846
Yonghan He *Department of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Xuan ZhangDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL, USA.ORCID http://orcid.org/0000-0001-6062-6708
Yaxia YuanDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Shaoyan PuState Key Laboratory of Genetic Resources and Evolution, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China.
Qingpeng KongState Key Laboratory of Genetic Resources and Evolution, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China.ORCID http://orcid.org/0000-0002-6046-4494
Guangrong ZhengDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Daohong ZhouDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, FL, USA. zhoudaohong@cop.ufl.edu.ORCID http://orcid.org/0000-0002-2400-6461
University of Florida · USKunming Institute of Zoology · CN

Funding

Use of BCL-xL Proteolysis targeting chimeras to treat pancreatic cancerR01CA242003 · NCI · UNIVERSITY OF FLORIDA · PI TREVINO, JOSE G., ZHENG, GUANGRONG · 2019 to 2023
$2.6M
Role of Senescent Cells in Radiation-induced Pulmonary FibrosisR01CA219836 · NCI · UNIV OF ARKANSAS FOR MED SCIS · PI ZHOU, DAOHONG · 2017 to 2021
$1.8M
Ionizing radiation induced hematological malignanciesR01CA211963 · NCI · UNIV OF ARKANSAS FOR MED SCIS · PI ZHOU, DAOHONG · 2017 to 2021
$1.8M
NCI Clinical and Translational Exploratory/ Developmental StudiesR21CA223371 · NCI · UNIVERSITY OF FLORIDA · PI ZHENG, GUANGRONG · 2018 to 2019
$359k
NCI NIH HHS R01 CA211963NCI NIH HHS R01 CA219836NCI NIH HHS R01 CA242003NCI NIH HHS R21 CA223371
6 · The paper itself

Abstract

Using PROteolysis TArgeting Chimeras (PROTACs) to degrade proteins that are important for tumorigenesis has emerged as a potential therapeutic strategy for cancer. PROTACs are heterobifunctional molecules consisting of one ligand for binding to a protein of interest (POI) and another to an E3 ubiquitin (E3) ligase, connected via a linker. PROTACs recruit the E3 ligase to the POI and cause proximity-induced ubiquitination and degradation of the POI by the ubiquitin-proteasome system (UPS). PROTACs have been developed to degrade a variety of cancer targets with unprecedented efficacy against a multitude of tumor types. To date, most of the PROTACs developed have utilized ligands to recruit E3 ligases that are ubiquitously expressed in both tumor and normal tissues. These PROTACs can cause on-target toxicities if the POIs are not tumor-specific. Therefore, identifying and recruiting the E3 ligases that are enriched in tumors with minimal expression in normal tissues holds the potential to develop tumor-specific/selective PROTACs. In this review, we will discuss the potential of PROTACs to become anticancer therapeutics, chemical and bioinformatics approaches for PROTAC design, and safety concerns with a special focus on the development of tumor-specific/selective PROTACs. In addition, the identification of tumor types in terms of solid versus hematological malignancies that can be best targeted with PROTAC approach will be briefly discussed.

Indexed as

Antineoplastic AgentsCarcinogenesisDrug DiscoveryHumansNeoplasmsProteasome Endopeptidase ComplexProtein BindingProteinsProteolysisUbiquitin-Protein LigasesAntineoplastic AgentsProteasome Endopeptidase ComplexProteinsUbiquitin-Protein Ligases

Identifiers

PMID32475992
PMCPMC7319888
OpenAlexW3031903798

What OpenQuestion holds

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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.