Evidence map›Paper›PMID 32718354›Full record

ReviewJournal of hematology & oncology2020

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies.

Yonghan He, Sajid Khan, Zhiguang Huo, Dongwen Lv, Xuan Zhang, Xingui Liu, Yaxia Yuan, Robert Hromas, Mingjiang Xu, Guangrong Zheng and 1 more

Open access · goldAbstract readReview
In one paragraph

Review in Journal of hematology & oncology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 62 papers.

0numbers the graph read from it
0cells of the map it votes in
62citing papers in PubMed
5.4field-weighted citation impact, top 3% 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

62 citing papers in PubMed, 114 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
  4. Review
  5. Article
  6. Review
  7. Review
  8. Article
  9. Article
  10. Review
  11. Article
  12. Review
  13. Review
  14. Article
  15. Article
  16. Article
  17. Article
  18. Article
  19. Influence of Nucleophosmin (Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2025
    Article
  20. Article

2 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

11 authors at 2 institutions in 1 country.

Yonghan HeDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Sajid KhanDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Zhiguang HuoDepartment of Biostatistics, College of Public Health & Health Professions and College of Medicine, University of Florida, Gainesville, FL, USA.
Dongwen LvDepartment 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.
Xingui LiuDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Yaxia YuanDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Robert HromasDepartment of Medicine, The University of Texas Health Science Center at San Antonio, San Antonio, TX, USA.
Mingjiang XuDepartment of Molecular Medicine, College of Medicine, The University of Texas Health Science Center at San Antonio, San Antonio, TX, USA.
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 0000-0002-2400-6461
University of Florida · USThe University of Texas Health Science Center at San Antonio · US

Funding

Inhibition of Bcl-xL by Targeted DegradationR01CA241191 · NCI · UNIVERSITY OF FLORIDA · PI KONOPLEVA, MARINA Y, ZHENG, GUANGRONG · 2020 to 2024
$2.6M
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 CA241191NCI NIH HHS R01 CA242003NCI NIH HHS R21 CA223371NIH HHS R01CA211963NIH HHS R01CA219836NIH HHS R01CA241191NIH HHS R01CA242003NIH HHS R21CA223371
6 · The paper itself

Abstract

Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI). PROTACs are potentially superior to conventional small molecule inhibitors (SMIs) because of their unique mechanism of action (MOA, i.e., degrading POI in a sub-stoichiometric manner), ability to target "undruggable" and mutant proteins, and improved target selectivity. Therefore, PROTACs have become an emerging technology for the development of novel targeted anticancer therapeutics. In fact, some of these reported PROTACs exhibit unprecedented efficacy and specificity in degrading various oncogenic proteins and have advanced to various stages of preclinical and clinical development for the treatment of cancer and hematologic malignancy. In this review, we systematically summarize the known PROTACs that have the potential to be used to treat various hematologic malignancies and discuss strategies to improve the safety of PROTACs for clinical application. Particularly, we propose to use the latest human pan-tissue single-cell RNA sequencing data to identify hematopoietic cell type-specific/selective E3 ligases to generate tumor-specific/selective PROTACs. These PROTACs have the potential to become safer therapeutics for hematologic malignancies because they can overcome some of the on-target toxicities of SMIs and PROTACs.

Indexed as

LigandsAnimalsClinical Trials as TopicHumansLeukemiaLymphomaMolecular Targeted TherapyMultiple MyelomaNeoplasm ProteinsNeoplasmsOrgan SpecificityProteasome Endopeptidase ComplexProtein Processing, Post-TranslationalProteolysisRecombinant ProteinsUbiquitinLigandsNeoplasm ProteinsProteasome Endopeptidase ComplexRecombinant ProteinsUbiquitinUbiquitin-Conjugating EnzymesUbiquitin-Protein LigasesCell-specific E3 ligasesHematologic malignancyPROTACSmall molecule inhibitor

Identifiers

PMID32718354
PMCPMC7384229
OpenAlexW3044807330

What OpenQuestion holds

Textmetadata
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.