Application of PROTACs in Hematological Malignancies--Review.
10.19746/j.cnki.issn.1009-2137.2023.06.051
- Author:
Yan-Nan JIA
1
;
Ying-Chang MI
2
Author Information
1. Institute of Hematology & Blood Diseases Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College, State Key Laboratory of Experimental Hematology, National Clinical Research Center for Blood Diseases, Haihe Laboratory of Cell Ecosystem, Tianjin 300020, China.
2. Institute of Hematology & Blood Diseases Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College, State Key Laboratory of Experimental Hematology, National Clinical Research Center for Blood Diseases, Haihe Laboratory of Cell Ecosystem, Tianjin 300020, China.E-mail: miyingch@126.com.
- Publication Type:Journal Article
- Keywords:
hematological malignancies;
proteasome system;
proteolysis-targeting chimera;
target
- MeSH:
Humans;
Hematologic Neoplasms/drug therapy*;
Proteasome Endopeptidase Complex/metabolism*;
Ubiquitin-Protein Ligases/metabolism*;
Proteolysis Targeting Chimera
- From:
Journal of Experimental Hematology
2023;31(6):1921-1924
- CountryChina
- Language:Chinese
-
Abstract:
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional small molecules by utilizing the ubiquitin proteasome system (UPS) to degrade proteins of interest. PROTACs have exhibited unprecedented efficacy and specificity in degrading various oncogenic proteins because of their unique mechanism of action, ability to target "undruggable" and mutant proteins. A series of PROTACs have been developed to degrade multiple key protein targets for the treatment of hematologic malignancy. Notably, PROTACs that target BCL-XL, IRAK4, STAT3 and BTK have entered clinical trials. The known PROTACs that have the potential to be used to treat various hematological malignancies are systematically summarized in this review.
