Work

The clinical advances of proteolysis targeting chimeras in oncology

Year: 2021

Type: review

Abstract: Proteolysis targeting chimeras (PROTACs) are a class of small molecules designed to target proteins for degradation. Their novel and unique modes of action provide PROTACs with the potential for their application in the management of both solid and hematologic malignancies. Since its initial discovery, the technology of targeted protein degradation, especially in the form of PROTACs, has had significant advances. A number of PROTACs have entered a late stage of preclinical development. Several of them are either in phase 1/2 clinical trials or approaching approval for initial clinical evaluation. This article discusses the preclinical and clinical findings of PROTACs of clinically relevant protein targets in cancer.

Source: Exploration of Targeted Anti-tumor Therapy

DOI: 10.37349/etat.2021.00061

Authors: Hao Xie, Junjia Liu, Diego M. Alem Glison, Jason B. Fleming

Institutions: Moffitt Cancer Center, Albert Einstein College of Medicine

Language: English

Topic: Protein Degradation and Inhibitors

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: diamond

Funder: Moffitt Cancer Center