Protein degradation technology: a strategic paradigm shift in drug discovery.

ABSTRACT: Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely used strategy for treating malignant tumors. However, most intracellular proteins have been proven to be undruggable due to a lack of active sites, leading to a significant challenge in the design and development of SMIs. In recent years, the proteolysis-targeting chimeric technology and related emerging degradation technologies have provided additional approaches for targeting these undruggable proteins. These degradation technologies show a tendency of superiority over SMIs, including the rapid and continuous target consumption as well as the stronger pharmacological effects, being a hot topic in current research. This review mainly focuses on summarizing the development of protein degradation technol

SUBMITTER: Li H 

PROVIDER: S-EPMC8419833 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature