CRBN‐PROTACs in Cancer Therapy: From Mechanistic Insights to Clinical Applications

Chemical Biology & Drug Design, Год журнала: 2024, Номер 104(5)

Опубликована: Ноя. 1, 2024

Cereblon (CRBN), a member of the E3 ubiquitin ligase complex, has gained significant attention as therapeutic target in cancer. CRBN regulates degradation various proteins cancer progression, including transcription factors and signaling molecules. PROTACs (proteolysis-targeting chimeras) are novel approach that uses cell's system to remove disease-causing selectively. CRBN-dependent work by tagging harmful for destruction through ubiquitin-proteasome system. This strategy offers several advantages over traditional protein inhibition methods, potential overcome drug resistance. Recent progress developing CRBN-based shown promising preclinical results both hematologic malignancies solid tumors. Additionally, have enhanced our understanding CRBN's role cancer, potentially serving biomarkers patient stratification predicting responses. In this review, we delineate mechanisms action (CRBN-PROTACs), summarize recent advances clinical applications, provide perspective on future development.

Язык: Английский

Protacs in cancer therapy: mechanisms, design, clinical trials, and future directions

Drug Delivery and Translational Research, Год журнала: 2024, Номер unknown

Опубликована: Ноя. 29, 2024

Язык: Английский

Computational strategies for the design of proteolysis targeting chimera degraders: Artificial intelligence enabled PROTAC design

Annual reports in medicinal chemistry, Год журнала: 2024, Номер unknown

Опубликована: Янв. 1, 2024

Язык: Английский