Cancer is one the major causes of morbidity and mortality around the world. Cancer cells self-replicate and divide without any external stimulus and with metastatic properties. Various treatment options are available, such as chemotherapy, nanomedicines, etc, however such therapies do not specifically target cancer cells but also damage normal growing cells.
Proteolysis-targeting chimeras (PROTACs) can be used as a targeted treatment option for cancer. PROTACs are specific, versatile, and biologically active small molecules, able to induce selective intracellular proteolysis, which can be used for targeted degradation of proteins promoting tumorigenesis. PROTACs initiate the degradation process by recruiting the E3 ubiquitin ligase to the target protein, resulting into polyubiquitination of the protein of interest and its consequent degradation by 26S proteasome, a component of the ubiquitin-proteasome system (UPS) within eukaryotic cells. New insights into the molecular mechanisms of PROTAC-mediated degradation are needed, in order to improve their design and application as targeted therapy drugs in the fight against cancer.
The aim of the current Research Topic is to discuss the latest advances in the design and application of PROTACs-based therapies for cancer treatment. We welcome research articles, review articles, and perspectives that address, but are not limited to, the following themes:
• PROTACs design and clinical implications in cancer studies;
• Molecular basis of protein degradation mediated by PROTACs;
• Modulation of the ubiquitination system for the treatment of cancer;
• Innovative methodologies for designing PROTACs-based therapies;
• Comparison between previous non-targeted therapies and PROTACs.
Cancer is one the major causes of morbidity and mortality around the world. Cancer cells self-replicate and divide without any external stimulus and with metastatic properties. Various treatment options are available, such as chemotherapy, nanomedicines, etc, however such therapies do not specifically target cancer cells but also damage normal growing cells.
Proteolysis-targeting chimeras (PROTACs) can be used as a targeted treatment option for cancer. PROTACs are specific, versatile, and biologically active small molecules, able to induce selective intracellular proteolysis, which can be used for targeted degradation of proteins promoting tumorigenesis. PROTACs initiate the degradation process by recruiting the E3 ubiquitin ligase to the target protein, resulting into polyubiquitination of the protein of interest and its consequent degradation by 26S proteasome, a component of the ubiquitin-proteasome system (UPS) within eukaryotic cells. New insights into the molecular mechanisms of PROTAC-mediated degradation are needed, in order to improve their design and application as targeted therapy drugs in the fight against cancer.
The aim of the current Research Topic is to discuss the latest advances in the design and application of PROTACs-based therapies for cancer treatment. We welcome research articles, review articles, and perspectives that address, but are not limited to, the following themes:
• PROTACs design and clinical implications in cancer studies;
• Molecular basis of protein degradation mediated by PROTACs;
• Modulation of the ubiquitination system for the treatment of cancer;
• Innovative methodologies for designing PROTACs-based therapies;
• Comparison between previous non-targeted therapies and PROTACs.
