Characteristic roadmap of linker governs the rational design of PROTACs
Guizhou University · Macao Polytechnic University · +1 more institution
Abstract
Proteolysis targeting chimera (PROTAC) technology represents a groundbreaking development in drug discovery, leveraging the ubiquitin‒proteasome system to specifically degrade proteins responsible for the disease. PROTAC is characterized by its unique heterobifunctional structure, which comprises two functional domains connected by a linker. The linker plays a pivotal role in determining PROTAC's biodegradative efficacy. Advanced and rationally designed functional linkers for PROTAC are under development. Nonetheless, the correlation between linker characteristics and PROTAC efficacy remains under-investigated. Consequently, this study will present a multidisciplinary analysis of PROTAC linkers and their…
Citation impact
- FWCI
- 23.21
- Percentile
- 100%
- References
- 214
Authors
9Topics & keywords
- Linker
- Rational design
- Flexibility (engineering)
- Proteolysis
- Computer science
- Computational biology
- Chemistry
- Nanotechnology