The therapeutic potential of PROTACs

Area of Science:

• Biochemistry
• Medicinal Chemistry
• Drug Discovery

Background:

• Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules that induce target protein degradation via ubiquitination and proteasomal pathways.
• PROTACs offer unique mechanisms for modulating target biology, distinct from traditional inhibitors.
• The therapeutic potential of PROTACs is significant, promising new treatments for various diseases.

Purpose of the Study:

• To review patent applications for PROTACs.
• To analyze the landscape of PROTAC development in patent literature.

Main Methods:

• Review of published PCT (WO) patent applications from January 2013 to June 2020.
• Inclusion of English-language applications with exemplified PROTACs that degrade target proteins.
• Definition of PROTACs as bifunctional molecules with discrete target and E3 ligase binding elements.

Main Results:

• Analysis of patent filings reveals active development in the PROTAC field.
• Exemplified PROTACs demonstrate the capability to induce target protein degradation.

Conclusions:

• Developing differentiated PROTAC medicines is crucial for realizing their full therapeutic potential.
• The modular nature of PROTACs presents unique intellectual property opportunities and challenges.
• Evolving novelty requirements are anticipated as the PROTAC field matures.