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AAT Bioquest

What are the applications of covalent inhibitors?

Posted April 4, 2024


Answer

Covalent inhibitors are drugs that bind covalently with specific target proteins, creating a lasting connection that alters the protein irreversibly and causes it to lose its function, resulting in enhanced potency and an extended duration of action. This has the advantages of increasing efficacy while lowering dosage, minimizing drug resistance, and targeting shallow binding sites. 

Some of the more notable applications of covalent inhibitors include: 

  • Drug design: The irreversible binding nature makes covalent inhibitors ideal for developing long-lasting drugs with enhanced efficacy and selectivity. 
  • Targeted therapy: The ability of covalent inhibitors to selectively bind to specific disease-causing proteins, makes them a promising option for targeted drug therapies. 
  • Chemical biology: Covalent inhibitors are valuable tools for studying protein function, interactions, and signaling pathways in biological systems. 
Additional resources

Extended Applications of Small-Molecule Covalent Inhibitors toward Novel Therapeutic Targets

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