Outside Front Cover: Covalent Protein Inhibitors via Tyrosine and Tryptophan Conjugation with Cyclic Imine Mannich Electrophiles

Key Points

• The aim is to explore the use of cyclic imine Mannich electrophiles for covalently targeting protein residues.
• Developed covalent inhibitors using cyclic imine Mannich electrophiles.
• Targeted tyrosine and tryptophan residues in proteins.
• Demonstrated selectivity over other protein functional groups.
• Showed successful covalent modification of tyrosine and tryptophan.
• Established a new method for creating irreversible covalent inhibitors.
• Highlighted improved selectivity in covalent targeting of proteins.