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An unnatural amino acid that forms a covalent bond with a proximal cysteine can be introduced into proteins, facilitating a variety of applications. Natural proteins often rely on the disulfide ...
MRTX849's acrylamide (red in the structure) forms a covalent bond to a cysteine's sulfur (yellow) in KRAS G12C (shown in the crystal structure on the left). Credit: J. Med. Chem.
Cytotoxic Activity of Salicylic Acid-Containing Drug Models with Ionic and Covalent Binding. ACS Medicinal Chemistry Letters, 2015; 151002131101002 DOI: 10.1021/acsmedchemlett.5b00258 ...
It described an unnatural amino acid that can turn a protein into a covalent binder (Cell 2020, DOI: 10.1016/j.cell.2020.05.028).
Crystallographic studies reveal that 2α,3ax-difluoro-N-acetylneuraminic acid forms a covalent bond with influenza neuraminidase Tyr406 and the compound was found to possess potent anti-influenza ...