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(left) TMPRSS2 in complex with the camostat/nafamostat fragment GBA (PDB ID 7MEQ(151)) and (right) a focus of its binding site in the S1 hydrolytic pocket of the enzyme. The catalytic triad of the enzyme (Ser441, His296, and Asp345) cleaves the inhibitor at its ester function, which results in the formation of a covalent bond between Ser441 and the carbonyl group of the remaining GBA.
