Chlorambucyl-proline

Chlorambucyl-proline is a chloroplatinyl amino acid derivative with inhibitory activity against bovine pulmonary vasoconstrictor enzyme. Chlorambucyl-proline reacts with the convertase in a 1:1 ratio, and the removal of its radiolabel indicates that the compound has an irreversible inhibitory effect on the enzyme activity. Chlorambucyl-proline binds to the aspartic acid or glutamic acid side chain of the enzyme by forming an ester bond, resulting in irreversible inactivation of the enzyme. The inactivation rate constant of chlororambucyl-proline increases in the pH range of 5-8, indicating that its effect on the enzyme activity is affected by the pH environment[1].