Enkephalin convertase, also known as carboxypeptidase E, removes C-terminal residues during the processing of propeptides, including enkephalin and proinsulin. 2-Guanidinoethylmercaptosuccinic acid (GEMSA) is a potent inhibitor of enkephalin convertase (Ki = 8.8 nM) that is functional in vivo. It is a peptidomimetic inhibitor, occupying the specificity pocket of the enzyme. GEMSA can also inhibit other carboxypeptidases, including thrombin-activatable fibrinolysis inhibitor.
