Covalent Reversible Peptidic Inhibitors

As an alternative to peptidic inhibitors, which display electrostatic interactions with the active site, covalent inhibitors have also been described recently. Such peptides bear a functional group that can react reversibly with the catalytic serine of the protease. These include aldehydes, a-ketoacid derivates, lactams and boronates.

Research groups at Vertex and Lilly optimized inhibitors starting from pyrazinoyl capped tetrapeptidic aldehydes (Table 2.4) [137]. The main SAR

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