Vinyl-ACCA

Further optimization of the tetrapeptide series led to very potent inhibitors allowing for size reduction to tiipeptides (Figure 2.5) [104]. Further structural studies revealed that macrocyclization can improve potency by constraining the vinyl-ACCA into the correct conformation for binding [42, 105]. In this series of macrocyclic inhibitors, the cyclopropyl PI moiety is... 

Table 2.1 VINYL-ACCA IN COMPARISON WITH VARIUOS PI RESIDUES...

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