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Dipeptidyl peptidase-4 (DPP-4) inhibitors enhance insulin secretion and reduce glucose production by inhibiting DPP-4 enzyme activity (128)

Bottom line: the largest weight-loss signal of any obesity peptide so far about 24% mean loss at 48 weeks in a phase 2 trial but investigational only, now in phase 3 (the TRIUMPH program) and not approved by any regulator

N3 is the representative peptidomimetic inhibitor, and harbours a Michael acceptor as a warhead and substituents spanning all substrate-binding subsites

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10.1016/j.freeradbiomed.2017.05.002 Free Radic