文摘
VPAC2P-PEG is a VPAC2 receptor agonist peptide that acts as a glucose-dependent insulin secretagogue.Proteolysis by DPPIV may contribute to the in vivo clearance of VPAC2P-PEG. Here, the N-terminus ofVPAC2P-PEG is modified by N-terminal acetylation to impart DPPIV resistance. The acetylated peptide,Ac-VPAC2P-PEG, is a selective and potent VPAC2 agonist, resistant to DPPIV proteolysis, and exhibitssubstantially improved half-life and glucose disposal in rodents. Ac-VPAC2P-PEG has therapeutic potentialfor diabetes management.