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• W1977679840 abstract "To find potent and selective inhibitors of dipeptidyl peptidase IV (DPP-IV), we synthesized a series of 2-cyanopyrrolidine with P2-site 4-substituted glutamic acid derivatives and tested their activities against DPP-IV, DPP8, and DPP-II. Analogues that incorporated a bulky substituent at the first carbon position of benzylamine or isoquinoline showed over 30-fold selectivity for DPP-IV over both DPP8 and DPP-II. From structure-activity relationship studies, we speculate that the S2 site of DPP8 might be similar to that of DPP-IV, while DPP-IV inhibitor with N-substituted glycine in the P2 site and/or with a moiety involving in hydrophobic interaction with the side chain of Phe357 might provide a better selectivity for DPP-IV over DPP8." @default.
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• W1977679840 date "2005-07-01" @default.
• W1977679840 modified "2023-10-09" @default.
• W1977679840 title "Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors" @default.
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• W1977679840 doi "https://doi.org/10.1016/j.bmcl.2005.04.051" @default.
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