Title : NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(S)- pyrrolidine), a slow-binding inhibitor of dipeptidyl peptidase IV.

Pub. Date : 1999 Sep 7

PMID : 10512614






3 Functional Relationships(s)
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1 Through kinetic evaluation of DPP-IV inhibition by the D-antipode, des-cyano, and amide analogues of NVP-DPP728, it was determined that the nitrile functionality at the 2-pyrrolidine position is required, in the L-configuration, for maximal activity (K(i) of 11 nM vs K(i) values of 5.6 to >300 microM for the other analogues tested). dpp728 dipeptidyl peptidase 4 Homo sapiens
2 NVP-DPP728 inhibited DPP-IV in a manner consistent with a two-step inhibition mechanism. dpp728 dipeptidyl peptidase 4 Homo sapiens
3 Taken together, these data suggest that NVP-DPP728 inhibits DPP-IV through formation of a novel, reversible, nitrile-dependent complex with transition state characteristics. dpp728 dipeptidyl peptidase 4 Homo sapiens