Koo, Ki Dong, Kim, Min Jung, Kim, Sungsub, Kim, Kyoung-Hee, Hong, Sang Yong, Hur, Gwong-Cheung, Yim, Hyeon Joo, Kim, Geun Tae, Koh, Jong Sung, Lee, Chang-Seok
Synthesis of a novel series of DPPIV inhibitors with 1,2,4- and 1,3,4-oxadiazolyl ketone derivatives and its structure-activity relationships are discussed. Compound 18h showed good inhibitory activity against DPPIV and favorable pharmacokinetic properties. In vivo pharmacodynamic efficacy and co-crystal structure of compound 18h with DPPIV is also described.
        
Representative scheme of DPP4N_Peptidase_S9 structure and an image from PDBsum server
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PDB-Sum
2QKY Previously Class, Architecture, Topology and Homologous superfamily - PDB-Sum server
FSSP
2QKYFold classification based on Structure-Structure alignment of Proteins - FSSP server