title: The crystal structure of human dipeptidyl peptidase IV (DPPIV) complex with diprotin A.
abstract: Dipeptidyl peptidase IV (DPPIV) is a serine protease, a member of the prolyl oligopeptidase (POP) family, and has been implicated in several diseases. Therefore, it seems important to develop selective inhibitors for human DPPIV (hDPPIV) that are able to control the biological function of hDPPIV. In order to elucidate the binding mode and substrate specificity, we determined the crystal structure complex of hDPPIV and diprotin A (IIe-Pro-IIe), a slowly hydrolyzed substrate of hDPPIV, at 2.2 A resolution. In this paper, we discuss the molecular interaction mechanism of diprotin A with hDPPIV based on the X-ray crystal structure.
authors.affiliation: Tanabe Seiyaku Co. Ltd., 3-16-89 Kashima, Yodogawa-ku, Osaka 532-8505, Japan.
authors.forename: Hajime
authors.initials: H
authors.lastname: Hiramatsu
authors.forename: Atsushi
authors.initials: A
authors.lastname: Yamamoto
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Kyono
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Higashiyama
authors.forename: Chiaki
authors.initials: C
authors.lastname: Fukushima
authors.forename: Hideaki
authors.initials: H
authors.lastname: Shima
authors.forename: Shigeru
authors.initials: S
authors.lastname: Sugiyama
authors.forename: Koji
authors.initials: K
authors.lastname: Inaka
authors.forename: Ryo
authors.initials: R
authors.lastname: Shimizu
mesh_terms: D001665:Binding Sites; D003460:Crystallization; D018360:Crystallography, X-Ray; D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry*; D006801:Humans; D008958:Models, Molecular; D009842:Oligopeptides / Q000737:chemistry*; D011487:Protein Conformation; D017434:Protein Structure, Tertiary
chemical_list: D009842:Oligopeptides; C041445:diprotin A; D018819:Dipeptidyl Peptidase 4