title: A highly selective probe for human cytochrome P450 3A4: isoform selectivity, kinetic characterization and its applications.
abstract: Bufalin 5β-hydroxylation was found to be an isoform-specific biotransformation probe substrate for cytochrome P450 3A4 (CYP3A4). The probe reaction was well-characterized and it can be used for measuring the real catalytic activities of CYP3A4 from different enzyme sources.
authors.affiliation: Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, China. ylingdicp@gmail.com.
authors.forename: Guang-Bo
authors.initials: GB
authors.lastname: Ge
authors.forename: Jing
authors.initials: J
authors.lastname: Ning
authors.forename: Liang-Hai
authors.initials: LH
authors.lastname: Hu
authors.forename: Zi-Ru
authors.initials: ZR
authors.lastname: Dai
authors.forename: Jie
authors.initials: J
authors.lastname: Hou
authors.forename: Yun-Feng
authors.initials: YF
authors.lastname: Cao
authors.forename: Zhen-Wen
authors.initials: ZW
authors.lastname: Yu
authors.forename: Chun-Zhi
authors.initials: CZ
authors.lastname: Ai
authors.forename: Jing-Kai
authors.initials: JK
authors.lastname: Gu
authors.forename: Xiao-Chi
authors.initials: XC
authors.lastname: Ma
authors.forename: Ling
authors.initials: L
authors.lastname: Yang
mesh_terms: D055162:Biocatalysis; D002018:Bufanolides / Q000737:chemistry / Q000378:metabolism*; D051544:Cytochrome P-450 CYP3A / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D006900:Hydroxylation; D007527:Isoenzymes / Q000737:chemistry / Q000378:metabolism; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D015335:Molecular Probes / Q000737:chemistry / Q000378:metabolism*
chemical_list: D002018:Bufanolides; D007527:Isoenzymes; D015335:Molecular Probes; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; C022777:bufalin