title: [High-throughput screening for hamster chymase 2 inhibitors].
abstract: To screen potential hamster chymase 2 inhibitors, a high-throughput screening (HTS) model was established. Recombinant hamster chymase 2 with active form was cloned and expressed in E. coli. The HTS model with total volume of 50 microL in 384-well microplate was based on fluorescence analysis and was proved sensitive as well as specific (Z' = 0.84). A total of 40 080 samples (including 28 060 compounds and 12 020 natural products) were screened, and 613 samples with inhibition greater than 90% were selected for further rescreening. Finally, compounds J16647 and J16648 were identified with high inhibitory activity on chymase 2, and whose IC50 values were 0.823 and 0.690 micromol x L(-1), respectively.
authors.affiliation: National Center for Pharmaceutical Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
authors.forename: Shou-Bao
authors.initials: SB
authors.lastname: Wang
authors.forename: Xiao-Ming
authors.initials: XM
authors.lastname: Zhu
authors.forename: Feng
authors.initials: F
authors.lastname: Gao
authors.forename: Xiao-Bin
authors.initials: XB
authors.lastname: Pang
authors.forename: Guan-Hua
authors.initials: GH
authors.lastname: Du
mesh_terms: D000818:Animals; D053818:Chymases / Q000032:analysis / Q000037:antagonists & inhibitors*; D006224:Cricetinae; D004791:Enzyme Inhibitors / Q000032:analysis* / Q000494:pharmacology; D004926:Escherichia coli / Q000378:metabolism; D057166:High-Throughput Screening Assays / Q000379:methods*; D020128:Inhibitory Concentration 50; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; C083294:chymase 2; D053818:Chymases