title: High-throughput screening for human collagenase 1 inhibitors.
abstract: OBJECTIVE
  To establish a high-throughput method for inhibitor screening using a recombinant collagenase catalytic domain.
  
  
  METHODS
  Human collagenase 1 catalytic domain protein was expressed in E coli and used for screening a set of 2720 compounds in a high-throughput fashion.
  
  
  RESULTS
  The screening was accomplished within 2 h and 10 min with consumption of each compound at 4 micrograms. Sixty-six compounds were identified with > 60% inhibitory activity at 20 mg/L, among which 44 compounds were confirmed by subsequent testing at multiple concentrations. The most potent compound showed an IC50 at 4.3 mumol/L, and there were total 15 compounds with IC50 less than 20 mumol/L.
  
  
  CONCLUSIONS
  The high-throughput method using the recombinant collagenase is fast, effective and practical in identifying inhibitors.
authors.affiliation: National Centers for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China.
authors.forename: Q Z
authors.initials: QZ
authors.lastname: Ye
authors.forename: F J
authors.initials: FJ
authors.lastname: Nan
authors.forename: L Y
authors.initials: LY
authors.lastname: Hu
authors.forename: Z
authors.initials: Z
authors.lastname: Qian
authors.forename: J
authors.initials: J
authors.lastname: Qian
mesh_terms: D017364:Collagenases / Q000096:biosynthesis; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004926:Escherichia coli / Q000378:metabolism; D020128:Inhibitory Concentration 50; D061965:Matrix Metalloproteinase Inhibitors; D011994:Recombinant Proteins / Q000096:biosynthesis
chemical_list: D061965:Matrix Metalloproteinase Inhibitors; D011994:Recombinant Proteins; D017364:Collagenases; C417249:collagenase 1