Biomaterial Database

High-throughput screening for human collagenase 1 inhibitors. 2000

Q Z Ye, and F J Nan, and L Y Hu, and Z Qian, and J Qian

National Centers for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China.

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.

UI	MeSH Term	Description	Entries
D011994	Recombinant Proteins	Proteins prepared by recombinant DNA technology.	Biosynthetic Protein,Biosynthetic Proteins,DNA Recombinant Proteins,Recombinant Protein,Proteins, Biosynthetic,Proteins, Recombinant DNA,DNA Proteins, Recombinant,Protein, Biosynthetic,Protein, Recombinant,Proteins, DNA Recombinant,Proteins, Recombinant,Recombinant DNA Proteins,Recombinant Proteins, DNA
D004353	Drug Evaluation, Preclinical	Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.	Drug Screening,Evaluation Studies, Drug, Pre-Clinical,Drug Evaluation Studies, Preclinical,Drug Evaluations, Preclinical,Evaluation Studies, Drug, Preclinical,Evaluation, Preclinical Drug,Evaluations, Preclinical Drug,Medicinal Plants Testing, Preclinical,Preclinical Drug Evaluation,Preclinical Drug Evaluations,Drug Screenings,Screening, Drug,Screenings, Drug
D004926	Escherichia coli	A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.	Alkalescens-Dispar Group,Bacillus coli,Bacterium coli,Bacterium coli commune,Diffusely Adherent Escherichia coli,E coli,EAggEC,Enteroaggregative Escherichia coli,Enterococcus coli,Diffusely Adherent E. coli,Enteroaggregative E. coli,Enteroinvasive E. coli,Enteroinvasive Escherichia coli
D017364	Collagenases	Enzymes that catalyze the degradation of collagen by acting on the peptide bonds.	Collagen Peptidase,Collagen-Degrading Enzyme,Collagenase,Collagen Degrading Enzyme,Peptidase, Collagen
D061965	Matrix Metalloproteinase Inhibitors	Compounds that inhibit the enzyme activity or activation of MATRIX METALLOPROTEINASES.	Collagenase Inhibitor,Gelatinase Inhibitor,MMP Inhibitor,Matrix Metalloproteinase Inhibitor,Collagenase Inhibitors,Gelatinase Inhibitors,MMP Inhibitors,Stromelysin Inhibitors,Inhibitor, Collagenase,Inhibitor, Gelatinase,Inhibitor, MMP,Inhibitor, Matrix Metalloproteinase,Inhibitors, Collagenase,Inhibitors, Gelatinase,Inhibitors, MMP,Inhibitors, Matrix Metalloproteinase,Inhibitors, Stromelysin,Metalloproteinase Inhibitor, Matrix,Metalloproteinase Inhibitors, Matrix
D020128	Inhibitory Concentration 50	The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.	IC50,Concentration 50, Inhibitory