High-throughput screening for human collagenase 1 inhibitors

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

Research output: Contribution to journalArticle

6 Scopus citations

Abstract

AIM: 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 μg. 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 μmol/L, and there were total 15 compounds with IC50 less than 20 μmoL/L. CONCLUSION: The high-throughput method using the recombinant collagenase is fast, effective and practical in identifying inhibitors.

Original languageEnglish (US)
Pages (from-to)1021-1026
Number of pages6
JournalActa Pharmacologica Sinica
Volume21
Issue number11
StatePublished - Dec 4 2000
Externally publishedYes

Keywords

  • Drug screening
  • High-throughput screening
  • Matrix metalloproteinase

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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  • Cite this

    Ye, Q. Z., Nan, F. J., Hu, L. Y., Qian, Z., & Qian, J. (2000). High-throughput screening for human collagenase 1 inhibitors. Acta Pharmacologica Sinica, 21(11), 1021-1026.