High-throughput screening for human collagenase 1 inhibitors

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

Research output: Contribution to journalArticle

6 Citations (Scopus)

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 - 2000
Externally publishedYes

Fingerprint

Matrix Metalloproteinase Inhibitors
Collagenases
Inhibitory Concentration 50
Catalytic Domain
Screening
Throughput
High-Throughput Screening Assays
Escherichia coli
Proteins
Testing
collagenase 1

Keywords

  • Drug screening
  • High-throughput screening
  • Matrix metalloproteinase

ASJC Scopus subject areas

  • Chemistry(all)
  • Pharmacology

Cite this

Ye, Q., 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.

High-throughput screening for human collagenase 1 inhibitors. / Ye, Qizhuang; Nan, F. J.; Hu, L. Y.; Qian, Z.; Qian, J.

In: Acta Pharmacologica Sinica, Vol. 21, No. 11, 2000, p. 1021-1026.

Research output: Contribution to journalArticle

Ye, Q, Nan, FJ, Hu, LY, Qian, Z & Qian, J 2000, 'High-throughput screening for human collagenase 1 inhibitors', Acta Pharmacologica Sinica, vol. 21, no. 11, pp. 1021-1026.
Ye, Qizhuang ; Nan, F. J. ; Hu, L. Y. ; Qian, Z. ; Qian, J. / High-throughput screening for human collagenase 1 inhibitors. In: Acta Pharmacologica Sinica. 2000 ; Vol. 21, No. 11. pp. 1021-1026.
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