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Multi-enzyme Screening Using a High-throughput Genetic Enzyme Screening System
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A high-throughput screening system for G-protein-coupled receptors using β-lactamase enzyme complementation

Chuan-ke ZHAO1, Qi YIN, Shi-you LI

  • 1Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing 100029, China.

Acta Pharmacologica Sinica
|November 25, 2010
PubMed
Summary

A new assay monitors G-protein-coupled receptor (GPCR) activation using β-lactamase enzyme fragment complementation (EFC). This method successfully screened a natural compound library for β2-adrenoceptor (β2AR) agonists.

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Molecular Biology

Background:

  • G-protein-coupled receptors (GPCRs) are crucial drug targets.
  • Monitoring GPCR activation is essential for drug discovery.
  • Existing methods may lack efficiency or specificity.

Purpose of the Study:

  • To develop a novel cell-based assay for monitoring GPCR activation.
  • To utilize β-lactamase enzyme fragment complementation (EFC) technology for this purpose.
  • To screen a natural compound library for β2-adrenoceptor (β2AR) agonists.

Main Methods:

  • Fused inactive β-lactamase fragments to β-arrestin and GPCR.
  • Generated a stable cell line (HEK/293-β2a2) expressing these fusion proteins.
  • Performed high-throughput screening (HTS) of HPLC-fractionated natural compounds on the cell line.
  • Validated hits by measuring cyclic adenosine monophosphate (cAMP) production.

Main Results:

  • The HEK/293-β2a2 cell line showed dose-dependent responses to β2AR agonists/antagonists.
  • Isoproterenol and propranolol EC50/IC50 values were determined.
  • HTS yielded a Z' factor of 0.68.
  • Three potent β2AR agonists were identified from the natural compound library.

Conclusions:

  • Established a cell-based HTS assay for monitoring GPCR activation.
  • The assay relies on β-arrestin and GPCR interaction via β-lactamase EFC.
  • This system is effective for identifying drug leads from natural compound libraries.