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Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
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In vitro expression and analysis of the 826 human G protein-coupled receptors

Xuechen Lv1, Junlin Liu1, Qiaoyun Shi1

  • 1iHuman Institute, ShanghaiTech University, Shanghai, 201210, China.

Protein & Cell
|April 18, 2016
PubMed

Insights

Researchers quantified protein expression for all 826 human G protein-coupled receptors (GPCRs) in an insect cell system. This study aids in prioritizing GPCRs for future structure determination, advancing drug discovery efforts.

Area of Science:

  • Biochemistry
  • Structural Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial cell signaling proteins involved in numerous physiological processes.
  • GPCRs represent significant therapeutic targets, yet their structural determination is hindered by challenges in protein expression.

Purpose of the Study:

  • To quantify protein expression levels for all 826 human GPCRs using an insect cell expression system.
  • To analyze expression characteristics across different GPCR subfamilies and fusion constructs.
  • To identify trends and prioritize GPCRs for future structural studies.

Main Methods:

  • Utilized an insect cell expression system to produce all 826 human GPCRs.
  • Employed two distinct fusion constructs for protein expression analysis.
  • Quantified and analyzed protein expression levels in aggregate and by GPCR subfamily.

Main Results:

  • Successfully quantified protein expression for the entire human GPCRome in an insect cell system.
  • Identified variations in expression efficiency based on GPCR subfamily and fusion construct.
  • Established a data-driven approach to predict expression feasibility for GPCRs.

Conclusions:

  • The study provides a comprehensive resource for understanding GPCR expression in insect cells.
  • Expression data can guide the selection of GPCRs for structural biology efforts.
  • This work facilitates the advancement of GPCR-targeted drug discovery and development.
Keywords:
G protein-coupled receptorsfusion constructinsectprotein expressionsurface expression analysis

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