Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Assessing GPCR activation using protein complementation: a novel technique for HTS.

R M Eglen1

  • 1Discovery and Research Reagents, PerkinElmer Life and Analytical Sciences, 940 Winter Street, Waltham, MA 02451-1457, USA. richard.eglen@perkinelmer.com

Biochemical Society Transactions
|July 20, 2007
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Muscarinic receptor subtypes in neuronal and non-neuronal cholinergic function.

Autonomic & autacoid pharmacology·2006
Same author

A homogeneous cell-based assay to measure nuclear translocation using beta-galactosidase enzyme fragment complementation.

Assay and drug development technologies·2006
Same author

No evidence for activation of alpha(2)-adrenoceptors by methanolic extracts of bovine brain and lung containing clonidine-displacing substance.

Annals of the New York Academy of Sciences·2004
Same author

High-affinity interactions of ligands at recombinant guinea pig 5HT7 receptors.

Journal of computer-aided molecular design·2002
Same author

Pharmacological characterization of muscarinic receptors in mouse isolated urinary bladder smooth muscle.

British journal of pharmacology·2001
Same author

Therapeutic opportunities from muscarinic receptor research.

Trends in pharmacological sciences·2001
Same journal

TDP-43 proteinopathy as a biomarker and therapeutic target in amyotrophic lateral sclerosis.

Biochemical Society transactions·2026
Same journal

Advancing the monitoring of organelle contact sites in vitro and in vivo.

Biochemical Society transactions·2026
Same journal

Mechanisms influencing transient cytoplasmic protein targeting to intracellular lipid droplets.

Biochemical Society transactions·2026
Same journal

Replication associated nuclear DNA mismatch repair across kingdoms.

Biochemical Society transactions·2026
Same journal

Phosphatases of regenerating liver downregulate PTEN to promote tumorigenesis.

Biochemical Society transactions·2026
Same journal

Implications of Rho GTPase signaling in cancer immunotherapy.

Biochemical Society transactions·2026
See all related articles

Novel high-throughput screening (HTS) methods are needed to study G-protein-coupled receptors (GPCRs) beyond simple agonism/antagonism. Oligomerization-assisted complementation assays offer sensitive detection of GPCR protein interactions.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • G-protein-coupled receptors (GPCRs) are crucial drug targets, but current high-throughput screening (HTS) methods primarily assess agonism and antagonism.
  • GPCRs exhibit complex functions involving interactions with various proteins like RAMPs, beta-arrestins, G-proteins, and form homo/heteromeric complexes.
  • Existing HTS assays are insufficient for interrogating these complex protein-protein interactions of GPCRs.

Purpose of the Study:

  • To develop novel HTS technologies for investigating GPCRs beyond traditional functional assays.
  • To enable the study of GPCRs' complex cellular protein-protein interactions.
  • To introduce a sensitive and robust assay for GPCR research.

Main Methods:

  • Utilizing oligomerization-assisted complementation of monomeric protein fragments to detect GPCR complex reassembly.

Related Experiment Videos

  • Employing enzyme complementation for sensitive signal generation, enabling low-volume HTS protocols.
  • Developing luminescent assays using complementing proteins to minimize artefactual interferences.

    • Main Results:

    • Demonstrated the feasibility of using enzyme complementation for sensitive detection of GPCR interactions.
    • Established HTS protocols requiring minimal fluid volumes.
    • Developed assays with reduced susceptibility to artefactual interferences.

    Conclusions:

    • Oligomerization-assisted complementation assays represent a significant advancement for GPCR research.
    • These novel HTS technologies facilitate the study of complex GPCR protein interactions.
    • The developed luminescent assays offer high sensitivity and robustness for drug discovery efforts targeting GPCRs.