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Updated: Jan 22, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Advances in Therapeutic Antibody Discovery and Development Targeting G Protein-Coupled Receptors
Catherine J Hutchings1, Serbülent Ünsal2, Mathieu Rappas3
1Independent Consultant, Hertfordshire, UK.
None:
G protein-coupled receptors (GPCRs) are integral to numerous biological processes and are associated with various diseases across all therapeutic areas. Consequently, GPCRs present substantial potential for antibody-based therapies. This review offers an overview of the therapeutic GPCR-antibody target landscape and examines the diversity within current therapeutic programs at different stages of the research and development pipeline. The progression of the GPCR-antibody pipeline demonstrates ongoing maturation, reflecting advancements that have addressed several longstanding technical challenges. Additionally, we discuss the rapid expansion of artificial intelligence and machine learning platforms designed to accelerate antibody discovery and clinical development, providing specific examples of their application to GPCRs.
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