Geodesy

Function (biology)

Biology

Pace

Particle physics

Receptor

Computer science

Drug

Computational biology

Drug discovery

Genetics

Physics

G protein-coupled receptor

Bioinformatics

Geography

Structure function

Drug development

Pharmacology

Data science

Signal Transduction and Targeted Therapy

As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to knowledge-driven drug design. We are eye-witnessing tremendous progresses made recently in the understanding of their structure-function relationships that facilitated drug development at an unprecedented pace. This article intends to provide a comprehensive overview of this important field to a broader readership that shares some common interests in drug discovery.

G protein-coupled receptors: structure- and function-based drug discovery