Emerging Approaches to GPCR Ligand Screening for Drug Discovery.
The superfamily of G-protein-coupled receptors (GPCRs) represents the largest class of cell surface receptors and, thus, a prominent family of drug targets. Recently, there has been significant progress in determination of GPCR crystal structures. The structure-based ligand discovery of GPCRs is emerging as a powerful path to drug development. Sensor surface-immobilized GPCRs can identify direct receptor-ligand interactions of a range of chemical libraries. This type of screening shows great promise as an alternative strategy for ligand discovery. Here, we summarize the most recent developments of structure- and sensor-based GPCR ligand discovery. We also highlight certain areas where GPCRs harbor great potential for the development of novel therapeutics, emphasizing the strategic approaches that may yield significant breakthroughs.
Department of Biological Sciences and Bioengineering, Indian Institute of Technology, Kanpur 208016, India.
Punita
P
Kumari
Department of Biological Sciences and Bioengineering, Indian Institute of Technology, Kanpur 208016, India.
Eshan
E
Ghosh
Department of Biological Sciences and Bioengineering, Indian Institute of Technology, Kanpur 208016, India. Electronic address: arshukla@iitk.ac.in.
Arun K
AK
Shukla
D000818:Animals; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology
D008024:Ligands; D043562:Receptors, G-Protein-Coupled; D054852:Small Molecule Libraries