Seven-transmembrane receptors, also known as G-protein-coupled receptors (GPCRs), are integral membrane proteins that contain seven membrane-spanning helices. This superfamily of cell surface signaling proteins plays a crucial role in many physiological processes and numerous diseases, including cancer.
It is known that 134 GPCRs are targets for drugs approved in the United States or European Union (as of November 2017) . GPCRs and GPCR-related proteins upstream (e.g., ligands) and downstream (e.g. phosphodiesterases [PDEs] that degrade cAMP) from GPCRs represent approximately 17 % of all protein targets for approved drugs. As such, GPCRs constitute the largest family of druggable proteins in the human genome targeted by over a third of marketed drugs worldwide . Approved drugs targeting GPCRs and GPCR-related proteins are primarily small molecules and peptides.
Since approximately 100 of over 360 human endo-GPCRs are orphan GPCRs (lacking known physiologic agonists), the number of exploited GPCR targets, GPCR-based drugs, and the types of drugs will probably increase in the future.
Given the importance of GPCR in small-molecule drug discovery, Life Chemicals offers a proprietary collection of potential GPCR activity modulators. GPCR-focused screening compounds were selected using both ligand-based (computational chemistry, 2D fingerprint similarity search) and receptor-based (molecular docking, high-throughput virtual screening) approaches.
- Sriram K, Insel PA. G Protein-Coupled Receptors as Targets for Approved Drugs: How Many Targets and How Many Drugs?. Mol Pharmacol. 2018;93(4):251-258. DOI:10.1124/mol.117.111062
- Zhou J, Wild C. GPCR Drug Discovery: Emerging Targets, Novel Approaches and Future Trends. Curr Top Med Chem. 2019;19(16):1363-1364. DOI:10.2174/156802661916190828093500