Peptide-class targeted receptors and protein–protein interaction surfaces

Peptide-class targeted receptors and protein–protein interaction surfaces represent a broad classification of therapeutic targets rather than a single molecular entity. This category includes receptors that recognize peptide hormones or neurotransmitters, such as Class B G protein-coupled receptors, as well as the contact surfaces between proteins that facilitate intracellular signaling (Source: PubMed, PMID: 30635403). These targets are central to numerous physiological processes, including glucose homeostasis, immune cell activation, and programmed cell death (Source: UniProt). While historically challenging to target with small molecules due to the large and often flat nature of their binding interfaces, they are now major focuses for peptide mimetics and monoclonal antibodies (Source: Nature Reviews Drug Discovery, doi:10.1038/nrd.2016.29). Prominent examples of drugs targeting these classes include semaglutide for peptide receptors and venetoclax for protein-protein interactions (Source: PubChem). Because the term refers to a diverse set of thousands of different proteins, it is considered a target class rather than a specific, individual drug target.

Other names

Peptide-binding receptorsProtein-protein interaction (PPI) interfacesPeptide-GPCRsPPI targets

Modulation of receptor signaling through peptide-mimetic binding or physical disruption of protein-protein complexes to inhibit downstream signaling.