Abstract

Peptides are a leading therapeutic modality due to their biological ubiquity and relative ease of optimisation. G-Protein Coupled Receptors (GPCRs) remain a prominent drug targeting paradigm, with many established GPCR families known to be modulated by peptide ligands, such as the melanocortin receptor families. Current screening strategies can be categorised as either affinity strategies, where library molecules are scanned against the target molecule in isolation to find potential binders, or functional strategies, where ligands are tested against cells to see if they elicit a functional response. While affinity screening can produce large numbers of potential binders, the process of confirming functional modulation and binding specificity can be time consuming. Functional screening, while mitigating these concerns, is traditionally lower throughput.