New approaches for G-protein coupled receptor ligands identification

ABSTRACT

G protein-coupled receptors (GPCRs) represent the class of proteins with the highest impact from social, therapeutic and economic point of view. Today, more than 50% of drug targets are based on GPCRs and the annual worldwide sales exceeds 50 billion dollars. GPCRs are involved in all major diseases areas such as cardiovascular, metabolic, neurodegenerative, psychiatric, cancer and infectious diseases. The classical drug discovery process has relied on screening compounds, which interact favorably with the GPCR of interest followed by further chemical engineering as a mean of improving efficacy and selectivity. On the other hand, several new peptides with potential bioactivity are discovery every year. This review will focus on recent advancement on methods for identification of novel peptides with potential ability to activate GPCRs.