Functional peptide screening is emerging as a significant area in the competitive field of AI-driven drug discovery, with G protein-coupled receptors (GPCRs) and radiopharmaceutical targets drawing increased attention. This trend was highlighted on May 14, when recent scientific literature pointed to high-throughput GPCR-activating peptide screening as a timely technical topic.
Big pharmaceutical companies are showing interest in this area. Eli Lilly made a $140 million upfront payment to Radionetics Oncology for access to novel GPCR targets and secured an exclusive future right to acquire the biotech for $1 billion in July 2024. According to a press release, this agreement gave Eli Lilly “access to novel GPCR targets.”
Contract research organizations are also participating in functional screening, particularly for GPCR agonists and peptide-mediated targeting methods such as radioligand therapies. GPCRs remain central because they control cell signaling from membranes and represent a large share of approved drug targets. Despite their prominence, many GPCRs—especially orphan receptors—are still underexplored, presenting opportunities for discovering new ligands and mechanisms.
A ligand is defined as a molecule that binds to the GPCR receptor; radiopharmaceutical approaches use these ligands as targeting components of radioactive drugs. BioSpace previously reported that radiotherapeutics offer significant potential due to the variety of cancer surface targets available for different carriers, isotopes, and formulation methods.
“GPCRs have always been a major focus for drug discovery, and even more so with the advent of drugs targeting GLP-1R and other incretin receptors,” said Simon Bushell, External Innovation and Business Development lead at Orbit Discovery. He noted that these molecules target receptors like glucagon-like peptide-1 receptor (GLP-1R), which is important in treating metabolic diseases.
Orbit Discovery has collaborated with various biotechs and large pharmaceutical firms to identify peptides involved in modulating inflammation or directing treatments across the blood-brain barrier or toward specific cancers. Its platform also identifies differentiated peptides aimed at pain relief or neurological conditions.
Other service providers active in this market include Charnwood Discovery, Creative Bioarray, and Creative Biogene. The global market for peptide library screening services was projected last year to reach $50 billion. “Peptide libraries offer a powerful tool for identifying lead compounds with therapeutic potential... The continuous innovation in peptide synthesis and high-throughput screening platforms also plays a crucial role,” according to Data Insights market report.
Orbit’s platform screens extensive peptide libraries directly against cells using functional readouts—a process designed not just for binding but also activating signaling pathways by identifying agonists capable of inducing conformational changes necessary for activation.
Functional peptide screening platforms are being positioned as differentiators within AI-based drug discovery by providing accurate hits needed by pharmaceutical companies looking to reduce risk during development programs.
