G Protein-Coupled Receptors (GPCRs)
G Protein-Coupled Receptors (GPCRs) are involved in a wide range of physiological and pathological processes and represent a large class of drug targets accounting for >30% of all drugs on the market. These drugs, however, only cover 15% of the entire GPCR family, and many valuable receptors remain undrugged. In particular, GPCRs whose natural ligands are large peptides or small proteins are challenging for drug development due to their large and complex binding pockets.
Our novel scientific approach makes previously undruggable GPCRs accessible, providing Orion Biotechnology with the unique opportunity of developing first-in-class GPCR-targeting therapeutics. Our breakthrough technology involves precision engineering the peptide and protein ligands of these GPCRs to develop analogs with superior binding affinity, potency, and pharmacological control.
Enabled by our proprietary drug discovery platform, we are rapidly advancing a diversified portfolio of therapeutics against high-value GPCR targets in oncology and other serious diseases.
Orion’s drug discovery engine integrates a suite of complimentary methods:
Streamlined Phage Display
Phage display approach enabling millions of peptide and protein analogs to be screened directly on cells expressing the targeted receptor, bypassing the need for receptor purification
Multiplex Chemical Synthesis
Proprietary multiplex chemical synthesis technology designed to enable rapid parallel production of candidate analogs identified by phage display
Structure-Activity Matrix
In-depth evaluation of libraries of structurally related peptide and protein analogs in a panel of cell-based assays, generating a structure-activity matrix for the target receptor
Refinement and Optimization
Use of both in silico and lab-based approaches supported by the structure-activity matrix to optimize initial leads (potency improvement, fine-tune signaling activity)
The company’s fully integrated discovery process leverages our proprietary technology to produce optimized leads within 12 months, resulting in one of the most rapid discovery engines available in the industry today.
