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Download our whitepaper to learn more about Orion’s novel drug modality and approach to targeting previously-undrugged GPCRs.

A Novel Approach to Targeting Previously Undruggable 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 peptide and small proteins, have proven 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 small protein ligands of these GPCRs to develop analogs with superior binding affinity, potency, and pharmacological control.

Enabled by our PROcisionX^TMDiscovery Platform, we are rapidly advancing a diversified portfolio of therapeutics against high-value GPCR targets for the treatment of metabolic and immunological diseases.

The PROcisionX Discovery Platform

Orion’s drug discovery engine integrates a suite of complimentary methods:

Streamlined Phage Display

Phage display approach enabling millions of peptide and small 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 small 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.

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Orion Biotechnology

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