GPCRs, an untapped source of transformative therapies

G protein-coupled receptors (GPCRs) are at the heart of cellular communication, translating extracellular signals into intracellular actions. As the largest and the most diverse group of cell receptors, GPCRs are central to regulating many vital processes in the body. Their ability to regulate key biological processes, including immune responses and inflammation, makes them especially attractive for therapeutic intervention.

Representing the most validated drug target family, with around 30-35% of marketed drugs acting on them, GPCRs have proven their importance in drug discovery. Yet, despite their validation, only about 10% of the total druggable GPCRs are currently targeted by existing therapies, leaving a vast opportunity for innovation. Until now, most efforts in GPCR drug discovery and development have been traditionally focused on cardiometabolic and central nervous system disorders.

At Domain, we are harnessing GPCR science and leveraging decades of expertise, to address high unmet medical needs in fields where current treatment solutions often fall short such as immuno-oncology and inflammation. We are committed to unlocking new and intractable GPCR targets to bring the most effective therapies to patients.

What makes GPCRs a game-changer in immuno-oncology and inflammation?

GPCRs play pivotal roles in regulating immune and inflammatory processes, making them invaluable targets for therapeutic breakthroughs in immuno-oncology and inflammation.

In immuno-oncology, GPCRs offer the groundbreaking opportunity to overcome tumor driven immunosuppression. Tumors often evade immune surveillance by silencing anti-tumor immune responses via immune checkpoints or releasing immunosuppressive molecules into the tumor microenvironment. These strategies undermine immunotherapy’s efficacy and limit clinical outcomes. By targeting specific GPCRs that regulate immune cell activity and infiltrated cells within the tumor microenvironment, we develop therapies that rearm the immune system, counter tumor escape mechanisms, and improve clinical outcomes for cancer patients.

Similarly, GPCRs regulate key inflammatory pathways, making them valuable targets for restoring balance. While inflammation is a natural response to injury or infection, when dysregulated, it can lead to serious conditions and diseases. By modulating GPCR activity, we can disrupt pathological inflammatory signals, paving the way for transformative therapies for patients with complex inflammatory conditions.

By harnessing the potential of GPCRs in immuno-oncology and inflammation, we are translating promising GPCR science into life-changing medicines.

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