GPCR Profiling Services with 231-targets Safety Panel

Due to their ability to regulate a wide range of physiological processes and the availability of druggable sites at the cell surface, GPCRs have long been sought after as pharmacological targets. Of the approximately 800 members of the human membrane protein family, approximately 400 are olfactory receptors, making GPCRs the biggest group. GPCR-targeted medication indications are growing beyond formerly well-known conditions including depression, schizophrenia, hypertension, allergies, and analgesics to include new conditions like AD and obesity. Moreover, new indications for GPCRs have been identified, including as hypocalcemia, short bowel syndrome, smoking cessation, and multiple sclerosis.

Numerous GPCRs have been found to function as nutritional sensors, making them viable targets for the treatment of inflammatory and metabolic disorders. Moreover, it's possible that a number of orphan receptors have developed to identify infections and trigger the proper immune reactions. Characterizing the residual orphan receptors may provide novel targets for a variety of applications. Since many of the approximately 400 olfactory GPCRs are now known to be widely distributed throughout the body and to have crucial activities beyond the perception of odors, the number of orphan receptors may expand significantly. It has also been discovered that tumor cells overexpress olfactory receptors. Creative Biolabs can provide GPCR profiling services with 231-targets safety panel to help GPCR drug development.

Fig.1. G protein coupled receptors. ¹

Applications of the 231-targets Safety Panel

• Compounds Screening

There are several applications for the 231-safety panel, contingent on the needs of compound screening. To aid with lead optimization, it could be applied to profile compounds against a family of receptors. Additionally, the 231 GPCR panel may be utilized to determine targets for various therapeutic domains, such as in vivo pain models.

• Addressing Off-target

GPCRs are expressed widely in human tissues. High similarity is usually shared by GPCRs in the same families. Multiple GPCRs can be functionally activated by certain endogenous ligands. Many of the drugs unintentionally activate additional GPCRs that weren't meant to be targets. In early stages of discovery, the 231-safety panel can be used to identify off-target effects of lead compounds in order to increase safety and specificity.

• Evaluation of Drugs

The 231-safety panel is a helpful tool for facilitating the drugs with established functionalities but ambiguous mechanisms of action. The target and mode of action of many bioactive compounds are yet unclear. There is significant therapeutic value in identifying the molecular mechanisms and therapeutic targets of these bioactive compounds.

• Drug Repurposing

The process of finding new applications, or secondary indications, for approved or experimental medications that fall outside the purview of the original indications is known as "drug repurposing." In GPCR drug discovery, medication repurposing is a compelling idea due to the abundance of current pharmaceuticals that target this particular target class.

Creative Biolabs' 231-targets safety panel covers 66 GPCR families. It is a complete and robust system for high-throughput compound profiling, and it may be used at any point in the drug development process. Please contact us for more information.

Reference

1. Audebrand, Anais, Laurent Désaubry, and Canan G. Nebigil. "Targeting GPCRs against cardiotoxicity induced by anticancer treatments." Frontiers in Cardiovascular Medicine 6 (2020): 194.