GPCR Profiling Services with 294-targets Safety Panel

The human genome has around 800 receptors, making GPCRs the biggest class of druggable targets on the cell surface. GPCR-targeting medications have a great safety record, which makes them popular for treating chronic illnesses. GPCRs are overexpressed in cancer and play a role in a number of cellular processes, including metastasis, angiogenesis, and tumor formation.

GPCRs play a role in numerous human illnesses. Thus, the study of acceptable specificity toward numerous targets, interconnected signaling pathways that produce therapeutic benefit, or cross-reactivity that may result in undesirable consequences is known as polypharmacology. Major indications for GPCR modulators include obesity, cancer, Alzheimer's disease, and type 2 diabetes. While modulators aimed against β2AR, DRD2, and AGTR1 can attain desirable efficacies for certain respiratory ailments, cardiovascular diseases, and CNS disorders, respectively, these polygenic diseases cannot be entirely treated with a single drug. Creative Biolabs can provide GPCR profiling services with 294-targets safety panel covering many therapeutic areas.

Fig.1. GPCR families are major drug targets. ¹

Assay Modes of the 294-targets Safety Panel

Finding agonists and antagonists has been a major focus of GPCR drug discovery. An agonist is a type of ligand that stimulates the GPCR to initiate intracellular signaling and trigger a biological response. Conversely, an antagonist is a class of ligand that can stop an agonist—natural or synthetic—from inhibiting signaling and biological response. The agonist and antagonist versions are the two assay modalities available in our 294-targets safety panel. Orphan GPCRs are only tested in the agonist mode. We are capable of identifying and characterizing each of these compounds with our 294-targets safety panel.

Therapeutic Areas in the 294-targets Safety Panel

Many human G protein-coupled receptors (GPCRs) have both activating and inactivating mutations, and these changes are linked to a variety of illness characteristics. Only a small portion of the GPCR mutations linked to diseases have been functionally described. GPCR malfunctions have been linked to numerous diseases, including immunological, metabolic, and reproductive abnormalities, cancer, and neurodegenerative diseases. Our 294-targets safety panel includes a wide range of GPCR targets from various research fields, such as immunology, cancer, hematology, metabolism, psychiatry, neurology, ophthalmology, cardiology, respiratory, gastrointestinal, dermatology, musculoskeletal, and reproduction research.

Creative Biolabs is always monitoring the membrane protein drug discovery and development. Our scientists have years of experience working with clients worldwide and are extremely skilled. Your drug discovery and development projects will benefit greatly from Creative Biolabs' excellent service and products. Please contact us for more information about our GPCR profiling services with 294-targets safety panel.

Reference

Hauser, Alexander S., et al. "Trends in GPCR drug discovery: new agents, targets and indications." Nature reviews Drug discovery 16.12 (2017): 829-842.

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