GPR17 - G Protein Coupled Receptor | Elisa - Clia - Antibody - Protein

Background

GPR17, also known as G protein-coupled receptor 17, is a member of the G protein-coupled receptor (GPCR) family, which is one of the largest families of cell surface receptors involved in signal transduction. GPCRs play crucial roles in various physiological processes by transducing extracellular signals into intracellular responses. It was first identified in the early 2000s through bioinformatics approaches and subsequently characterized as an orphan receptor, meaning its endogenous ligand was unknown at the time of discovery. It is expressed in various tissues and organs, including the brain, spinal cord, immune system, and reproductive system. Initially classified as an orphan receptor, GPR17 was later found to be activated by two endogenous ligands: uracil nucleotides (UDP and UDP-glucose) and cysteinyl leukotrienes (CysLTs), including leukotriene D4 (LTD4). These ligands bind to GPR17 with varying affinities and activate distinct signaling pathways. In summary, GPR17 is a G protein-coupled receptor with diverse physiological functions, including roles in central nervous system myelination, immune regulation, and reproductive physiology. Dysregulation of GPR17 signaling is implicated in various clinical conditions, highlighting its potential as a therapeutic target for neurological disorders, inflammatory diseases, and reproductive disorders

Structural Features:

GPR17, like other GPCRs, consists of seven transmembrane domains connected by three extracellular and three intracellular loops, with an extracellular N-terminus and an intracellular C-terminus. This structure allows GPR17 to interact with extracellular ligands and activate intracellular signaling pathways.

Physiological Functions:

1.   Central Nervous System: GPR17 is highly expressed in the central nervous system, particularly in regions involved in myelination, such as oligodendrocytes, astrocytes, and neurons. It has been implicated in regulating oligodendrocyte differentiation, myelination, and remyelination processes.

2.   Immune System: GPR17 is expressed in immune cells, including microglia, macrophages, and T cells, where it modulates immune responses, inflammation, and cytokine production. Its role in immune regulation suggests involvement in inflammatory and autoimmune disorders.

3.   Reproductive System: GPR17 is expressed in the testes and ovaries, where it may play a role in reproductive physiology and gametogenesis. Its specific functions in the reproductive system are still being elucidated.

Clinical Implications:

1.   Neurological Disorders: Dysregulation of GPR17 signaling has been implicated in neurological disorders associated with demyelination, such as multiple sclerosis. Modulating GPR17 activity may have therapeutic potential for promoting remyelination and neuroprotection.

2.   Inflammatory Disorders: GPR17 is involved in immune regulation and inflammation, suggesting potential implications in inflammatory diseases and autoimmune conditions. Targeting GPR17 may offer therapeutic strategies for managing inflammation.

3.   Reproductive Disorders: Although less well-studied, alterations in GPR17 function may contribute to reproductive disorders or fertility issues. Further research is needed to understand its specific roles in the reproductive system.

Therapeutic Potential:

1.   Multiple Sclerosis: Developing GPR17 modulators as potential therapeutics for promoting remyelination and neuroprotection in multiple sclerosis and other demyelinating disorders.

2.   Inflammatory Diseases: Targeting GPR17 signaling pathways to modulate immune responses and inflammation in inflammatory and autoimmune diseases.

3.   Reproductive Medicine: Investigating the role of GPR17 in reproductive physiology and fertility to identify potential targets for reproductive interventions or contraceptives.