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G protein-coupled receptors (GPCRs) play important roles in inflammation. Inflammatory cells such as polymorphonuclear leukocytes (PMN), macrophages and monocytes express many GPCRs for classic chemoattractants and chemokines. These receptors are essential to the migration of phagocytes and their accumulation at sites of inflammation, where these cells can exacerbate inflammation but also contribute to its resolution. A number of GPCRs present in inflammatory cells also mediate transcription factor activation, resulting in the synthesis and secretion of inflammatory factors and, under certain conditions, molecules that suppress inflammation.
Inflammation is characterized by the cardinal signs of calor (heat), dolor (pain), rubor (redness), tumor (swelling) and function laesa (loss of function). These signs reflect tissue response to inflammatory factors that are either external or host-derived. GPCRs contribute directly to these clinical manifestations due to their wide presence and various functions. Inflammation is shaped not only by leukocytes that accumulate at the site of inflammation, but also by cells in specific tissues and organs such as synovial fibroblasts in the joints and microglial cells in the brain. Endothelial cells are actively involved in the process of inflammation and interact closely with leukocytes in all tissues. GPCRs expressed in these cells play significant roles in sensing the presence of chemoattractants, transducing signals which lead to the production of inflammatory cytokines, nociception, and regulation of intracellular and intercellular communications associated with increased blood flow and increased vascular endothelial permeability. Functions mediated by GPCRs can both exacerbate inflammation and promote the resolution.
An understanding of the signaling paradigms of GPCRs in inflammatory cells can facilitate translational research and development of improved anti-inflammatory therapies. Creative Biogene can offer the largest commercial portfolio of GPCR assay solutions for inflammation research areas. Select targets are shown - view more GPCR targets.
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