G protein-coupled receptors (GPCRs) on immune and inflammatory cells (GPCRs)

G protein-coupled receptors (GPCRs) on immune and inflammatory cells constitute a diverse superfamily of membrane proteins that serve as critical sensors for chemical gradients and inflammatory signals (StatPearls, 2023). These receptors, which include chemokine, leukotriene, and prostanoid receptors, coordinate the complex processes of leukocyte rolling, adhesion, and migration into tissues during an immune response (Frontiers in Immunology, 2018). Dysregulation of these GPCR-mediated pathways is a hallmark of various inflammatory and autoimmune conditions, such as asthma, rheumatoid arthritis, and multiple sclerosis, where excessive leukocyte infiltration leads to tissue damage (Nature Reviews Drug Discovery, 2004). Pharmacological intervention typically involves the use of small molecule antagonists or monoclonal antibodies to block receptor-ligand interactions, thereby dampening the inflammatory cascade. Notable examples include Maraviroc for HIV entry inhibition via CCR5 and Fingolimod for treating multiple sclerosis by modulating S1P receptors (Pharmacological Reviews, 2015). However, targeting these receptors requires careful consideration of their pleiotropic roles to avoid significant immunosuppression or off-target systemic effects.

Other names

7-transmembrane receptors on leukocytesGPCRs in inflammationImmune cell GPCRsInflammatory GPCRs

Antagonism of chemokine or lipid mediator receptors to inhibit leukocyte chemotaxis; modulation of sphingosine-1-phosphate receptors to regulate lymphocyte egress from lymphoid tissues (Nature Reviews Drug Discovery, 2004; Pharmacological Reviews, 2015).