Chemokine receptors on antigen-presenting cells

Chemokine receptors on antigen-presenting cells (APCs) are a specialized group of G protein-coupled receptors (GPCRs) that regulate the movement and positioning of dendritic cells, macrophages, and B cells within the immune system [1]. These receptors, such as CCR7, CXCR4, and CCR5, respond to specific chemokine ligands to direct APCs from peripheral tissues to lymphoid organs, a process essential for initiating adaptive immune responses [1, 4]. Beyond migration, these receptors influence APC maturation, phagocytosis, and the formation of the immunological synapse with T cells [1]. In various pathologies, chemokine receptors are implicated in the recruitment of inflammatory cells to sites of chronic inflammation or the infiltration of tumor-associated macrophages into the tumor microenvironment, which can promote cancer progression [3]. Furthermore, certain receptors like CCR5 and CXCR4 are well-known for their role as co-receptors for HIV-1 entry into host cells [2]. Therapeutic strategies targeting these receptors include small molecule antagonists and monoclonal antibodies designed to block ligand binding and subsequent intracellular signaling [4]. While drugs like Maraviroc and Plerixafor have reached clinical use, the high degree of redundancy in the chemokine system remains a significant hurdle for achieving high therapeutic efficacy in complex inflammatory diseases [3, 4]. References: [1] Forster R, et al. (2008). CCR7 and its ligands: balancing immunity and tolerance. Nature Reviews Immunology. [2] Alkhatib G, et al. (1996). CC CKR5: a RANTES, MIP-1alpha, MIP-1beta receptor as a fusion cofactor for macrophage-tropic HIV-1. Science. [3] Nagarsheth N, et al. (2017). Chemokines in cancer-associated inflammation, and therapeutic optimization. Nature Reviews Cancer. [4] IUPHAR/BPS Guide to PHARMACOLOGY. Chemokine receptors.

Other names

Chemokine receptorsCC chemokine receptorsCXC chemokine receptorsG protein-coupled receptors on APCs

Antagonism of chemokine binding to G protein-coupled receptors to inhibit cellular migration and signaling.