CC Chemokine Receptor 1 Antibodies
C-C chemokine receptor 1 (CCR1), encoded by CCR1, is a class A G protein-coupled receptor activated by several endogenous chemokines, including CCL3, CCL5, CCL7, and CCL15. It couples predominantly to Gi/o, inhibiting adenylyl cyclase and activating pathways that control intracellular calcium, adhesion, and directional cell migration. CCR1 is expressed on monocytes, macrophages, and subsets of granulocytes and lymphocytes. It helps recruit leukocytes to inflamed tissues and has been implicated in rheumatoid arthritis and other inflammatory disorders. Agonist exposure can induce receptor desensitization and internalization, with the extent of these responses depending on the ligand and cellular context. CCR1 also contributes to interactions between myeloma cells and the bone marrow microenvironment in preclinical models. The oral small-molecule antagonists CCX354-C and MLN3897 were evaluated in phase 2 trials for rheumatoid arthritis, with mixed results across studies. No CCR1-selective antagonist is currently approved for therapeutic use. For more information on CCR1 pharmacology please refer to the IUPHAR database. For further reading refer to:
Bachelerie F, Ben-Baruch A, Burkhardt AM, Combadiere C, Farber JM, Graham GJ, Horuk R, Sparre-Ulrich AH, Locati M, Luster AD, Mantovani A, Matsushima K, Murphy PM, Nibbs R, Nomiyama H, Power CA, Proudfoot AE, Rosenkilde MM, Rot A, Sozzani S, Thelen M, Yoshie O, Zlotnik A. International Union of Basic and Clinical Pharmacology. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors. Pharmacol Rev. 2013 Nov 11;66(1):1-79. doi: 10.1124/pr.113.007724. Print 2014. Review. Erratum in: Pharmacol Rev. 2014 Apr;66(2):467. PubMed PMID: 24218476; PubMed Central PMCID: PMC3880466.