Introduction of CCR-2

CCR-2 (alternatively known as monocyte chemoattractant protein 1 receptor, MCP-1-R) is a G protein-coupled receptor, which is encoded by the CCR2 gene in human. The ligands of CCR-2 receptor include CCL2, CCL7, CCL13, and beta-defensin DEFB106A/DEFB106B. CCR-2 is expressed on both hematopoietic cells such as macrophages, and nonhematopoietic cells such as endothelial cells, fibroblasts, and mesenchymal stem cells. It is the main functional receptor for CCL2, which specifically mediates monocyte chemotaxis.

Function of CCR-2 Membrane Protein

The CCL2-mediated CCR-2 activation leads to the activation of intracellular signaling cascades which mediate chemotactic response. CCR-2 has an effect on both pro-inflammatory (mediated by APC and T cells) and anti-inflammatory (mediated by regulatory T cells) process. This receptor plays a role in the inflammatory response against tumors, as well as in monocyte infiltration of inflammatory diseases such as rheumatoid arthritis. CCR-2 also mediate agonist-dependent calcium mobilization and inhibition of adenylyl cyclase. It has been reported that CCR-2 plays a role in various diseases such as allergic asthma, and prostate cancer. Thus, CCL-2/CCR-2 is supposed to be a potential target for prostate cancer treatment. Moreover, CCR2 antagonists are proved to be potential therapeutic agents in preventing, treating, or ameliorating a CCR2-mediated inflammatory disease such as psoriasis, rheumatoid arthritis, uveitis, asthma, multiple sclerosis, obesity, and chronic obstructive pulmonary disease. Recently, CCR-2 is demonstrated as a critical factor in balancing the bone remodeling process and supposed to be a therapeutic target in postmenopausal bone loss.

Application of CCR-2 Membrane Protein in Literature

1. Gale J.D., et al. A CCR2/5 Inhibitor, PF-04634817, Is Inferior to Monthly Ranibizumab in the Treatment of Diabetic Macular Edema. Invest Ophthalmol Vis Sci. 2018, 59(6): 2659-2669. PubMed ID: 29847672

Authors in this group evaluated the efficacy and safety of PF-04634817, an oral CCR2/5 dual antagonist, versus intravitreal ranibizumab, in adult subjects with DME. The result indicated that treatment with oral CCR2/5 receptor dual antagonist PF-04634817 was associated with a modest improvement in BCVA

2. Deci M.B., et al. Modulating macrophage polarization through CCR2 inhibition and multivalent engagement. Mol Pharm. 2018, 15(7): 2721-2731. PubMed ID: 29791797

This article demonstrates that CCR2 inhibition polarizes macrophages towards an inflammatory M1 phenotype and that multivalent engagement of CCR2 increases the effects of 58C-scFv on polarization and migration. These data provide important insights into the role of multivalency in modulating binding, downstream signaling, and cellular fate.

3. D'Antoni M.L, et al. Improved Cognitive Performance and Reduced Monocyte Activation in Virally Suppressed Chronic HIV Following Dual CCR2 and CCR5 Antagonism. J Acquir Immune Defic Syndr. 2018, 79(1): 108-116. PubMed ID: 29781885

This article focuses on the evaluation of changes in neuropsychological (NP) performance and in plasma and cell surface markers of peripheral monocyte activation/migration following treatment with cenicriviroc (CVC), a dual C-C chemokine receptor type 2 (CCR2) and type 5 (CCR5) antagonist, in treatment-experienced, HIV-infected individuals.

4. Fujimura N., et al. CCR2 inhibition sequesters multiple subsets of leukocytes in the bone marrow. Sci Rep. 2015, 5: 11664. PubMed ID: 26206182

This study demonstrates the central role CCR2 plays in mediating leukocyte mobilization from the BM and suggests a role for CCR2 inhibition in managing monocytes / macrophages-mediated chronic inflammatory conditions.

5. Morganti J.M, et al. CCR2 antagonism alters brain macrophage polarization and ameliorates cognitive dysfunction induced by traumatic brain injury. J Neurosci. 2015, 35(2): 748-60. PubMed ID: 25589768

This article indicates that therapeutically targeting the CCR2(+) subset of monocytes / macrophages may provide a new avenue of clinical intervention following TBI.

CCR-2 Preparation Options

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