Target intelligence / Profile preview

C-C motif chemokine ligand 2 (CCL2) (CCL2)

Target
CCL2
Molecular classification
Cytokine, Chemokine, CC chemokine family
01

Overview

C-C motif chemokine ligand 2 (CCL2), also known as Monocyte Chemoattractant Protein-1 (MCP-1), is a pivotal proinflammatory cytokine that recruits monocytes, memory T cells, and dendritic cells to sites of injury and infection. By binding to its primary receptor, CCR2, it triggers signaling cascades such as PI3K/Akt and MAPK that regulate cellular migration, survival, and proliferation. In disease contexts, CCL2 plays a critical role in chronic inflammation, organ fibrosis, and the development of an immunosuppressive tumor microenvironment that facilitates cancer metastasis and drug resistance. Therapeutic strategies targeting CCL2 include monoclonal antibodies like carlumab and synthesis inhibitors like bindarit, though clinical success has been hindered by the high degree of redundancy in the chemokine network and rebound effects where ligand levels increase following treatment. Consequently, while it remains a high-interest target for oncology and inflammatory diseases, achieving sustained pharmacological inhibition remains a significant therapeutic challenge.

Other names
Monocyte chemoattractant protein 1MCP-1Small inducible cytokine A2SCYA2Monocyte chemotactic and activating factorMCAFGDCF-2HC11HSMCR30SMC-CF
02

Mechanism of action

Neutralization of the chemokine ligand to prevent receptor binding; inhibition of ligand synthesis; disruption of the CCL2/CCR2 signaling axis.

03

Biological functions

ChemotaxisMonocyte recruitmentImmune responseInflammationCell proliferationCell survivalBasophil degranulationAngiogenesis
04

Disease associations

CancerInflammationFibrosisCardiovascular diseaseNeurodegenerative diseaseType 2 diabetesRheumatoid arthritisMultiple sclerosisAtherosclerosisNonalcoholic steatohepatitis (NASH)
05

Safety considerations

Compensatory ligand upregulation (rebound effect)Biological redundancy in the chemokine systemSusceptibility to infectionPotential for lack of clinical efficacy due to alternative recruitment pathways
06

Interacting drugs

Carlumab (CNTO 888)

2 more in the full profile.

07

Biomarkers

Serum CCL2 concentrationPlasma MCP-1 levelsUrinary CCL2 levelsCCL2 promoter hypomethylation

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