Target intelligence / Profile preview

Scavenger receptor cysteine-rich type 1 protein M130 (CD163) (CD163)

Target
CD163
Molecular classification
Receptor, Scavenger receptor, Other (Structural protein for beta-tubulin)
01

Overview

CD163 is a high-affinity scavenger receptor for hemoglobin-haptoglobin complexes, primarily expressed on the surface of M2-polarized macrophages and monocytes. It plays a critical role in the resolution of inflammation by clearing free hemoglobin and inducing the production of anti-inflammatory cytokines. The combination of "CD163 + β-tubulin" typically refers to a therapeutic strategy involving antibody-drug conjugates (ADCs) where CD163 serves as the cell-surface targeting receptor and a tubulin inhibitor (which targets β-tubulin) serves as the cytotoxic payload. This approach is designed to selectively deplete or reprogram tumor-associated macrophages (TAMs) or inflammatory macrophages, which are often associated with immunosuppression and poor prognosis in cancer and chronic inflammatory diseases. By delivering tubulin-disrupting agents directly to these specific immune cells, researchers aim to modulate the immune microenvironment and enhance anti-tumor or anti-inflammatory responses while minimizing systemic toxicity.

Other names
M130Hemoglobin scavenger receptorsCD163TUBBBeta-tubulin
02

Mechanism of action

Receptor-mediated endocytosis of the antibody-drug conjugate (ADC) upon binding to CD163, followed by lysosomal degradation and intracellular release of the payload (e.g., tubulin inhibitors like MMAE which bind to β-tubulin to disrupt microtubule polymerization and induce cell death).

03

Biological functions

Immune responseHemoglobin clearanceAnti-inflammatory responseMacrophage polarizationEndocytosisMicrotubule organization (via beta-tubulin)
04

Disease associations

CancerInflammationNon-alcoholic steatohepatitis (NASH)SepsisRheumatoid arthritisCardiovascular disease
05

Safety considerations

Potential for off-target depletion of resident tissue macrophages (e.g., Kupffer cells in the liver)Systemic toxicity if the payload is prematurely released from the linkerPotential for immunosuppression due to depletion of anti-inflammatory macrophage populations
06

Interacting drugs

Cymac-001 (anti-CD163-dexamethasone ADC)

3 more in the full profile.

07

Biomarkers

CD163 expression on M2-polarized macrophagesSoluble CD163 (sCD163) serum levelsCD163+ tumor-associated macrophage (TAM) densityBeta-tubulin III (TUBB3) expression (as a marker of resistance or neuronal damage)

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