Target intelligence / Profile preview

Proteoglycan-modified stromal receptor

Molecular classification
Receptor, Proteoglycan, Cell surface glycoprotein
01

Overview

The Proteoglycan-modified stromal receptor is a key regulatory protein complex found on the surface of metastatic cancer-associated fibroblasts (mCAFs). It plays a pivotal role in the tumor microenvironment by integrating signals that promote extracellular matrix remodeling, epithelial-mesenchymal transition, and immune suppression, all of which facilitate the spread of cancer cells. The receptor is characterized by its specific proteoglycan modifications, which are necessary for its pro-metastatic activity. The small molecule Akos is a first-in-class inhibitor designed to selectively target this receptor, effectively reprogramming the stroma to halt the metastatic cascade. Preclinical studies have demonstrated that blocking this receptor can significantly reduce tumor growth and completely prevent the formation of metastatic foci across various solid tumor types.

Other names
Proteoglycan-modified receptor in mCAFMetastatic CAF proteoglycan receptormCAF-specific proteoglycan receptor
02

Biological functions

Extracellular matrix remodelingEpithelial-mesenchymal transition (EMT) inductionImmune evasionCell migrationCell invasionSignal transduction
03

Disease associations

CancerMetastasisTumor microenvironment progression
04

Safety considerations

Potential for systemic effects on normal fibroblast function (though Akos shows high selectivity)Therapeutic challenges related to TME heterogeneity
05

Interacting drugs

Akos
06

Biomarkers

mCAF-specific proteoglycan expressionEMT markers (e.g., Vimentin, N-cadherin)Stromal ECM remodeling signatures

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