Target intelligence / Profile preview

Neuropilin-1–Platelet-derived growth factor receptor beta complex (NRP-1–PDGFRβ complex)

Target
NRP-1–PDGFRβ complex
Molecular classification
Receptor complex, Co-receptor, Receptor tyrosine kinase, Non-tyrosine kinase receptor
01

Overview

The Neuropilin-1–Platelet-derived growth factor receptor beta (NRP-1–PDGFRβ) complex is a functional protein assembly that plays a pivotal role in vascular biology and tissue repair. Neuropilin-1 (NRP-1) acts as a versatile co-receptor, enhancing the signaling of Platelet-derived growth factor receptor beta (PDGFRβ) in response to ligands such as PDGF-BB and PDGF-D [1, 3, 5]. This interaction is crucial for the migration and proliferation of mesenchymal cells, including vascular smooth muscle cells and pericytes, which are essential for blood vessel maturation and stabilization [1, 4]. In the context of oncology, particularly in hepatocellular carcinoma, the formation of this complex has been linked to vascular normalization, a process that improves blood flow and immune cell infiltration into tumors [7, 10]. Conversely, overactivation of the complex is associated with pathological fibrosis and tumor progression in various cancers [3, 14, 15]. Therapeutic agents like Lenvatinib have been shown to modulate the formation of this complex, shifting NRP-1 from its association with VEGFR2 to PDGFRβ to promote a more stable vascular phenotype [7]. Understanding the dynamics of the NRP-1–PDGFRβ complex is vital for developing targeted therapies that balance anti-angiogenic effects with vascular stabilization.

Other names
NRP1-PDGFRB complexNeuropilin-1/PDGFR-beta complexNRP1-PDGFRβ heterocomplexNRP1-PDGFRB signaling complex
02

Mechanism of action

Modulation of receptor heterodimerization and downstream signaling pathways (e.g., Crkl-C3G-Rap1 or p130Cas) to regulate vascular stability, pericyte recruitment, and mesenchymal cell activity.

03

Biological functions

Signal transductionAngiogenesisCell migrationCell proliferationVascular remodelingFibrosisVascular normalization
04

Disease associations

CancerInflammationCardiovascular diseaseLiver fibrosisHepatocellular carcinoma
05

Safety considerations

Vascular toxicityImpaired wound healingHypertensionThromboembolic eventsPotential for paradoxical pro-fibrotic effects
06

Interacting drugs

Lenvatinib

4 more in the full profile.

07

Biomarkers

NRP-1 expressionPDGFRβ phosphorylation (p-PDGFRβ)PDGF-BB levelsPDGF-D levelsPericyte coverage (e.g., alpha-SMA, Desmin)

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