Target intelligence / Profile preview

Brain vascular pericyte and smooth muscle cell surface receptors

Molecular classification
Receptor, Tyrosine kinase receptor, G protein-coupled receptor, Ion channel, Other
01

Overview

Brain vascular pericyte and smooth muscle cell surface receptors represent a functional class of proteins essential for the maintenance and regulation of the neurovascular unit (Zlokovic, Neuron, 2011; PubMed: 21943591). These receptors, including Platelet-Derived Growth Factor Receptor Beta (PDGFRB) on pericytes and Notch3 on smooth muscle cells, mediate critical signaling pathways for vascular development, blood-brain barrier (BBB) integrity, and vasomotor tone (Sweeney et al., Nature Medicine, 2019; PubMed: 30643284). In neurodegenerative conditions such as Alzheimer's disease, the loss of pericyte receptor signaling is linked to BBB breakdown and cognitive decline. Mutations in smooth muscle receptors like Notch3 cause hereditary stroke syndromes such as CADASIL (Joutel et al., Nature, 1996; PubMed: 8875936). Pharmacological targeting of these receptors is explored for stabilizing the cerebral vasculature and controlling angiogenesis in brain tumors. Agents like Imatinib target PDGFRB, while calcium channel blockers like Nifedipine modulate smooth muscle cell activity (PubChem CID 5291; StatPearls). Therapeutic strategies also investigate these receptors for enhancing the clearance of metabolic waste like amyloid-beta from the brain. However, therapeutic challenges include the risk of systemic vascular toxicity and the potential for exacerbating BBB permeability if signaling is improperly modulated.

Other names
Mural cell surface receptorsCerebral perivascular cell receptorsNeurovascular unit mural receptorsBrain mural cell surface proteins
02

Mechanism of action

Modulation of mural cell signaling pathways, including inhibition of receptor tyrosine kinases (e.g., PDGFRB), antagonism of Notch signaling, and regulation of voltage-gated calcium channels (PubMed: 30643284, 8875936).

03

Biological functions

Blood-brain barrier maintenanceVascular tone regulationAngiogenesisNeurovascular couplingPericyte recruitmentCell proliferationExtracellular matrix deposition
04

Disease associations

Alzheimer's diseaseCADASILStrokeVascular dementiaFahr's diseaseGlioblastomaNeurodegenerative diseaseInflammation
05

Safety considerations

Blood-brain barrier disruptionSystemic hypotensionCerebral hemorrhageImpaired neurovascular couplingEdemaTherapeutic challenges in crossing the blood-brain barrier
06

Interacting drugs

6 more in the full profile.

07

Biomarkers

Soluble PDGFR-beta (sPDGFRB)Notch3 ectodomainAlpha-smooth muscle actin (ACTA2)NG2 (CSPG4)Regulator of G-protein signaling 5 (RGS5)CD13 (ANPEP)

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