Target intelligence / Profile preview

Cell surface F1-F0 ATP synthase (ATP synthase)

Target
ATP synthase
Molecular classification
Enzyme, Transporter, Receptor
01

Overview

Cell surface F1-F0 ATP synthase, also known as ectopic ATP synthase, is a form of the mitochondrial enzyme complex found on the plasma membrane of various cells, particularly endothelial cells. In this location, it serves as a high-affinity receptor for the anti-angiogenic protein angiostatin and plays a critical role in regulating extracellular ATP levels and intracellular pH (Moser et al., 1999, PNAS). These functions are essential for the proliferation, migration, and survival of endothelial cells during angiogenesis (Chi and Pizzo, 2006, Drug News Perspect). In cancer, the expression of this enzyme is significantly upregulated on the surface of tumor-associated endothelial cells, facilitating tumor vascularization and growth (Chang et al., 2012, Cancer Science). Targeting cell surface ATP synthase with inhibitors like angiostatin or specific antibodies has been shown to effectively suppress angiogenesis and induce apoptosis in tumor-associated vessels. Because the enzyme is selectively accessible on the surface of activated endothelial cells compared to the sequestered mitochondrial pool in normal tissues, it represents a promising target for site-specific anti-cancer therapies (Vantourout et al., 2010, Blood).

Other names
Ecto-ATP synthaseEctopic ATP synthaseAngiostatin receptorEcto-F1-F0-ATPaseCell surface mitochondrial ATP synthase
02

Mechanism of action

Inhibition of extracellular ATP synthesis and hydrolysis, leading to suppression of endothelial cell proliferation and migration.

03

Biological functions

Extracellular ATP synthesisExtracellular ATP hydrolysisAngiogenesis regulationIntracellular pH regulationSignal transduction
04

Disease associations

CancerCardiovascular diseaseInflammationObesity
05

Safety considerations

Potential cross-reactivity with mitochondrial ATP synthaseSystemic metabolic disruptionInhibition of normal wound healingPotential for off-target effects in tissues with high metabolic demand
06

Interacting drugs

Angiostatin

6 more in the full profile.

07

Biomarkers

Cell surface expression of ATP synthase beta subunit (ATP5B)Extracellular ATP/ADP ratioEndothelial cell proliferation markers (e.g., Ki-67) in tumor vasculature

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