Proposed scheme for the anti-angiogenic activities of PZ-DHA

Proposed scheme for the anti-angiogenic activities of PZ-DHA. PZ-DHA inhibits angiogenesis by inhibiting endothelial cell proliferation, migration, and tubule formation. The antiproliferative effects of PZ-DHA on endothelial cells are mediated through Rho GTPase-driven G1 arrest through the p53-p21 axis, as well as inhibition of upstream and downstream components of the PI3K/Akt/mTOR signaling pathway. PZ-DHA inhibits endothelial cell migration and differentiation by inhibiting VEGF-induced activation of small molecular Rho GTPase and activation of PDK1, cyclin D3, and mTOR. Akt: protein kinase B; AP: activator protein; Cdc42, Rac1/2/3, and RhoA: Rho family small GTPases; CRE: cAMP (cyclic adenosine monophosphate) response element; CREB: cAMP response element binding protein; GSK3-β: glycogen synthase kinase 3-β; mTOR: mammalian target of rapamycin; p21: cyclin-dependent kinase inhibitor 1; PDK1: phosphoinositide-dependent kinase-1; PI3K: phosphoinositide 3-kinase; PIP2: phosphatidylinositol-4,5-bisphosphate; PIP3: phosphatidylinositol-3,4,5-trisphosphate; PTEN: phosphatase and tensin homolog; PZ-DHA: phloridzin docosahexaenoate; ROCK: Rho-associated protein kinase; RTK: receptor tyrosine kinase; VEGF: vascular endothelial growth factor; VEGFR2: vascular endothelial growth factor receptor

Publication

Phloridzin Docosahexaenoate, an Omega-3 Fatty Acid Ester of a Flavonoid Precursor, Inhibits Angiogenesis by Suppressing Endothelial Cell Proliferation, Migration, and Differentiation (2024) Wasundara Fernando, et al. Biomolecules. 2024 Jul;14(7). Figure: F7. Homo sapiens

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