2-[ methyl-11C]Methoxyestradiol

Excerpt

Endothelial cells are important cells in angiogenesis (1). Tumor growth requires the formation of new blood vessels. Potent angiogenic factors (e.g., vascular endothelial growth factor and basic fibroblast growth factor) induce proliferation, sprouting, migration, and tube formation of endothelial cells (2). 2-Methoxyestradiol (2-ME), an endogenous metabolite of 17β-estradiol, inhibits proliferating tumor cells and angiogenesis in vitro and in vivo (3, 4). It also inhibits the proliferation of endothelial cells and has low affinity for estrogen receptors. Huang et al. (5) demonstrated that the anti-proliferation effect of 2-ME may be the result of its inhibition of superoxide dismutase (SOD) and induction of apoptosis. Inhibition of SOD leads to free radical–mediated damage to mitochondrial membranes resulting in apoptosis. 2-[methyl-¹¹C]Methoxyestradiol ([¹¹C]2-ME) has been evaluated as an imaging probe to study angiogenesis (6).