ABSTRACT

This review examines the anti-angiogenic and anti-cancer properties of Nanotetrac that exploit the novel small molecule receptor for thyroid hormone-Nanotetrac on αvβ3. Integrin αvβ3 controls a variety of intracellular and transcellular functions. It is a transmembrane structural protein that is differentially expressed/activated in tumor cells and dividing blood vessel cells. The anti-angiogenic activity of tetrac was confirmed to be present in the vascular supply to a variety of human tumor xenografts and was interpreted to reflect only the disruption of the thyroid hormone-integrin receptor interaction. The anti-cancer properties of Nanotetrac are broadly based in terms of mechanisms, despite initiation of the actions of the drug at a single target receptor on integrin αvβ3, and in this regard resemble the pluralistic anti-angiogenic actions of the drug. Nanotetrac is a prototypic anti-angiogenic and anti-cancer agent focused on a single, specific small molecule receptor site on the extracellular domain of αvβ3.