Inhibition of Tumor-induced Angiogenesis
Boronic acid, and a series of boron-containing phenoxyacetanilide derivatives, have also been shown to greatly inhibit hypoxia-inducible factor (HIF) 1.111 HIFs are heterodimeric (α/β) transcriptional factors and are major physiological stimuli for expression of angiogenesis factors. Angiogenesis, the formation of new blood vessels sprouting from existing host capillaries, must occur for tumors to grow beyond a certain critical size. Inhibition of tumor-induced angiogenesis prevents growth of many types of solid tumors and provides a novel approach for cancer treatment; thus, HIF-1 is a target of antineoplastic therapy.
Induction of Cancer-cell Apoptosis
Sugar-borate esters act as boron vehicles, increasing the concentration of borate inside cancer cells relative to normal cells. Increased intracellular concentration of borate not only activates borate transporters but also leads to growth inhibition and apoptosis. In normal cells, the 2 latter, cell-destructive effects do not occur because the amount of borate present in a healthy diet, 1 to 10 mg/d, is easily exported from normal cells. Cancer cells, however, commonly overexpress sugar transporters and/or underexpress borate export, rendering sugar-borate esters as promising chemopreventive agents.112