Medical and therapeutic value of gold has
been recognized thousands of years ago, but its rational
use in medicine has not begun until the early 1920s.
Cisplatin is one of the first metal-containing compounds
with anti-cancer activity discovered in the 1960s.
Despite the fact that cisplatin treatment is efficient for
several types of solid tumors, its effectiveness is limited
by toxic side effects and tumor resistance that often leads
to the occurrence of secondary malignancies. Since
gold(III) is isoelectronic with platinum(II) and
tetracoordinate gold(III) complexes have the same
square-planar geometries as cisplatin, the anticancer
activity of gold(III) compounds has been investigated.
Previous studies suggested that, in contrast to cisplatin,
gold complexes target proteins but not DNA. Recently,
we have investigated gold(III) dithiocarbamates for their
anticancer activity and showed that their primary target
is the proteasome. Treatment of human breast tumorbearing
nude mice with a gold(III) dithiocarbamate
complex resulted in significant inhibition of tumor
growth, associated with proteasome inhibition and
massive apoptosis induction in vivo. Better
understanding of physiological processing of gold
compounds will provide a rational basis for their further
development into novel anticancer drugs
