In the last few decades, advances in the cancer chemotherapy have been a marked success. A
large number of anticancer drugs currently in use include drugs based on platinum complexes such as
cisplatin, base analogues such as 5-florouracil and some ruthenium drugs. This review provides a bird’s
eye view of interaction of a number of clinically important drugs currently in use that show covalent or
non-covalent interaction with serum proteins. Platinum drug-cisplatin interacts covalently and alters the
function of the key plasma protease inhibitor molecule -alpha-2-macroglobulin and induces the conformational
changes in the protein molecule and inactivates it. 5-fluorouracil (5-FU) is extensively metabolized
and at physiological concentrations, is found to be associated with Human Serum Albumin (HSA).
Similarly ruthenium compounds bind tightly to plasma proteins- serum albumin and serum transferrin,
modifying their biological activity and increasing the toxicity of drug to cancer cells. Insight into varied
anticancer drug- protein interaction will go a long way in understanding in totality of the mechanism of
action of any anticancer drug and its possible effects/side effects.
Keywords: Alpha-2-macroglobulin, cisplatin, 5-FU, chemotherapeutic drugs, plasma proteins, new dimensions.
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