Falcipain inhibitors as potential therapeutics for resistant strains of malaria: a patent review

Abstract

Introduction: There is an urgent need to discover new antimalarial drugs due to emergence of resistance in the parasite to the existing drugs. Malarial cysteine proteases falcipin-2 (FP-2) and falcipain-3 (FP-3) are attractive targets for antimalarial chemotherapy. The structures and functions of FP-2/3, their binding domains and their interactions with small- and macro-molecules are well studied. These studies could provide important insight into rational designing of FP inhibitors as potential antimalarial drugs.

Areas covered: This review is focused on a selection of interesting patents published during 1999 – 2011 on peptidic and nonpeptidic chemotypes of the FP-2/FP-3 inhibitors.

Expert opinion: It is a known fact that malaria is a serious health problem worldwide due to the emergence of resistant strains. Hence, development of novel, potent and affordable antimalarial drugs devoid of side effects is of great significance and in great demand. FPs, the malarial cysteine proteases are potential targets for development of new antimalarial drugs. Assessing the available literature on FP-2/3 and their inhibitors it could be speculated that these inhibitors have the potential to enter the clinical stages of development for the treatment of malaria in the years to come.

Keywords::

• cysteine protease
• falcipain
• falcipain-2
• falcipain-3
• malaria
• Plasmodium falciparum
• trophozoite cysteine protease

Notes

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