Cysteine Proteinase Falcipain-2 Of P.falciparum Inhibitor Discovery And Relevant Inhibition Mechanisms Investigation

Malaria remains one of the most important infectious diseases in the word. In recent years, the alarming rise of drug-resistance among malarial is stimulating an urgent need to discover novel antimalarial drugs acting on new drug targets.The cysteine protease falcipain-2 from P. falciparum is an attractive and most promising target enzyme, which plays a key role in hemoglobin degradation in throphozoites. Suggesting this protein may be a valuable target for the design of novel antimalarial drugs. In this text, recombinant falcipain-2 was successfully cloned, expressed and purified in M15 E. coli. Moreover, a series of new compounds were discovered to demonstrate inhibitory activities against falcipain-2. The three compounds were 513,1024,1031 with IC50 values of 1.45,0.44,1.5μM. These compounds were discovered to be new falcipain-2 inhibitors based on their biological activities. It is expected that our findings could supply potent structure information for the discovery of the potential lead compound against the antimalarial drugs.