The Plasmodium falciparum cysteine protease falcipain-2(FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC50 value of 0.44 μ...The Plasmodium falciparum cysteine protease falcipain-2(FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC50 value of 0.44 μmol L–1. The most exciting finding is that both in vitro and in vivo, NP1024 directly targets FP-2 in malaria parasite-infected erythrocytes as a natural fluorescent probe, thereby paving the way for an integration of malaria diagnosis and treatment.展开更多
基金supported by the National Key Research and Development Program (2016YFA0502304 to H.L.)the National Natural Science Foundation of China (81825020)+5 种基金the National Science & Technology Major Project “Key New Drug Creation and Manufacturing Program”, China (2018ZX09711002)the Fundamental Research Funds for the Central UniversitiesSpecial Program for Applied Research on Super Computation of the NSFC-Guangdong Joint Fund (the second phase) (U1501501)Professor of Chang Jiang Scholars Program (to W.Z.)the Natural Science Foundation of Zhejiang Province (LY15H190007)sponsored by the National Program for Special Supports of Eminent Professionals and National Program for Support of Top-notch Young Professionals。
文摘The Plasmodium falciparum cysteine protease falcipain-2(FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC50 value of 0.44 μmol L–1. The most exciting finding is that both in vitro and in vivo, NP1024 directly targets FP-2 in malaria parasite-infected erythrocytes as a natural fluorescent probe, thereby paving the way for an integration of malaria diagnosis and treatment.
