发现一种针对恶性疟原虫半胱氨酸蛋白酶 falcipain-2 的天然荧光探针。
Discovery of a natural fluorescent probe targeting the Plasmodium falciparum cysteine protease falcipain-2.
机构信息
Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai, 200237, China.
Department of Natural Product Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 200433, China.
出版信息
Sci China Life Sci. 2020 Jul;63(7):1016-1025. doi: 10.1007/s11427-019-1581-2. Epub 2020 Feb 9.
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 IC value of 0.44 μmol L. 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.
恶性疟原虫半胱氨酸蛋白酶 falcipain-2（FP-2）是一种很有吸引力的抗疟靶点。在这里，我们发现天然化合物 NP1024 是 FP-2 的非肽类抑制剂，IC 值为 0.44 μmol·L。最令人兴奋的发现是，NP1024 无论是在体外还是在体内，都直接将 FP-2 作为天然荧光探针靶向感染疟原虫的红细胞，从而为疟疾诊断和治疗的整合铺平了道路。
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