化学
恶性疟原虫
硼酸
选择性
蛋白酶体
药理学
生物化学
化学合成
组合化学
体外
疟疾
免疫学
催化作用
医学
生物
作者
Chrislaine Withers‐Martinez,Elīna Līdumniece,Fiona Hackett,Christine R. Collins,Ziad Taha,Michael J. Blackman,Aigars Jirgensons
标识
DOI:10.1021/acs.jmedchem.4c01005
摘要
subtilisin-like serine protease 1 (PfSUB1) is essential for egress of invasive merozoite forms of the parasite, rendering PfSUB1 an attractive antimalarial target. Here, we report studies aimed to improve drug-like properties of peptidic boronic acid PfSUB1 inhibitors including increased lipophilicity and selectivity over human proteasome (H20S). Structure-activity relationship investigations revealed that lipophilic P
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