Reference of Isoquinolin-6-ol. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Isoquinolin-6-ol, is researched, Molecular C9H7NO, CAS is 7651-82-3, about Orthosteric-allosteric dual inhibitors of PfHT1 as selective antimalarial agents. Author is Huang, Jian; Yuan, Yafei; Zhao, Na; Pu, Debing; Tang, Qingxuan; Zhang, Shuo; Luo, Shuchen; Yang, Xikang; Wang, Nan; Xiao, Yu; Zhang, Tuan; Liu, Zhuoyi; Sakata-Kato, Tomoyo; Jiang, Xin; Kato, Nobutaka; Yan, Nieng; Yin, Hang.
Artemisinin-resistant malaria parasites have emerged and have been spreading, posing a significant public health challenge. Antimalarial drugs with novel mechanisms of action are therefore urgently needed. In this report, we exploit a ′selective starvation′ strategy by inhibiting Plasmodium falciparum hexose transporter 1 (PfHT1), the sole hexose transporter in P. falciparum, over human glucose transporter 1 (hGLUT1), providing an alternative approach to fight against multidrug-resistant malaria parasites. The crystal structure of hGLUT3, which shares 80% sequence similarity with hGLUT1, was resolved in complex with C3361, a moderate PfHT1-specific inhibitor, at 2.3-Å resolution Structural comparison between the present hGLUT3-C3361 and our previously reported PfHT1-C3361 confirmed the unique inhibitor binding-induced pocket in PfHT1. We then designed small mols. to simultaneously block the orthosteric and allosteric pockets of PfHT1. Through extensive structure-activity relationship studies, the TH-PF series was identified to selectively inhibit PfHT1 over hGLUT1 and potent against multiple strains of the blood-stage P. falciparum. Our findings shed light on the next-generation chemotherapeutics with a paradigm-shifting structure-based design strategy to simultaneously target the orthosteric and allosteric sites of a transporter.
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Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method