Design, synthesis, and biological evaluation of multiple targeting antimalarials.
10.1016/j.apsb.2021.05.008
- Author:
Yiqing YANG
1
;
Tongke TANG
2
;
Xiaolu LI
3
;
Thomas MICHEL
4
;
Liqin LING
5
;
Zhenghui HUANG
2
;
Maruthi MULAKA
5
;
Yue WU
1
;
Hongying GAO
1
;
Liguo WANG
1
;
Jing ZHOU
6
;
Brigitte MEUNIER
4
;
Hangjun KE
5
;
Lubin JIANG
2
;
Yu RAO
1
Author Information
1. MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University, Beijing 100084, China.
2. Unit of Human Parasite Molecular and Cell Biology, Key Laboratory of Molecular Virology and Immunology, Institut Pasteur of Shanghai, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 200031, China.
3. Department of Biochemistry and Molecular Biology, State Key Laboratory of Medical Molecular Biology, Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100005, China.
4. Institute for Integrative Biology of the Cell (I2BC), CEA, CNRS, Université Paris-Saclay, Gif-sur-Yvette 91198, France.
5. Center for Molecular Parasitology, Department of Microbiology and Immunology, Drexel University College of Medicine, Philadelphia, PA 19129, USA.
6. Department of Laboratory Medicine, West China Hospital, Sichuan University, Chengdu 610041, China.
- Publication Type:Journal Article
- Keywords:
Antimalarial inhibitors;
Drug design;
Mechanism of action;
Membrane proteins;
Multiple targeting compounds
- From:
Acta Pharmaceutica Sinica B
2021;11(9):2900-2913
- CountryChina
- Language:English
-
Abstract:
Malaria still threatens global health seriously today. While the current discoveries of antimalarials are almost totally focused on single mode-of-action inhibitors, multi-targeting inhibitors are highly desired to overcome the increasingly serious drug resistance. Here, we performed a structure-based drug design on mitochondrial respiratory chain of
