Journal of Medicinal Chemistry p. 9703 - 9717 (2019)
Update date:2022-07-30
Topics:
Cain, Ricky
Salimraj, Ramya
Punekar, Avinash S.
Bellini, Dom
Fishwick, Colin W. G.
Czaplewski, Lloyd
Scott, David J.
Harris, Gemma
Dowson, Christopher G.
Lloyd, Adrian J.
Roper, David I.
Aminoacyl-tRNA synthetases are ubiquitous and essential enzymes for protein synthesis and also a variety of other metabolic processes, especially in bacterial species. Bacterial aminoacyl-tRNA synthetases represent attractive and validated targets for antimicrobial drug discovery if issues of prokaryotic versus eukaryotic selectivity and antibiotic resistance generation can be addressed. We have determined high-resolution X-ray crystal structures of the Escherichia coli and Staphylococcus aureus seryl-tRNA synthetases in complex with aminoacyl adenylate analogues and applied a structure-based drug discovery approach to explore and identify a series of small molecule inhibitors that selectively inhibit bacterial seryl-tRNA synthetases with greater than 2 orders of magnitude compared to their human homologue, demonstrating a route to the selective chemical inhibition of these bacterial targets.
View Morewebsite:http://www.weichichem.com
Contact:+8613912949432
Address:Fine Chemical Industrial Base,Wujiang town,He County,Anhui China.
website:http://www.sigmaaldrich.com
Contact:800 558-9160
Address:Industriestrasse 25CH-9471 Buchs SGSwitzerland
Shanghai Coupling Pharmaceutical R&D Co., Ltd.(expird)
Contact:+86 021 50106671
Address:403 Room No.4 Buiding, No. 526 Ruiqing Road, Shanghai Zhangjiang Hi-Tech Park
TIANJIN NORTH JINHENG CHEMICAL PLANT.
Contact:0086-22-59952083
Address:DongShigu Country In JiXian TianJin China
Zhejiang Hoshine Silicon Industry Co., Ltd.
Contact:86-573-89179966
Address:Zhapu Town, Pinghu City, Zhejiang, China
Doi:10.1016/j.jorganchem.2007.02.043
(2007)Doi:10.1002/ejic.201701361
(2018)Doi:10.1002/hlca.19620450224
(1962)Doi:10.1111/j.2042-7158.1958.tb10389.x
(1958)Doi:10.1016/j.tetlet.2007.03.150
(2007)Doi:10.1002/asia.201402463
(2014)