Structural genomics and drug discovery: all in the family

被引:30
作者
Weigelt, Johan [1 ]
McBroom-Cerajewski, Linda D. B. [2 ]
Schapira, Matthieu [2 ,3 ]
Zhao, Yong [2 ]
Arrowmsmith, Cheryl H. [2 ,4 ,5 ]
机构
[1] Karolinska Inst, Struct Genom Consortium, MBB SGC, S-17177 Stockholm, Sweden
[2] Univ Toronto, Struct Genom Consortium, Toronto, ON M5G 1L5, Canada
[3] Univ Toronto, Dept Pharmacol, Toronto, ON M5G 1L5, Canada
[4] Univ Toronto, Ontario Canc Inst, Toronto, ON M5S 1A1, Canada
[5] Univ Toronto, Dept Med Biophys, Toronto, ON M5S 1A1, Canada
基金
英国惠康基金;
关键词
D O I
10.1016/j.cbpa.2008.01.045
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Structural genomics is starting to have an impact on the early stages of drug discovery and target validation through the contribution of new structures of known and potential drug targets, their complexes with ligands and protocols and reagents for additional structural work within a drug discovery program. Recent progress includes structures of targets from bacterial, viral and protozoan human pathogens, and human targets from known or potential druggable protein families such as, kinases, phosphatases, dehydrogenases/oxicloreductases, sulfo-, acetyl- and methyl-transferases, and a number of other key metabolic enzymes. Importantly, many of these structures contained ligands in the active sites, including for example, the first structures of target-bound therapeutics. Structural genomics of protein families combined with ligand discovery holds particular promise for advancing early stage discovery programs.
引用
收藏
页码:32 / 39
页数:8
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