Current perspectives in fragment-based lead discovery (FBLD)
作者： Bas Lamoree , Roderick E. Hubbard
DOI: 10.1042/EBC20170028
关键词:
摘要: It is over 20 years since the first fragment-based discovery projects were disclosed. The methods are now mature for most ‘conventional’ targets in drug such as enzymes (kinases and proteases) but there has also been growing success on more challenging targets, disruption of protein–protein interactions. main application to identify tractable chemical startpoints that non-covalently modulate activity a biological molecule. In this essay, we overview current practice discuss how they have had an impact lead – generating large number fragment-derived compounds clinical trials two medicines treating patients. addition, some recent applications biology providing tools investigate molecules, mechanisms systems.
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biochemistry.org参考文章(56)
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