作者
Ashutosh Kumar, Arnout Voet, Kam YJ Zhang
发表日期
2012/10/1
来源
Current medicinal chemistry
卷号
19
期号
30
页码范围
5128-5147
出版商
Bentham Science Publishers
简介
Fragment based drug design has emerged as an effective alternative to high throughput screening for the identification of lead compounds in drug discovery in the past fifteen years. Fragment based screening and optimization methods have achieved credible success in many drug discovery projects with one approved drug and many more compounds in clinical trials. The fragment based drug design starts with the identification of fragments or low molecular weight compounds that generally bind with weak affinity to the target of interest. The fragments that form high quality interactions are then optimized to lead compounds with high affinity and selectivity. The weak affinity of fragments for their target requires the use of biophysical techniques such as nuclear magnetic resonance, X-ray crystallography or surface plasmon resonance to identify hits. These techniques are very sensitive and some of them provide …
学术搜索中的文章
A Kumar, A Voet, KYJ Zhang - Current medicinal chemistry, 2012