A Bioinorganic Approach to Fragment-Based Drug Discovery Targeting Metalloenzymes
نویسندگان
چکیده
منابع مشابه
Fragment-Based Drug Discovery
Fragment-based drug discovery (FBDD), while still a relatively new approach, has been so successful for identifying ligands for protein targets that it is alreadywidely regarded as representing a sea-change in drug discovery techniques. The strategy involves identifying small (typically ,300Da), low-affinity ligands (‘fragments’) and combining or expanding these to produce larger, higher-affini...
متن کامل1 Introduction to Fragment - based Drug Discovery
Fragment screening is the process of identifying relatively simple, often weakly potent, bioactivemolecules. It is gainingwide acceptance as a successful hit-finding technique both in its own right and as a method of finding hit molecules when traditional high-throughput screening (HTS) methods fail. Fragment hits are typically highly ‘ligand efficient’, i.e. possess a high binding affinity per...
متن کاملTethering: fragment-based drug discovery.
The genomics revolution has provided a deluge of new targets for drug discovery. To facilitate the drug discovery process, many researchers are turning to fragment-based approaches to find lead molecules more efficiently. One such method, Tethering1, allows for the identification of small-molecule fragments that bind to specific regions of a protein target. These fragments can then be elaborate...
متن کاملFragment approaches in structure-based drug discovery
There has been considerable interest recently in what is known as ;fragment-based lead discovery'. The novel feature of the approach is to begin with small low-affinity compounds. The main advantage is that a larger potential chemical diversity can be sampled with fewer compounds, which is particularly important for new target classes. The approach relies on careful design of the fragment libra...
متن کاملExperiences in fragment-based drug discovery.
Fragment-based drug discovery (FBDD) has become established in both industry and academia as an alternative approach to high-throughput screening for the generation of chemical leads for drug targets. In FBDD, specialised detection methods are used to identify small chemical compounds (fragments) that bind to the drug target, and structural biology is usually employed to establish their binding...
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ژورنال
عنوان ژورنال: Accounts of Chemical Research
سال: 2017
ISSN: 0001-4842,1520-4898
DOI: 10.1021/acs.accounts.7b00242