Abstract:
:In light of the low success rate of target-based genomics and HTS (High Throughput Screening) approaches in anti-infective drug discovery, in silico structure-based drug design (SBDD) is becoming increasingly prominent at the forefront of drug discovery. In silico SBDD can be used to identify novel enzyme inhibitors rapidly, where the strength of this approach lies with its ability to model and predict the outcome of protein-ligand binding. Over the past 10 years, our group have applied this approach to a diverse number of anti-infective drug targets ranging from bacterial D-ala-D-ala ligase to Plasmodium falciparum DHODH. Our search for new inhibitors has produced lead compounds with both enzyme and whole-cell activity with established on-target mode of action. This has been achieved with greater speed and efficiency compared with the more traditional HTS initiatives and at significantly reduced cost and manpower.
journal_name
Parasitologyjournal_title
Parasitologyauthors
Cunningham F,McPhillie MJ,Johnson AP,Fishwick CWdoi
10.1017/S0031182013000693subject
Has Abstractpub_date
2014-01-01 00:00:00pages
17-27issue
1eissn
0031-1820issn
1469-8161pii
S0031182013000693journal_volume
141pub_type
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