The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
The Discovery of GSK2251052: A First-in-Class Boron ... - Anacor
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Genomic Revolution did not Improve Antibacterial Lead<br />
Identification: Results <strong>of</strong> GSK’s Target-based HTS<br />
70 HTS were conducted on the most<br />
promis<strong>in</strong>g essential gene targets<br />
GSK library conta<strong>in</strong>ed ~500K<br />
compounds<br />
Only 16 HTS campaigns yielded any hits<br />
Only 5 leads were developed<br />
– Peptide deformylase (PDF)<br />
– Enoyl-acyl carrier prote<strong>in</strong> reductase (FabI)<br />
– 3-ketoacyl-acyl carrier prote<strong>in</strong> III (FabH)<br />
– Methionyl tRNA synthetase (MetRS)<br />
– Phenylalanyl tRNA synthetase (PheRS)<br />
Better leads already existed for PDF<br />
FabI and MetRS were not broad<br />
spectrum and subsequently partnered<br />
with biotech<br />
FabH did not advance beyond lead<br />
Only PheRS was pursued<br />
7<br />
Nat Rev Drug Discov. 2007;6,29-40
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