Increasing bacterial drug resistance and hard-to-eradicate opportunistic in
fections have created a need for new antibiotics. Sequencing of microbial g
enomes has yielded many new potential targets for antibacterial drug discov
ery. However, little is known about the biochemical activities of many of t
hese targets, making it difficult to develop HTS assays for them. Peptides
isolated by phage display can be used as 'surrogate ligands' in competition
assays for screening of targets of unknown function with small-molecule li
braries. These screening assays can be adapted into a variety of high-throu
ghput formats, including those based on radioactive, luminescence or fluore
scence detection.