The completion of the human genome project has opened novel scientific aven
ues in functional genomics, structural genomics and proteomics. These areas
have a common goal: the identification of all the proteins acting and cros
s-talking in a single cell at a defined moment of its lifecycle. The expans
ion of these areas in bioscience has been facilitated by the rapid developm
ent of high throughput screening (HTS) methods which has, in turn, attracte
d the business community to make investments in this novel business segment
of biotechnology. By using these HTS methods, the hope is that novel targe
ts will be validated much more rapidly speeding up the development of novel
drugs. Numerous techniques and tools have emerged over the past decade for
the identification of small target-specific molecular ligands that exploit
a common feature: the exploration of molecular diversity using combination
al methods. While chemists developed new methods for rapidly and efficientl
y synthesising and screening large collections of small molecules, biologis
ts used recombinant DNA techniques for selecting displayed repertoires. To
this end, the discovery of new low molecular weight peptides is becoming in
creasingly important, not only as molecular tools for the understanding of
protein-protein interactions but also for the generation of lead compounds.