Ra. Houghten et al., Drug discovery and vaccine development using mixture-based synthetic combinatorial libraries, DRUG DISC T, 5(7), 2000, pp. 276-285
The approaches and concepts that encompass combinatorial chemistry represen
t a paradigm shift in drug discovery and basic research. Viewed initially a
s a curiosity by the pharmaceutical industry, combinatorial chemistry appro
aches are now recognized as essential drug discovery tools that decrease th
e time taken for discovery and increase the throughput of chemical screenin
g by as much as 1000-fold. Although the use of mixture-based synthetic comb
inatorial libraries was one of the first approaches presented, its inherent
strengths are only recently being recognized. Numerous mixture-based libra
ries of peptides, peptidomimetics and heterocycles have been synthesized an
d deconvoluted using the positional scanning approach. Mixture-based librar
y approaches for drug discovery and vaccine development will be reviewed he
rein.