Recent Progress in Combinatorial Solid Phase Synthesis: Techniques, Characterization and its Application in Drug Development
Combinatorial chemistry has rapidly evolved from its interest in the generation of large
number of compounds for the discovery of actives amongst them in random screening procedure to a
powerful designed combinatorial technology for the creation and optimization of pharmaceutical lead
compounds to produce drug candidates. The introduction of solid phase synthesis methods has rich
impulse in this field, through automation and miniaturization. This review summarizes the present
techniques of solid phase synthesis associated with combinatorial chemistry. The conventional methods
for the synthesis of peptide libraries on solid support are split and mix synthesis, pre-mixed synthesis
and parallel synthesis. In order to fulfil the increasing demand of synthetic peptides, several
techniques have been developed, for example, pin synthesis, tea-bag synthesis, photolithography,
SPOT synthesis, microchip synthesis, nanotechnology, lab-on-a-chip and bioinformatics and further
their deconvolution to access the contribution of every peptide to the desired biological activity. This
review also discusses about the combinatorial peptide library characterization and purity as well as
their applications in drug development.
Keywords: Solid phase peptide synthesis, combinatorial chemistry, deconvolution, high throughput screening, pharmaceutical.
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