Recent Progress in Combinatorial Solid Phase Synthesis: Techniques, Characterization and its Application in Drug Development

Publisher： Bentham Science Publishers

ISSN： 2212-7119

Source： Current Biochemical Engineering, Vol.4, Iss.1, 2017-02, pp. : 9-33

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Abstract

Combinatorial chemistry has rapidly evolved from its interest in the generation of largenumber of compounds for the discovery of actives amongst them in random screening procedure to apowerful designed combinatorial technology for the creation and optimization of pharmaceutical leadcompounds to produce drug candidates. The introduction of solid phase synthesis methods has richimpulse in this field, through automation and miniaturization. This review summarizes the presenttechniques of solid phase synthesis associated with combinatorial chemistry. The conventional methodsfor the synthesis of peptide libraries on solid support are split and mix synthesis, pre-mixed synthesisand parallel synthesis. In order to fulfil the increasing demand of synthetic peptides, severaltechniques have been developed, for example, pin synthesis, tea-bag synthesis, photolithography,SPOT synthesis, microchip synthesis, nanotechnology, lab-on-a-chip and bioinformatics and furthertheir deconvolution to access the contribution of every peptide to the desired biological activity. Thisreview also discusses about the combinatorial peptide library characterization and purity as well astheir applications in drug development.