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Curr Opin Drug Discov Devel. 2008 Nov;11(6):762-70.

Advances in automatic, manual and microwave-assisted solid-phase peptide synthesis.

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Laboratorio Interdipartimentale di Chimica e Biologia dei Peptidi e Proteine, c/o Dipartimento di Chimica Organica Ugo Schiff', Polo Scientifico e Tecnologico dell Università di Firenze, Via della Lastruccia 13, I-50019 Sesto Fiorentino (FI), Italy.


Solid-phase strategies speed up the production of both short- and long-sequence peptides compared with solution methodologies. Therefore, solid-phase peptide synthesis (SPPS), proposed by Merrifield in the early 1960s, contributed to the 'Peptide Revolution' in the fields of diagnostics, and drug and vaccine development. Since then, peptide chemistry research has aimed to optimize these synthetic procedures, focusing on areas such as amide bond formation (the coupling step), solid supports and automation. Particular attention was devoted to the environmental impact of SPPS: the requirement for large amounts of organic solvents meant high costs for industrial peptide manufacturing that needed to be reduced. SPPS, alone or in hybrid technologies, has become strategic for the production of peptides as active pharmaceutical ingredients on a commercial scale.

[Indexed for MEDLINE]

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