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Solid-phase synthesis of c(RGDfK) derivatives: on-resin cyclisation and lysine functionalisation
Catherine F McCusker1, Philip J Kocienski, F Thomas Boyle
1Department of Chemistry, Leeds University, LS2 9JT, Leeds, UK.
Bioorganic & Medicinal Chemistry Letters
|February 15, 2002
Abstract:
The cyclic pentapeptide c(RGDfK), a selective ligand for the alpha(v)beta3 integrin, was synthesised on solid phase. All synthetic operations including the cyclisation step and the appendage of the Bolton-Hunter reagent was conducted on-resin.