Solid-phase synthesis of c(RGDfK) derivatives: on-resin cyclisation and lysine functionalisation.
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.
McCusker
Catherine F
CF
Department of Chemistry, Leeds University, LS2 9JT, Leeds, UK.
Kocienski
Philip J
PJ
Boyle
F Thomas
FT
Schätzlein
Andreas G
AG
D003500:Cyclization; D039302:Integrin alphaVbeta3; D008024:Ligands; D008239:Lysine / Q000737:chemistry; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D012117:Resins, Synthetic / Q000737:chemistry
D039302:Integrin alphaVbeta3; D008024:Ligands; D010456:Peptides, Cyclic; D012117:Resins, Synthetic; C099250:cyclic (arginyl-glycyl-aspartyl-phenylalanyl-lysyl); D008239:Lysine