An improved synthesis of a selective αvβ3-integrin antagonist cyclo(-RGDfK-)

✍ Scribed by Xuedong Dai; Zhuang Su; Jun O Liu

• Book ID: 104210673
• Publisher: Elsevier Science
• Year: 2000
• Tongue: French
• Weight: 118 KB
• Volume: 41
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(00)01060-1

✦ Synopsis

The cyclic pentapeptide cyclo(-Arg-Gly-Asp-d-Phe-Lys-) is a highly potent and selective inhibitor for the a v b 3 integrin. A related compound, cyclo(-Arg-Gly-Asp-d-Phe-Val-), is a promising anticancer drug candidate; it inhibits angiogenesis and induces apoptosis in vascular cells. We have developed an improved solid-phase synthesis based on Kessler's procedure to aord cyclo(-RGDfK-) peptide in high purity and high yield in a multi-gram scale. This improved synthesis is environmentally friendly and may be generally applicable to other related cyclic peptide syntheses.