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

X. Dai, Z. Su, Jun Liu

Research output: Contribution to journalArticle

Abstract

The cyclic pentapeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys-) is a highly potent and selective inhibitor for the αvβ3 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 afford 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. (C) 2000 Elsevier Science Ltd.

Original languageEnglish (US)
Pages (from-to)6295-6298
Number of pages4
JournalTetrahedron Letters
Volume41
Issue number33
StatePublished - Aug 12 2000
Externally publishedYes

Fingerprint

Cyclic Peptides
Solid-Phase Synthesis Techniques
Integrins
Blood Vessels
Apoptosis
Peptides
Pharmaceutical Preparations
cyclo-DfKRG
cyclo(arginyl-glycyl-aspartyl-phenylalanyl-valyl)

Keywords

  • αvβ3-integrin antagonist
  • Cyclic RGD peptide
  • Solid-phase synthesis

ASJC Scopus subject areas

  • Biochemistry
  • Organic Chemistry
  • Drug Discovery

Cite this

An improved synthesis of a selective αvβ3-integrin antagonist cyclo(-RGDfK-). / Dai, X.; Su, Z.; Liu, Jun.

In: Tetrahedron Letters, Vol. 41, No. 33, 12.08.2000, p. 6295-6298.

Research output: Contribution to journalArticle

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