The synthesis and properties of Gla-and Phe-containing analogues of cyclic RGD pentapeptides

…, C Enjalbal, C Nguyen, L Al-Jamri, C Naumer

Index: Davies, John S.; Enjalbal, Christine; Nguyen, Corrine; Al-Jamri, Loai; Naumer, Christian Journal of the Chemical Society, Perkin Transactions 1, 2000 , # 17 p. 2907 - 2915

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Abstract

Cyclopentapeptides containing the Arg-Gly-Asp motif have been synthesised using solid- phase assembly of side-chain-protected linear precursors, followed by solution-phase cyclisation. The replacement of the Asp residue by γ-carboxyglutamic acid (Gla) is a novel feature which gives rise to an analogue which inhibits cell adhesion, yet its congeners do not show activity in binding assays with recombinant integrin receptors. NMR techniques ...

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