Synthesis of Unnatural Lipohilic N??(9H??Fluoren??9??ylmethoxy) carbonyl??Substituted α??Amino Acids and Their Incorporation into Cyclic RGD??Peptides: A structure?? …

…, H Kessler, SL Goodman, A Jonczyk

Index: Koppitz, Marcus; Huenges, Martin; Gratias, Rainer; Kessler, Horst; Goodman, Simon L.; Jonczyk, Alfred Helvetica Chimica Acta, 1997 , vol. 80, # 4 p. 1280 - 1300

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Citation Number: 19

Abstract

Abstract The α v/β 3 integrin is implicated in human tumor metastasis and angiogenesis. It has been shown that structures of the sequence cyclo (-Arg 1-Gly 2-Asp 3-D-Phe 4-Xaa 5- )(I) and cyclo (-Arg 1-Gly 2-Asp 3-Phe 4-D-Xaa 5-)(II) bind with high affinity and the latter with high selectivity to this receptor. The residues Xaa and D-Xaa accept a broad variety of amino acids. Here, we report on the synthesis, activities, and conformational analysis of cyclic ...