Novel integrin-binding peptides

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/04 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61L 27/00 (2006.01) A61L 27/22 (2006.01) C07K 1/22 (2006.01) C07K 7/64 (2006.01) C07K 14/705 (2006.01) C07K 14/75 (2006.01) C07K 14/78 (2006.01) G01N 33/566 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2177070

This invention is directed to novel integrin-binding peptides. These peptides bind to .alpha.v- or .alpha.5-containing integrins and can exhibit high binding affinity. They contain one of the following sequence motifs: RX1ETX2WX3 [SEQ ID NO: 1] (especially RRETAWA [SEQ ID NO: 8]); RGDGX [SEQ ID NO: 2], in which X is an amino acid with a hydrophobic, aromatic side chain; the double cyclic CX1CRGDCX2C [SEQ ID NO: 15]; and RLD. The peptides generally exhibit their highest binding affinity when they assume a conformationally stabilized configuration. This invention also provides methods of using these peptides.

Cette invention se rapporte à de nouveaux peptides fixant l'intégrine. Ces peptides se fixent à des intégrines contenant .alpha.¿v? ou .alpha.¿5? et peuvent présenter une haute affinité de liaison. Ils contiennent un des motifs structuraux des séquences suivantes: RX¿1?ETX¿2?WX¿3? [NO ID SEQ: 1] (notamment RRETAWA [NO ID SEQ: 8]); RGDGX [NO ID SEQ: 2], dans lequel X représente un acide aminé ayant une chaîne latérale aromatique, hydrophobe; la double séquence cyclique CX¿1?CRGDCX¿2?C [NO ID SEQ: 15]; and RDL. Les peptides présentent généralement leur plus haute affinité de liaison lorsqu'ils prennent une configuration stabilisée par sa conformation. L'invention se rapporte également à des procédés d'utilisation de ces peptides.

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