La Jolla Cancer Research Foundation

The Burnham Institute

Erkki Koivunen

Erkki I Ruoslahti

This invention is directed to novel integrin binding peptides. These peptides bind to &#x3b1;- of &#x3b1;-containing integrins and can exhibit high binding affinity. They contain one of the following sequence motifs: RXETXWX[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 CXCRGDCXC [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.

Integrin-binding peptides

The present invention provides peptides having specificity for fibronectin-binding and vitronectin-binding integrins, and in particular for &agr;,&bgr;,integrin. These peptides are characterized by having the ability to interfere with extracellular matrix protein binding to integrins; to block attachment of cells expressing these integrins to extracellular matrix proteins; and to promote cell attachment when coated onto a surface.

This invention is directed to novel integrin binding peptides. These peptides bind to .alpha..sub.v - of .alpha..sub.5 -containing integrins and can exhibit high binding affinity. They contain one of the following sequence motifs: RX.sub.1 ETX.sub.2 WX.sub.3 [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 CX.sub.1 CRGDCX.sub.2 C [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.

The present invention provides peptides having specificity for fibronectin-binding and vitronectin-binding integrins, and in particular for .alpha..sub.5 .beta..sub.1 integrin. These peptides are characterized by having the ability to interfere with extracellular matrix protein binding to integrins; to block attachment of cells expressing these integrins to extracellular matrix proteins; and to promote cell attachment when coated onto a surface.

The present invention provides peptides having specificity for fibronectin-binding and vitronectin-binding integrins, and in particular for .alpha..sub.5 .beta..sub.1 integrin. These peptides are characterized by having the ability to interfere with fibronectin binding to .alpha..sub.5 .beta..sub.1 integrin, to block attachment of cells expressing integrins to extracellular matrix proteins and to promote cell attachment when immobilized onto a surface.

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San Diego, CA, United States of America

Erkki Koivunen