Process to inhibit binding of the integrin alpha 4 beta 1 to...

Details Process to inhibit binding of the integrin alpha 4 beta 1 to... Process to inhibit binding of the integrin alpha 4 beta 1 to...

C - Chemistry, Metallurgy

07

K

C07K 7/64 (2006.01) A61K 38/12 (2006.01) C07K 5/12 (2006.01) C07K 14/78 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2193828

The present invention is directed to an isolated and purified cyclic peptide of from 5 to about 13 residues modeled after a portion of the CS1 peptide. A peptide of this invention preferably has the amino acid residue sequence of SEQ ID NO:2-14 or 16-42. The present invention is further directed to a process of selectively inhibiting the binding of .alpha.4.beta.1 integrin to a protein such as VCAM-1, fibronectin or invasin comprising exposing a cell that expresses .alpha.4.beta.1 integrin to that protein in the presence of an effective inhibiting amount of such a peptide. The present invention is still further directed to a pharmaceutical composition comprising a physilogically acceptable carrier and a cyclic peptide of the invention.

La présente invention concerne un peptide cyclique isolé et purifié constitué de 5 à environ 13 résidus d'acide aminé modelés sur une partie du peptide CS1. Le peptide selon l'invention présente, de préférence, la séquence de résidus d'acide aminé correspondant au numéro d'identification de séquence 2-14 ou 16-42. La présente invention concerne également un procédé permettant d'inhiber, de façon sélective, la fixation de l'intégrine .alpha.¿4?.beta.¿1? à une protéine telle que la molécule d'adhérence cellulaire vasculaire 1, la fibronectine ou l'invasine, ledit procédé consistant à exposer une cellule qui exprime l'intégrine .alpha.¿4?.beta.¿1? à ladite protéine, en présence d'une quantité d'un tel peptide suffisante pour assurer une inhibition efficace. La présente invention concerne également une composition pharmaceutique comprenant un excipient physiologiquement acceptable et un peptide cyclique selon l'invention.

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