Selective alfavbeta3 receptor peptide antagonist for...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/46 (2006.01) A61P 19/02 (2006.01) A61P 19/10 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2625436

The present invention is related to new peptide antagonists of .alpha.v.beta.3 receptor, designed on the basis of the crystal structure of integrin .alpha.v.beta.3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the .alpha.v.beta.3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for .alpha.v.beta.3- targeted therapy and imaging.

La présente invention concerne de nouveaux antagonistes peptidiques du récepteur .alpha.v.beta.3, conçus sur la base de la structure cristalline de l'intégrine .alpha.v.beta.3 en complexe avec c(RGDf[NMe]V) et la structure NMR de l'échistatine. Ces peptides sont des antagonistes puissants et sélectifs du récepteur .alpha.v.beta.3 et peuvent être utilisés en tant que nouveaux médicaments anticancéreux et/ou en tant que nouvelle classe de traceurs de diagnostic non invasifs appropriés pour l'imagerie et la thérapie reposant sur .alpha.v.beta.3.

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