Method for preparing polyfunctionalized peptides and/or...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 1/02 (2006.01) C07K 14/505 (2006.01)

Patent

CA 2538005

The present invention provides a method for preparing polyfunctionalized peptides and/or proteins at non-adjacent designated sites via native chemical ligation. In certain embodiments, the inventive method is a method for preparing a polyfunctionalized peptide comprising a peptidic backbone made up of four or more amino acids, wherein two or more non-adjacent amino acids are independently subsituted with a moiety having the structure: wherein A and L1 are as defined herein. In certain other embodiments, the inventive method allows the preparation of polyfunctionalized peptides having the general structure: wherein A, RPO, RPI, PXI, RX2, L1, to, s, tand q are as defined herein.

L'invention concerne un procédé pour préparer des peptides et/ou protéines polyfonctionnalisé(e)s au niveau de sites spécifiques non adjacents, par ligation chimique native. Dans certains modes de réalisation, cette invention concerne un procédé pour préparer un peptide polyfonctionnalisé comprenant un squelette peptidique constitué de quatre amino-acides ou davantage, au moins deux amino-acides non adjacents étant substitués indépendamment par une fraction présentant la structure (I), dans laquelle A et L?1¿ sont tels que définis dans la description. Dans d'autres modes de réalisation, cette invention se rapporte à la préparation de peptides polyfonctionnalisés présentant la structure générale (II), dans laquelle A, R<SP>P0</SP>, R<SP>P1</SP>, R<SP>X1</SP>, R<SP>X2</SP>, L?1¿, t0, s, t et q sont tels que définis dans la description.

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