Alpha-helix mimetics and methods relating thereto

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/06 (2006.01) C07K 1/107 (2006.01) C07K 4/00 (2006.01) C07K 5/078 (2006.01) C07K 14/575 (2006.01)

Patent

CA 2142604

2142604 9500534 PCTABS00035 There are disclosed alpha-helix mimetics and methods relating to the same for imparting or stabilizing alpha-helicity to a peptide or protein. In one aspect, the alpha-helix mimetics contain six- or seven-membered rings covalently attached at the end or within the length of the peptide or protein. The alpha-helix mimetics render the resulting peptide or protein more stable with regard to thermal stability, as well as making the peptide or protein more resistant to proteolytic degradation. In addition, the alpha-helix mimetics may be used in standard peptide synthesis protocols.

L'invention concerne des structures mimétiques de l'hélice alpha, et des procédés connexes, pour stabiliser ou communiquer l'hélicité alpha à un peptide ou une protéine. Dans un aspect, les structures mimétiques de l'hélice alpha contiennent des noyaux hexagonaux ou heptagonaux liés de manière covalente à l'extrémité ou à l'intérieur de la longueur du peptide ou de la protéine. Les structures mimétiques de l'hélice alpha rendent le peptide ou la protéine obtenus plus stables thermiquement et les rendent également plus résistants à la dégradation protéolytique. De plus, les structures mimétiques de l'hélice alpha peuvent être utilisées dans des protocoles de synthèse peptidique standard.

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