C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/635 (2006.01) A61K 9/00 (2006.01) A61K 38/17 (2006.01) A61K 38/29 (2006.01) A61K 38/58 (2006.01) A61N 1/30 (2006.01) C07K 1/107 (2006.01) C07K 14/815 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2220060
Methods for modifying polypeptide agents to enhance their transdermal electrotransport flux are provided. The polypeptide is modified by reducing the potential of the polypeptide for forming .alpha.-helical or .beta.-sheet segments. In particular, amino acid residues known to stabilize .alpha.- helical and .beta.-sheet segments can be replaced with destabilizing residues and known helix breakers. Modified molecules and compositions including the molecules are also provided.
L'invention concerne des procédés pour modifier des agents polypeptidiques en vue d'améliorer leur flux transdermique par électrotransport. Le polypeptide est modifié par réduction de son potentiel pour former des segments .alpha.-hélicoïdaux ou .beta.-laminaires. En particulier, des résidus aminoacides connus pour stabiliser les segments .alpha.-hélicoïdaux et .beta.-laminaires peuvent être remplacés par des résidus déstabilisants et des agents de rupture d'hélice connus. Sont également décrites des molécules modifiées et des compositions les contenant.
Holladay Leslie A.
Oldenburg Kevin R.
Alza Corporation
Smart & Biggar
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