Ion-channel forming amphiphilic peptides having n-terminal...

A - Human Necessities – 61 – K

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A61K 38/16 (2006.01) A61K 38/09 (2006.01) A61K 38/10 (2006.01) C07K 7/08 (2006.01) C07K 14/00 (2006.01) C07K 14/435 (2006.01) C07K 14/46 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2180748

An N-terminal substituted peptide or pro- tein having formula (1). X is a biologically ac- tive amphiphilic ion channel-forming peptide or protein. T is a lipophilic moiety, and prefer- ably, T is formula (2), wherein R is a hydro- carbon (alkyl or aromatic or alkylaromatic) having at least 2 and no more than 10 carbon atoms. T is preferably an octanoyl group. W is T or hydrogen. The N-terminal substituted peptides and proteins have improved biological activity against target cells, viruses, and virally-infected cells.

Peptide ou protéine à substitution N-terminale correspondant à la formule (1), dans laquelle X est un peptide ou protéine biologiquement actif formant un canal ionique amphiphilique, T est une fraction lipophile et, de préférence, représente (2) (où R est un hydrocarbure (alkyle ou aromatique ou alkylaromatique) comportant au moins 2 et au maximum 10 atomes de carbone. T est de préférence un groupe octanoyle. W est T ou hydrogène. Ces peptides et protéines à substitution N-terminale présentent une activité biologique améliorée contre des cellules cibles, des virus et des cellules infectées par un virus.

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