C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
167/103, 530/7.1
C07K 14/00 (2006.01) A61K 38/16 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2035959
ABSTRACT OF THE DISCLOSURE A biologically active amphiphilic peptide which in accordance with an aspect of the present invention, includes one of the following basic structures X1 through X7, wherein: X1 is -[R1-R2-R2-R3-R1-R2-R2]-n X2 is -[R2-R2-R3-R1-R2-R2-R1]-n; X3 is -[R2-R3-R1-R2-R2-R1-R2]-n; X4 is -[R3-R1-R2-R2-R1-R2-R2]-n; X5 is -[R1-R2-R2-R1-R2-R2-R3]-n; X6 is -[R2-R2-R1-R2-R2-R3-R1]-n; and X7 is -[R2-R1-R2-R2-R3-R1-R2]-n; wherein R1 is a basic hydrophilic amino acid, R2 is a hydrophobic amino acid, R3 is a neutral hydrophilic, basic hydrophilic or hydrophobic amino acid and n is from 2 to 5. Preferred peptides are of the following formulae: (Lys Ile Ala Gly Lys Ile Ala)3-NH2 and (Lys Ile Ala Lys Ile Ala Gly)3-NH2 In another aspect of the prevent invention, there is provided a biologically active amphiphilic peptide which includes the following basic structure. R1-R2-R2-R3-R4-R2-R2-R1-R2-R2-R2-R4-R2-R2, wherein R1, R2, and R3 are as hereinabove described, and R4 is a basic hydrophilic or hydrophobic amino acid. Preferred peptides are of the following formulae: Image and Image In yet another aspect of the present invention, there is provided a biologically active amphiphilic peptide including the following structural formula: (Lys Ile Ala Lys Lys Ile Ala)n, wherein n is from 2 to 5. In a further aspect of the present invention, there is provided a biologically active amphiphilic peptide selected from the group consisting of: (SEQ ID NO:61)-NH2; (SEQ ID NO:62)-NH2; (SEQ ID NO:63)-NH2; and (SEQ ID NO:64)-NH2. The peptides may be used in pharmaceutical compositions.
Berkowitz Barry
Kari U. Prasad
Maloy W. Lee
Magainin Pharmaceuticals Inc.
Smart & Biggar
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