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    • 7. 发明公开
    • BIOLOGICALLY ACTIVE AMPHIPHILIC PEPTIDE COMPOSITIONS AND USES THEREFOR.
    • BIOLOGISCH AKTIVE AMPHIPHILE PEPTIDZUSAMMENSETZUNGEN UND IHRE VERWENDUNGEN。
    • EP0667871A4
    • 1995-04-06
    • EP92920492
    • 1992-09-04
    • MAGAININ PHARMA
    • MALOY W LEEKARI U PRASADWILLIAMS JON I
    • A61K38/00C07K7/06C07K7/08C07K14/00C07K14/46
    • C07K7/06A61K38/00C07K7/08C07K14/46
    • Biologically active amphiphilic peptides including one of the following basic structures: I) R1-R2-R2-R1-R2-R2-R1-R1-R2-R1-R1; II) R2-R1-R2-R2-R1-R1-R2-R2-R1-R2-R2; III) R1-R2-R2-R1-R1-R2-R2-R1-R2-R2-R1-R1-R2-R3; IV) R1-R2-R1-R1-R2-R2-R1-R1-R2-R2-R4; V) R1-R1-R2-R2-R1-R2-R2-R1-R1-R2-R2-R3; or VI) R1-R1-R3-R2-R1-R1-R1-R1-R1-R1-R2-R1-R1-R2-R2-R1-R1-R2-R2-R1. R1 is a hydrophobic amino acid and R2 is a basic hydrophilic or neutral hydrophilic amino acid, R3 is a neutral hydrophilic amino acid, and R4 is a neutral hydrophilic amino acid or proline. There is also provided a biologically active amphiphilic peptide having a structural formula selected from the group consisting of: (a) R1-R2-R2-R1-R2-R2-R1; (b) R1-R1-R2-R2-R1-R2-R2-R1; (c) R2-R1-R1-R2-R2-R1-R2-R2-R1; (d) R2-R2-R1-R1-R2-R2-R1-R2-R2-R1; and (e) R1-R2-R2-R1-R1-R2-R2-R1-R2-R2-R1, wherein R1 and R2 are hereinabove described. Such peptides may be employed as pharmaceuticals.
    • 包括以下基本结构之一的生物活性两亲性肽:I)R1-R2-R2-R1-R2-R2-R1-R1-R2-R1-R1; II)R2-R1-R2-R2-R1-R1-R2-R2-R1-R2-R2; III)R1-R2-R2-R1-R1-R2-R2-R1-R2-R2-R1-R1-R2-R3; IV)R1-R2-R1-R1-R2-R2-R1-R1-R2-R2-R4; V)R1-R1-R2-R2-R1-R2-R2-R1-R1-R2-R2-R3; 或VI)R 1 -R 1 -R 3 -R 2 -R 1 -R 1 -R 1 -R 1 -R 1 -R 1 -R 2 -R 1 -R 1 -R 2 -R 2 -R 1 -R 1 -R 2 -R 2 -R 1。 R1是疏水氨基酸,R2是碱性亲水或中性亲水氨基酸,R3是中性亲水氨基酸,R4是中性亲水氨基酸或脯氨酸。 还提供了具有选自以下的结构式的生物活性两亲性肽:(a)R1-R2-R2-R1-R2-R2-R1; (b)R1-R1-R2-R2-R1-R2-R2-R1; (c)R2-R1-R1-R2-R2-R1-R2-R2-R1; (d)R2-R2-R1-R1-R2-R2-R1-R2-R2-R1; 和(e)R1-R2-R2-R1-R1-R2-R2-R1-R2-R2-R1,其中R1和R2如上所述。 这样的肽可以用作药物。