| 摘要 |
<p>The invention is directed to a method to treat periodontal disease which method comprises administering to a subject afflicted with such disease an amount of a protegrin effective to treat said disease; wherein said protegrin contains the amino acid sequence (1): A1-A2-A3-A4-A5-C6-A7-C8-A9-A10-A11-A12-C13-A14-C15-A16-A17-A18, wherein said protegrin contains 10-30 amino acid residues, wherein the amino acid sequence of formula (1) may be extended at the N and/or C-terminus by additional noninterferring amino acids; and the N-terminal acylated and/or C-terminal amidated or esterified forms thereof, said protegrin either in the optionally -SH stabilized linear or in a disulfide-bridged form wherein each of C6, C8, C13 and C15 is independently a cysteine, homocysteine, or penicillamine, or wherein one or more of C6, C8, C13 and C15 is independently replaced by a basic, hydrophobic, large/polar or small amino acid or wherein C8 and/or C13 is not present; each of A1-A5 is independently present or not present, and if present each is independently a basic, hydrophobic, polar/large, or small amino acid; each of A7 and A14 is independently a hydrophobic or a small amino acid; A9-A12 are capable of effecting a β-turn when contained in the compound of formula (1) and at least one of A9-A12 must be a basic amino acid and wherein A9 and/or A12 may be present or not present; each of A16-A18 is independently present or not present, and if each present each is independently a basic, hydrophobic, polar/large or small amino acid; wherein in said protegrin at least about 15 % to about 50 % of the amino acids are basic amino acids, and wherein the protegrin compound has a net positive charge of at least +1 at physiological pH. </p> |
