| 摘要 |
Compounds based on the antimicrobial protegrins and tachyplesins are disclosed having a net positive charge of at least +1 at physiological pH, comprising from 15 % to 50 % basic amino acids, and having an amino acid sequence of the formula: A1-A2-A3-C4*-C5*-C6*-A7-C8-A9-A10-A11-A12-C13-A14-C15*-C16*-C17*-A18, within a size range of 11-24 amino acids when the above formula is extended at either the N- or C-terminus by additional, non-interfering, amino acids and wherein the N-terminus may be acylated and the C-terminus may be amidated or esterified and disulfide bridges may be present or absent in a -SH stabilized linear form. In one embodiment, C8 and C13 denote cysteine, homocysteine or penicillamine; C4*-C6* and C15*-C16* denote the preceding or any naturally-occurring amino acid save glutamic acid, aspartic acid and proline, except when either or both of C4* or C17* are optionally absent wherein only proline is excluded at C5* and C15*; A1-A3 and A18 may be present or absent and denote any naturally-occurring amino acid except glutamic acid, aspartic acid, proline and cysteine; A7 and A14 denote a hydrophobic or a small amino acid; A9-A12 must be capable of forming a beta -turn in the compound; and, at least one of A9-A12 must be a basic amino acid. |
