主权项 |
1. A modified polypeptide of Formula (I), wherein: each R1 and R2 are independently H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkylalkyl, heteroarylalkyl, or heterocyclylalkyl; each R3 is independently alkyl, alkenyl, alkynyl or [R4—K—R4]n; each of which is substituted with 0-6 R5; each R4 is independently alkyl, alkenyl, or alkynyl; each R5 is independently halo, alkyl, OR6, N(R6)2, SR6, SOR6, SO2R6, CO2R6, R6, a fluorescent moiety, or a radioisotope; each K is independently O, S, SO, SO2, CO, CO2, CONR6, or each R6 is independently H, alkyl, or a therapeutic agent; n is an integer from 1-4; x is 3, 4 or 6; y and w are independently an integer between 0 and 15; z is 1; and each Xaa is independently an amino acid; wherein the modified polypeptide consists of 8-20 contiguous amino acids of SEQ ID NO:1 and: (a) within a sequence of 8 contiguous amino acids the side chains of at least one pair of amino acids separated by 3, 4 or 6 amino acids are replaced by the linking group R3 which connects the alpha carbons of the pair of amino acids as depicted in Formula (I); and (b) the alpha carbon of the first of the pair of amino acids is substituted with R1 as depicted in Formula (I) and the alpha carbon of the second of the pair of amino acids is substituted with R2 as depicted in Formula (I); wherein and N or C can be substituted by PEG, spermine, or a carbohydrate. |