Hybrid immunoglobulin containing non-peptidyl linkage

Abstract

The present invention provides compounds producing compounds having the structure (I). Wherein A is a first polypeptide component of the compound; wherein C is a second polypeptide component of the compound, which polypeptide component comprises consecutive amino acids which (i) are identical to a stretch of consecutive amino acids present in a chain of an Fc domain of an antibody; (ii) bind to an Fc receptor, and (iii) have at their N-terminus a sequence selected from the group consisting of a cysteine, selenocysteine, CP, CPXCP (where X=P, R, or S), CDKTHTCPPCP, CVECPPCP, CCVECPPCP and CDTPPPCPRCP, wherein B is a chemical structure linking A and C; wherein the dashed line between B and C represents a peptidyl linkage; wherein the solid line between A and B represents a nonpeptidyl linkage comprising the structure (II).

1 - 231 . (canceled) 
     
     
         232 . A compound having the structure: 
       
         
           
           
               
               
           
         
         wherein C is a polypeptide component of the compound, which polypeptide component has at its N-terminus a sequence of amino acids selected from the group consisting of a cysteine, selenocysteine, CP, CPXCP (where X=P, R, or S) (SEQ ID NOs: 128-130), CDKTHTCPPCP (SEQ ID NO: 131), CVECPPCP (SEQ ID NO: 132), CCVECPPCP (SEQ ID NO: 133) and CDTPPPCPRCP (SEQ ID NO: 134), and comprises consecutive amino acids which (i) are identical to a stretch of consecutive amino acids present in a chain of an Fe domain of an antibody; and (ii) bind to an Fc receptor, 
         wherein B″ comprises chemical structure B and a terminal reactive group which is an azide or an alkyne; 
         wherein the dashed line between B″ and C represents a peptidyl linkage between B″ and the N-terminus of C. 
       
     
     
         233 . The compound according to claim  1 , wherein the terminal reactive group is a terminal alkyne. 
     
     
         234 . The compound according to claim  1 , wherein the terminal reactive group is a cycloalkyne. 
     
     
         235 . The compound according to claim  1 , wherein the terminal reactive group is an eight-membered ring. 
     
     
         236 . The compound according to claim  1 , wherein the terminal reactive group is an azacyclooctyne. 
     
     
         237 . The compound according to claim  1 , wherein the terminal reactive group is a biarylazacyclooctyne. 
     
     
         238 . The compound according to claim  1 , wherein the terminal reactive group is a cyclooctyne. 
     
     
         239 . The compound according to claim  1 , wherein the chemical structure B is (a) an organic acid residue or (b) a stretch of consecutive amino acid residues which is, or is present in any of the following sequences: EPKSCDKTHTCPPCP, ERKCCVECPPCP, ELKTPLGDTTHTCPRCP(EPKSCDTPPPCPRCP)3, or ESKYGPPCPSC. 
     
     
         240 . The compound according to claim  2 , wherein the chemical structure B is (a) an organic acid residue or (b) a stretch of consecutive amino acid residues which is, or is present in any of the following sequences: EPKSCDKTHTCPPCP, ERKCCVECPPCP, ELKTPLGDTTHTCPRCP(EPKSCDTPPPCPRCP)3, or ESKYGPPCPSC. 
     
     
         241 . The compound according to claim  3 , wherein the chemical structure B is (a) an organic acid residue or (b) a stretch of consecutive amino acid residues which is, or is present in any of the following sequences: EPKSCDKTHTCPPCP, ERKCCVECPPCP, ELKTPLGDTTHTCPRCP(EPKSCDTPPPCPRCP)3, or ESKYGPPCPSC.