abstract |
A method of preparing a multifunctional antibody (MAC) conjugate, the MAC comprising: (i) an antibody or antigen binding portion thereof, comprising at least a fragment of a light chain constant kappa (CLκ) region that it comprises K188 and H189 according to Kabat numbering; (ii) a linker comprising the formula XYZ, in which Z is a group of the formula and is covalently connected to the antibody through the ε-amino group of the side chain of K188 (according to Kabat numbering), Y is a biologically compatible, linear or branched connection chain, and X is a group covalently connected to at least one effector fraction, the method comprising covalently joining the effector fraction to a linker ending in an activated ester with a leaving group Z * of formula: wherein R1 is F, and h = 3, 4 or 5, and reacting the effector-linker-Z * complex complex thus formed with the antibody .. |