Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
Auristatin肽包括MeVal-Val-Dil-Dap-Norephedrine (
MMAE)和MeVal-Val-Dil-Dap-Phe (
MMAF),通过不同的连接剂,包括maleimidocaproyl-val-cit-PAB,制备并连接到
配体上。所得的
配体药物偶联物在体内外均具有活性。