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.
制备了
金丝桃素肽,包括 MeVal-Val-Dil-Dap-Norephedrine (
MMAE) 和 MeVal-Val-Dil-Dap-Phe (
MMAF),并通过马来
酰亚胺基-val-cit-PAB 等各种连接体连接到
配体上。所制备的
配体药物共轭物在体外和体内均具有活性。