[EN] CONJUGATES COMPRISING PEPTIDE GROUPS AND METHODS RELATED THERETO<br/>[FR] CONJUGUÉS COMPRENANT DES GROUPES PEPTIDIQUES ET PROCÉDÉS ASSOCIÉS À CEUX-CI
申请人:LEGOCHEM BIOSCIENCES INC
公开号:WO2017089894A1
公开(公告)日:2017-06-01
In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and at least two active agents. In preferred embodiments, the linker comprises a peptide sequence of a plurality of amino acids, and at least two of the active agents are covalently coupled to side chains of the amino acids. The antibody-drug conjugate may comprise a self-immolative group, preferably two-self-immolative groups. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
在某些方面,本发明涉及一种抗体药物偶联物,包括:抗体;连接体;以及至少两个活性剂。在优选的实施例中,连接体包括由多个氨基酸组成的肽序列,其中至少两个活性剂通过共价键与氨基酸的侧链连接。抗体药物偶联物可以包括自焚基团,优选地是两个自焚基团。连接体可以包括O-取代的肟,例如,其中肟的氧原子被取代以与活性剂形成共价键连接;肟的碳原子被取代以与抗体形成共价键连接。