ЛОУМАН Генри Бернард (US),ДЕНУАЕР Люк Ролан (US),ЛЮ Шоучунь (US),УЭСТ Джеймс Уилльям (US),СЭЙДЖЕРТ Джейсон Гэри (US),ВАСИЛЬЕВА Ольга (US),МЕНЕНДЕС Элизабет-Эдна Мэри (US)
申请号：
RU2014147684
公开号：
RU2014147684A
申请日:
2013.04.26
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. An activated antibody that, in an activated state, binds an epidermal growth factor receptor (EGFR), comprising: an antibody or antigen binding fragment (AB) that specifically binds to EGFR, where AB includes (i) a heavy chain amino acid sequence selected from the group consisting of SEQ ID NO: 26, SEQ ID NO: 30 and SEQ ID NO: 34, and an amino acid sequence of a light chain comprising SEQ ID NO: 68, or (ii) an amino acid sequence of a heavy chain selected from the group consisting of SEQ ID NO: 2, SEQ ID NO: 6 and SEQ ID NO: 10, and amino acid a light chain sequence comprising SEQ ID NO: 68； a masking fragment (MM) that inhibits the binding of the AB activated antibody in an uncleaved state to EGFR, where the masking fragment includes the amino acid sequence CISPRGCPDGPYVMY (SEQ ID NO: 14)； a cleavable fragment (CM) connected to AB, where CM is a polypeptide that functions as a substrate for the protease, and where CM includes the amino acid sequence LSGRSDNH (SEQ ID NO: 13), where the activated antibody in an uncleaved state has the following structural organization from N-end to C-end: MM-CM-AB or AB-CM-MM. 2. The activated antibody according to claim 1, wherein its antigen binding fragment is selected from the group consisting of a Fab fragment, F (ab ') fragment, scFv and scAb. 3. The activated antibody according to claim 1, wherein the activated antibody comprises a combination of heavy and light chains selected from the group consisting of: (a) a heavy chain comprising the amino acid sequence of SEQ ID NO: 26 and a light chain comprising the amino acid sequence of SEQ ID NO: 28； (b) a heavy chain comprising the amino acid sequence of SEQ ID NO: 2 and a light chain comprising the amino acid sequence of SEQ ID NO: 4； (c) a heavy chain comprising the amino acid sequence of SEQ ID NO: 6 and a light chain including1. Активируемое антитело, которое в активированном состоянии связывает рецептор эпидермального фактора роста (EGFR), включающее:антитело или его антиг
