发明名称 |
METHODS FOR MAKING CONJUGATES FROM DISULFIDE-CONTAINING PROTEINS |
摘要 |
<p>The invention provides methods to prepare protein conjugates from proteins having at least four accessible cysteine residues. In one embodiment, an antibody with four reducible disulfide linkages is reduced to provide four pairs of free cysteines. Each pair of free cysteines is reacted with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of each pair together though a 3-carbon tether with a reactive ketone. A pair of these reactive ketones are linked together with and used to attach a single payload molecule, thus conjugating the antibody to two payload groups. This method gives a stabilized antibody conjugate with high selectivity for a ratio of two payloads per antibody.</p> |
申请公布号 |
WO2015179734(A1) |
申请公布日期 |
2015.11.26 |
申请号 |
WO2015US32126 |
申请日期 |
2015.05.22 |
申请人 |
NOVARTIS AG;HU, QI-YING;ALLAN, MARTIN |
发明人 |
HU, QI-YING;ALLAN, MARTIN |
分类号 |
A61K47/48 |
主分类号 |
A61K47/48 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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