公开(公告)号：US20120009205A1

公开(公告)日：2012-01-12

申请号：US13171233

申请日：2011-06-28

申请人： Colin V. GEGG ,  Kenneth W. Walker ,  Leslie P. Miranda ,  Fei Xiong

发明人： Colin V. GEGG ,  Kenneth W. Walker ,  Leslie P. Miranda ,  Fei Xiong

IPC分类号： A61K39/395 ,  C12N9/96 ,  C12N15/13 ,  C12N15/63 ,  C12N1/21 ,  C07K16/46 ,  C07K17/00 ,  C07K1/107 ,  C12P21/02 ,  C07K19/00 ,  C08F126/10 ,  C08F116/06 ,  C07K16/00 ,  C12N5/10

CPC分类号： A61K47/48369 ,  A61K38/02 ,  A61K47/60 ,  A61K47/68 ,  A61K47/6817 ,  C07K16/00 ,  C07K17/00 ,  C07K2317/40 ,  C07K2317/52

摘要： Disclosed is a process for preparing a pharmacologically active compound, in which at least one internal conjugation site of an Fc domain sequence is selected that is amenable to conjugation of an additional functional moiety by a defined conjugation chemistry through the side chain of an amino acid residue at the conjugation site. An appropriate amino acid residue for conjugation may be present in a native Fc domain at the conjugation site or may be added by insertion (i.e., between amino acids in the native Fc domain) or by replacement (i.e., removing amino acids and substituting different amino acids). In the latter case, the number of amino acids added need not correspond to the number of amino acids removed from the previously existing Fc domain. This technology may be used to produce useful compositions of matter and pharmaceutical compositions containing them. A DNA encoding the inventive composition of matter, an expression vector containing the DNA, and a host cell containing the expression vector are also disclosed.

摘要翻译： 公开了制备药理活性化合物的方法，其中选择Fc结构域序列的至少一个内部缀合位点，其适于通过定义的缀合化学通过氨基酸残基的侧链与另外的功能部分缀合 在共轭位点。 用于缀合的合适的氨基酸残基可以在缀合位点处的天然Fc结构域中存在，或者可以通过插入（即天然Fc结构域中的氨基酸之间）或替换（即，除去氨基酸并用不同的氨基 酸）。 在后一种情况下，加入的氨基酸数不需要对应于从先前存在的Fc结构域去除的氨基酸的数目。 该技术可用于生产含有它们的物质和药物组合物的有用组合物。 还公开了编码本发明组合物的DNA，含有该DNA的表达载体和含有表达载体的宿主细胞。