申请人:Complex Biosystems GmbH
公开号:EP1525890A1
公开(公告)日:2005-04-27
The present invention relates to a protein encapsulated by an encapsulating organic compound (EOC) or proteophore wherein the protein and the encapsulating organic compound are present in 1:1 stoichiometry.
In one embodiment of the present invention, the encapsulation is realized by an EOC protein inclusion compound EPIC according to the formula (I) in which the EMCs are connected to each other by one branching unit B under formation of a cavity which is vertically and horizontally open
and wherein the symbols have the following meanings:
B:branching unit containing at least one branching center Bc and at least two branching functional groups Bfg connected to or capable of reacting with an encapsulating molecular chain EMC;
EMC:encapsulating molecular chain;
L:linker containing at least one functional group Lfg which is connected to the protein P or capable of connecting with functional groups present on the protein P under the formation of a chemical bond;
1:1, 2, 3, 4, 5, 6, 7, 8 or 9;
P:pharmacologically active protein.
In a further embodiment of the present invention, the encapsulation is realized by a macrocycle-protein inclusion compound MPIC according to the formula (IX)
containing a protein P and a macrocyclic structure, and wherein the symbols have the meanings given above for formula (I).
The EMCs can comprise substituents (capping groups), which can result in dendritic structures.
The encapsulation assures a controlled release of a protein.
本发明涉及由一个封装有机化合物(EOC)或蛋白质荷载体包裹的蛋白质,其中该蛋白质和封装有机化合物以1:1的化学计量比存在。在本发明的一个实施例中,封装是通过一个符合以下公式(I)的EOC蛋白质包含化合物EPIC实现的,其中EMCs通过一个分支单元B连接在一起,形成一个垂直和水平开放的空腔,符号的含义如下:B:包含至少一个分支中心Bc和至少两个连接到或能够与封装分子链EMC反应的分支功能基团Bfg的分支单元;EMC:封装分子链;L:包含至少一个与蛋白质P连接或能够在形成化学键时连接到蛋白质P上存在的功能基团Lfg的连接器;1:1、2、3、4、5、6、7、8或9;P:药理活性蛋白质。在本发明的另一个实施例中,封装是通过符合公式(IX)的大环-蛋白质包含化合物MPIC实现的,其中包含一个蛋白质P和一个大环结构,符号的含义如上所述。EMCs可以包括取代基(顶端基团),这可能导致树枝状结构。封装确保了蛋白质的受控释放。