SITE-SELECTIVE ACYL TRANSFER
    71.
    发明公开
    SITE-SELECTIVE ACYL TRANSFER 审中-公开
    特异性结合JOBS酰基

    公开(公告)号:EP1283873A2

    公开(公告)日:2003-02-19

    申请号:EP01932438.3

    申请日:2001-05-07

    发明人: BALTZER, Lars

    IPC分类号: C12N9/10 C07K1/10 C07K14/00

    摘要: A method for site-selective acyl transfer in or amidation of folded polypeptides and proteins based on the use of a chemical structure element comprising an imidazole function, such as histidine, in position i flanked by at least one functional group to be amidated, such as lysine, in position i+3+4k, where k is an integer equal to or higher than -1, or in position i-4-4n, wherein n is an integer equal to or higher than 0, and at least one activating group, such as serine, in position i+4+4n or i-3-4n, respectively.

    Site-specific conjugation of glycoproteins
    73.
    发明公开
    Site-specific conjugation of glycoproteins 审中-公开
    Stellungsspezifische Konjugation von糖蛋白

    公开(公告)号:EP0913691A1

    公开(公告)日:1999-05-06

    申请号:EP98119752.8

    申请日:1998-10-22

    IPC分类号: G01N33/531 C07K17/10

    摘要: The present invention describes a site specific conjugation method for glycoproteins wherein a stable dihydrazone bond is formed between the glycoproteins and the glycoproteins retain full activity. Also described is a novel glycoprotein-glycoprotein conjugate of the formula I
    wherein X and Y are glycoproteins modified such that the vicinal hydroxyl groups of the carbohydrate moieties in the glycoproteins have been oxidized to aldehydes which are then reacted with a hydrazide functional group to form a hydrazone bond which is represented in Formula I by "-C=NNH-".

    摘要翻译: 本发明描述了糖蛋白的位点特异性缀合方法,其中在糖蛋白和糖蛋白之间形成稳定的二腙键保持完全的活性。 还描述了式I 的新型糖蛋白 - 糖蛋白缀合物,其中X和Y是修饰的糖蛋白,使得糖蛋白中的碳水化合物部分的连位羟基已被氧化成醛,然后与酰肼官能团反应 以形成式I中“-C = NNH-”表示的腙键。

    METHOD FOR MODIFICATION OF RECOMBINANT POLYPEPTIDES
    74.
    发明公开
    METHOD FOR MODIFICATION OF RECOMBINANT POLYPEPTIDES 失效
    方法进行修改重组多肽。

    公开(公告)号:EP0651761A1

    公开(公告)日:1995-05-10

    申请号:EP93918187.0

    申请日:1993-07-13

    申请人: BIONEBRASKA, INC.

    摘要: The invention provides for a chemical method for preparing a recombinant single copy polypeptide or a portion thereof with a modified terminal amino acid α-carbon reactive group selected from the group consisting of N-terminal α-amine, C-terminal α-carboxyl, and a combination thereof. The steps of the method involve forming the recombinant single copy polypeptide or a portion thereof so that the single copy polypeptide is protected with one or more biologically added protecting groups at the N-terminal α-amine, C-terminal α-carboxyl. The recombinant single copy polypeptide can then be reacted with up to three chemical protecting agents to selectively protect reactive side chain groups and thereby prevent side chain groups from being modified. The recombinant single copy polypeptide can be cleaved with at least one cleavage reagent specific for the biological protecting group to form an unprotected terminal amino acid α-carbon reactive group. The unprotected terminal amino acid α-carbon reactive group is modified with at least one chemical modifying agent. The side chain protected terminally modified single copy polypeptide is then deprotected at the side chain groups to form a terminally modified recombinant single copy polypeptide. The number and sequence of steps in the method can be varied to achieve selective modification at the N- and/or C-terminal amino acid of a recombinantly produced polypeptide.

    Protein derivatives and a process for their preparation
    77.
    发明公开
    Protein derivatives and a process for their preparation 失效
    蛋白衍生物和Verfahren zu ihrer Herstellung。

    公开(公告)号:EP0360433A1

    公开(公告)日:1990-03-28

    申请号:EP89308680.1

    申请日:1989-08-25

    摘要: Protein derivatives of formula (1)
    A-CO-N(R¹)CH₂-Z-R²      (1)
    wherein A-CO is the residue of a protein or peptide A-CO₂H (especially where -CO₂H is the C-terminal carboxyl group of the protein or peptide); R¹ is a hydrogen atom or an alkyl, aryl or aralkyl group; Z¹, which may be present or absent is a spacer group; R² is a group -C(OH)(R³)CH₂NHR⁴ or -C(R³)O (where R³ and R⁴ which may be the same or different, is each a hydrogen atom or an alkyl, aryl or aralkyl group); with the proviso that when A-CO is a residue of insulin, R¹ is other than a hydrogen atom; and the salts thereof. The compounds may be prepared by a condensation reaction,, especially in the presence of an enzyme capable of catalysing the formation of a peptide bond. The compounds may be used to form protein conjugates in which a group of interest such as another protein or peptide or an effector or reporter group is coupled to the protein through a -N(R¹)CH₂-Z¹-C(OH)(R³)CH₂N= or -N(R¹)CH₂Z¹-CH= group.

    摘要翻译: 式(1)的蛋白衍生物A-CO-N(R 1)CH 2 -ZR 2(1)其中A-CO是蛋白质或肽A-CO 2 H的残基(特别是其中-CO 2 H是C - 蛋白质或肽的末端羧基); R 1是氢原子或烷基,芳基或芳烷基; 可能存在或不存在的Z 1是间隔基; R 2是基团-C(OH)(R 3)CH 2 NHR 4或-C(R 3)O(其中R 3和R 4可以相同或不同) 各自为氢原子或烷基,芳基或芳烷基); 条件是当A-CO是胰岛素的残基时,R 1不是氢原子; 及其盐。 化合物可以通过缩合反应制备,特别是在能够催化形成肽键的酶的存在下。 所述化合物可用于形成蛋白质缀合物,其中目标组如另一蛋白质或肽或效应物或报道基团通过-N(R 1)CH 2 -Z 1 -C (OH)(R 3)CH 2 N =或-N(R 1)CH 2 Z 1 -CH =基团。

    Protein derivatives and a process for their preparation
    78.
    发明公开
    Protein derivatives and a process for their preparation 失效
    蛋白质衍生物及其制备方法

    公开(公告)号:EP0359428A1

    公开(公告)日:1990-03-21

    申请号:EP89308681.9

    申请日:1989-08-25

    摘要: Protein derivatives of formula (1) A-CO-N(R 1 )N(R 2 )-Z 1 -
    wherein A-CO is the residue of a protein or peptide A-CO 2 H (especially where -C0 2 H is the C-terminal carboxyl group of the protein or peptide); R 1 , R 2 , R 3 and R 4 , which may be the same or different, and which may be present or absent, is each a spacer group, X is an oxygen or sulphur atom; and the salts thereof. The compounds may be prepared by a condensation reaction, especially in the presence of an enzyme capable of catalysing the formation of a peptide bond. The compounds may be used to form protein conjugates in which a group of interest such as another protein or peptide or an effector or reporter group is coupled to the protein through a -N-(R 1 )N(R 2 )-Z 1 -C(=X)-Z 2 -N(R 3 )N= group.

    摘要翻译: 式(1)的蛋白质衍生物A-CO-N(R1)N(R2)-Z1-其中A-CO是蛋白质或肽A-CO2H的残基(尤其是其中-CO2H是C端羧基 蛋白质或肽); R 1,R 2,R 3和R 4可以相同或不同,并且可以存在或不存在,各自为间隔基团,X为氧或硫原子; 及其盐。 化合物可以通过缩合反应来制备,特别是在能够催化形成肽键的酶的存在下。 该化合物可用于形成蛋白质偶联物,其中一组目的基团如另一种蛋白质或肽或效应物或报道基团通过-N-(R 1)N(R 2)-Z 1 -C(= X)-Z 2 -N(R 3)N =基团。