Selectively cleavabe linners based on iminodiacetic acid esters for
solid phase peptide synthesis
    1.
    发明授权
    Selectively cleavabe linners based on iminodiacetic acid esters for solid phase peptide synthesis 失效
    用于固相肽合成的基于亚氨基二乙酸酯的选择性切割的接头

    公开(公告)号:US5635598A

    公开(公告)日:1997-06-03

    申请号:US263289

    申请日:1994-06-21

    CPC分类号: C07K1/042

    摘要: The present invention is directed to linkers based on ester bond linkages, especially iminodiacetic acid ester bond linkages, for use in solid phase peptide synthesis. In particular, the invention is directed to cleavable linkers that can release peptide from the solid phase support under relatively mild conditions by formation of a diketopiperazine or other cyclic structure, such that the cyclic structure remains on the solid phase support, and, in a second cleavage, under more stringent conditions of high pH. The invention is further directed to solid phase supports prepared with multiple cleavable linkers, including a linker that is cleaved by formation of a cyclic product. One such second linker is an ester of hydroxymethylbenzoic acid, or esters formed by carboxy groups of aspartic or glutamic acid.

    摘要翻译: 本发明涉及用于固相肽合成的基于酯键连接的接头,特别是亚氨基二乙酸酯键键。 特别地,本发明涉及可切割的接头,其可以通过形成二酮哌嗪或其它环状结构在相对温和的条件下从固相支持物释放肽,使得环状结构保留在固相载体上,并且在第二 在更严格的高pH条件下开裂。 本发明还涉及用多个可切割接头制备的固相载体,其包括通过形成环状产物而被切割的连接体。 一个这样的第二接头是羟甲基苯甲酸的酯,或由天冬氨酸或谷氨酸的羧基形成的酯。

    Serum thymic factor peptide analogs and process for the preparation
thereof
    2.
    发明授权
    Serum thymic factor peptide analogs and process for the preparation thereof 失效
    血清胸腺因子肽类似物及其制备方法

    公开(公告)号:US4711952A

    公开(公告)日:1987-12-08

    申请号:US875230

    申请日:1986-06-17

    摘要: Novel peptide analogs of the serum thymic factor are disclosed, structurally modified, in comparison with the natural substance, both in their N-terminal and C-terminal parts and inside the amino-acid sequence, corresponding to the general formula IA-Gly-Gly-Ser-Asn-B-C-NH-R (I),in which A is pGlu, Gln, Ala-Lys-Ser-Gln, pGlu-Ala-Lys-Ser-Gln or Gln-Ala-Lys-Ser-Gln, B and C are Gly, Phe, Leu, Ala or a direct bond, and R is H, an alkyl with 1 to 6 carbon atoms or a 2-phenylethyl. Depending upon their chemical structure, the subject thymic factor analogs possess either agonistic (immunostimulative) or antagonistic (immunosuppressory) properties.

    摘要翻译: 与天然物质相比,在其N-末端和C末端部分以及氨基酸序列内部,与通式Ⅰ-Gly-1相对应,公开了与血清胸腺因子的新型肽类似物结构上的改变, Gly-Ser-Asn-BC-NH-R(I),其中A是pGlu,Gln,Ala-Lys-Ser-Gln,pGlu-Ala-Lys-Ser-Gln或Gln-Ala-Lys-Ser-Gln ,B和C为Gly,Phe,Leu,Ala或直接键,R为H,具有1至6个碳原子的烷基或2-苯基乙基。 根据其化学结构,受试者胸腺因子类似物具有激动(免疫刺激)或拮抗(免疫抑制)特性。