IMPROVED METHOD AND AGENTS FOR INHIBITING PROTEIN AGING
    2.
    发明申请
    IMPROVED METHOD AND AGENTS FOR INHIBITING PROTEIN AGING 审中-公开
    改进的抑制蛋白质老化的方法和试剂

    公开(公告)号:WO1997018223A1

    公开(公告)日:1997-05-22

    申请号:PCT/US1996018469

    申请日:1996-11-15

    CPC classification number: G01N33/6842 A61K31/11 C07H9/06 C07H19/01 G01N33/68

    Abstract: The present invention relates to compositions and methods for inhibiting the aging of amino-containing amino acid, peptides, proteins and biomolecules. Accordingly, a composition is disclosed which comprises an agent or compound capable of reacting with the glycosyl-amino moiety of the early glycosylation product (also known as the Amadori product or the Heyns product) formed by the reaction of glucose, or other reactive sugars, with an amino-containing peptide, protein or biomolecule, thus stabilizing this early glycosylation product, and preventing its further reaction to form open-chain, carbonyl-containing advanced glycosylation end products. Suitable agents may contain a reactive aldehyde group. A preferred agent is acetaldehyde. The method comprises contacting the target biomolecule with the composition. The compounds so obtained are represented by formulae (VI) and (VIII) wherein R is the residue of an amino-containing biomolecule such as a peptide and CH2R' is the residue of the reactive aldhehyde group. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.

    Abstract translation: 本发明涉及抑制含氨基酸,肽,蛋白质和生物分子的老化的组合物和方法。 因此,公开了一种组合物,其包含能够与由葡萄糖或其它反应性糖反应形成的早期糖基化产物(也称为Amadori产物或Heyns商品)的糖基 - 氨基部分反应的试剂或化合物, 含有氨基的肽,蛋白质或生物分子,从而稳定该早期糖基化产物,并防止其进一步反应形成开链的含羰基的高级糖基化终产物。 合适的试剂可以含有反应性醛基。 优选的试剂是乙醛。 该方法包括使目标生物分子与组合物接触。 如此获得的化合物由式(VI)和(VIII)表示,其中R是含氨基的生物分子的残基,例如肽,而CH2R'是反应性脱乙酰基的残基。 预想到本发明的工业和治疗应用,因为可以处理食物腐败和动物蛋白质老化。

    TREATMENT OF HIV-INFECTION BY INTERFERING WITH HOST CELL CYCLOPHILIN RECEPTOR ACTIVITY
    4.
    发明申请
    TREATMENT OF HIV-INFECTION BY INTERFERING WITH HOST CELL CYCLOPHILIN RECEPTOR ACTIVITY 审中-公开
    通过干扰宿主细胞环磷酰胺受体活性来治疗艾滋病毒感染

    公开(公告)号:WO1997033604A1

    公开(公告)日:1997-09-18

    申请号:PCT/US1997003819

    申请日:1997-03-12

    CPC classification number: C07K16/40 A61K38/13 A61K38/52

    Abstract: There is disclosed pharmaceutical compositions for the treatment of HIV-infection using cyclophilin A and its corresponding human cellular binding partner as a target for intervention. There is further disclosed a method of using cyclophilins, anti-cyclophilin antibodies, and pegylated cyclosporin A as a treatment for HIV-infection. The present invention further provides screening assays for the identification of compounds which inhibit the interaction of cyclophilin and its cellular receptor.

    Abstract translation: 公开了使用亲环蛋白A及其相应的人细胞结合配偶体作为干预靶标来治疗HIV感染的药物组合物。 还公开了使用亲环蛋白,抗亲环蛋白抗体和聚乙二醇化环孢菌素A作为HIV感染治疗的方法。 本发明进一步提供了用于鉴定抑制亲环蛋白及其细胞受体的相互作用的化合物的筛选试验。

    SCREENING ASSAY FOR THE IDENTIFICATION OF INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR
    5.
    发明申请
    SCREENING ASSAY FOR THE IDENTIFICATION OF INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR 审中-公开
    用于识别大量移动抑制因子抑制剂的筛选测定

    公开(公告)号:WO1997029635A1

    公开(公告)日:1997-08-21

    申请号:PCT/US1997002448

    申请日:1997-02-14

    CPC classification number: A61K31/404 A61K38/00 C07K14/52

    Abstract: There is disclosed assays to identify compounds that inhibit an enzymatic activity of MIF (macrophage migration inhibitory factor). The enzyme activity catalyzes a tautomerization of MIF-substrates, such as D-dopachrome to DHICA. In general, the assay is conducted in vitro by adding, mixing or combining MIF polypeptide and a suitable substrate in the presence or absence of a test compound, and measuring the tautomerization of the substrate. The test compounds that inhibit tautomerization in the assay are identified as MIF inhibitors.

    Abstract translation: 公开了鉴定抑制MIF的酶活性(巨噬细胞迁移抑制因子)的化合物的测定法。 酶活性催化MIF-底物的互变异构,例如D-多巴色素到DHICA。 通常,通过在存在或不存在测试化合物的情况下通过加入,混合或组合MIF多肽和合适的底物并测量底物的互变异构体进行测定。 在测定中抑制互变异构化的测试化合物被鉴定为MIF抑制剂。

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