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    FK-506 cytosolic binding protein
    5.
    发明授权
    FK-506 cytosolic binding protein 失效
    FK-506胞质结合蛋白

    公开(公告)号：US5109112A

    公开(公告)日：1992-04-28

    申请号：US548429

    申请日：1990-07-05

    申请人： John J. Siekierka ,  Hsuen-Yun Hung ,  Marie J. Staruch ,  Nolan H. Sigal ,  Richard A. Mumford

    发明人： John J. Siekierka ,  Hsuen-Yun Hung ,  Marie J. Staruch ,  Nolan H. Sigal ,  Richard A. Mumford

    IPC分类号： C12N9/90 ,  C12N15/90

    CPC分类号： C12N15/90 ,  C12N9/90 ,  Y10S530/81 ,  Y10S530/827

    摘要： A new homogeneous cytosolic binding (HCB) protein, having a specific binding activity of about 26 .mu.g FK-506 per mg protein and a molecular weight of about 10-12 kilodaltons, reversibly binds the immunosuppressant FK-506 but not cyclosporine A (CSA). The protein is stable to heating at 56 degrees C. for 30 minutes retaining its FK-506 binding affinity, and has the (partial) amino terminal amino acid sequence: H.sub.2 N-Gly-Val-Gln-Val-Glu-Thr-Ile-Ser-Pro- Gly-Asp-Gly-Arg-Thr-Phe-Pro-Lys- Ar g-Gly-Gln-Thr-X-Val-Val-His-Tyr-Thr-Gly-Met-Leu-Glu-Asp-Gly-Lys-Lys-Phe-Asp (wherein X is undefined). The HCB protein is isolated from the cytosol of mammalian tissues, preferably human neoplastic T-cell lines, e.g., Jurkat, and can be used in diagnostic and purification procedures involving FK-506 macrolide type immunosuppressants. The HCB protein also catalyzes the cis-trans isomerization of proline-containing peptide bonds.

    摘要翻译： 具有约26μgFK-506 / mg蛋白的特异性结合活性和约10-12千道尔顿分子量的新的均匀胞质结合（HCB）蛋白可逆地结合免疫抑制剂FK-506而不是环孢菌素A（CSA ）。 蛋白质在56℃下加热稳定30分钟，保持其FK-506结合亲和力，并具有（部分）氨基末端氨基酸序列：H2N-Gly-Val-Gln-Val-Glu-Thr-Ile- Ser-Pro-Gly-Asp-Gly-Arg-Thr-Phe-Pro-Lys-Ar g-Gly-Gln-Thr-X-Val-Val-His-Tyr-Thr-Gly-Met-Leu-Glu-Asp -Gly-Lys-Lys-Ph e-Asp（其中X未定义）。 HCB蛋白从哺乳动物组织的细胞溶质中分离，优选人类肿瘤T细胞系，例如Jurkat，并且可用于涉及FK-506大环内酯型免疫抑制剂的诊断和纯化方法。 HCB蛋白还催化含脯氨酸的肽键的顺式 - 反式异构化。

    N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors
    9.
    发明授权
    N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors 失效
    N-芳基磺酰基氮杂双环衍生物作为有效的细胞粘附抑制剂

    公开(公告)号：US06855708B2

    公开(公告)日：2005-02-15

    申请号：US10096607

    申请日：2002-03-13

    申请人： Linus S. Lin ,  George Doherty ,  Shrenik K. Shah ,  Linda L. Chang ,  William K. Hagmann ,  Richard A. Mumford

    发明人： Linus S. Lin ,  George Doherty ,  Shrenik K. Shah ,  Linda L. Chang ,  William K. Hagmann ,  Richard A. Mumford

    IPC分类号： C07D401/12 ,  C07D487/04 ,  C07D498/04 ,  A61K31/55 ,  A61K31/47

    CPC分类号： C07D401/12 ,  C07D487/04

    摘要： Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

    摘要翻译： 式I的化合物是VLA-4和/或α4/β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。 这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎， 接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症 关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。