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    Antiproliferative activity of microsclerodermins
    1.
    发明授权
    Antiproliferative activity of microsclerodermins 有权
    微生物的抗增殖活性

    公开(公告)号：US06384187B1

    公开(公告)日：2002-05-07

    申请号：US09568692

    申请日：2000-05-11

    Applicant: Amy E. Wright ,  Shirley A. Pomponi ,  Ross E. Longley ,  Richard A. Isbrucker

    Inventor： Amy E. Wright ,  Shirley A. Pomponi ,  Ross E. Longley ,  Richard A. Isbrucker

    IPC: C07K750

    CPC classification number: C07K7/56 ,  A61K38/00

    Abstract: The subject invention pertains to a series of cyclic peptides known as the microsclerodermins, which possess unusual amino acids, and which have been observed to inhibit the proliferation of tumor cell lines. The subject invention also pertains to methods useful in inhibiting pathological cellular proliferation in animals, including humans and other mammals. In accordance with the teachings of the subject invention, microsclerodermin compounds can be used to inhibit cellular proliferation including that which is responsible for tumors and other cancers. In a specific embodiment, the novel compositions and methods of use of the subject invention can advantageously be useful in the treatment of a patient hosting cancer cells, for example, inhibiting the growth of tumor cells in a mammalian host.

    Abstract translation: 本发明涉及一系列已知为具有不寻常氨基酸的微小霉菌的环状肽，其已被观察到抑制肿瘤细胞系的增殖。 本发明还涉及可用于抑制动物（包括人类和其他哺乳动物）的病理性细胞增殖的方法。 根据本发明的教导，可以使用微细胞毒素化合物来抑制细胞增殖，包括负责肿瘤和其它癌症的细胞增殖。 在一个具体实施方案中，本发明的新颖组合物和使用方法可以有利地用于治疗宿主癌细胞的患者，例如抑制哺乳动物宿主中肿瘤细胞的生长。

    Discalamide compounds and their use as anti-proliferative agents
    5.
    发明授权
    Discalamide compounds and their use as anti-proliferative agents 失效
    仙客来酰胺化合物及其作为抗增殖剂的用途

    公开(公告)号：US06476065B2

    公开(公告)日：2002-11-05

    申请号：US09835692

    申请日：2001-04-16

    Applicant: Sarath P. Gunasekera ,  Ross E. Longley ,  Gopal K. Paul ,  Richard A. Isbrucker ,  Shirley A. Pomponi

    Inventor： Sarath P. Gunasekera ,  Ross E. Longley ,  Gopal K. Paul ,  Richard A. Isbrucker ,  Shirley A. Pomponi

    IPC: A61K31335

    CPC classification number: C07D493/04 ,  A61K31/70

    Abstract: The subject invention provides novel biologically active compounds which are useful for inhibiting cellular proliferation. Because of the biological activity of these compounds, they can be used for immunomodulation and/or treating cancer. In a preferred embodiment, the novel compounds, compositions and methods of use of the subject invention can advantageously be used to inhibit the growth of tumor cells in a mammalian host. More particularly, the subject compounds can be used for inhibiting in a human the growth of tumor cells, including cells of breast, colon, CNS, ovarian, renal, prostate, bone, gastrointestinal, stomach, testicular, or lung tumors, as well as human leukemia or melanoma cells. Specifically exemplified are discalamides A and B.

    Abstract translation: 本发明提供了可用于抑制细胞增殖的新型生物活性化合物。 由于这些化合物的生物活性，它们可用于免疫调节和/或治疗癌症。 在优选的实施方案中，本发明的新颖化合物，组合物和使用方法可有利地用于抑制哺乳动物宿主中肿瘤细胞的生长。 更具体地，本发明化合物可用于在人体中抑制肿瘤细胞（包括乳腺，结肠，CNS，卵巢，肾，前列腺，骨，胃肠，胃，睾丸或肺肿瘤）的生长，以及 人白血病或黑素瘤细胞。 具体举例说明的是甲酰胺A和B.

    Use of imidazole and indole compounds as inhibitors of nitric oxide synthase
    6.
    发明授权
    Use of imidazole and indole compounds as inhibitors of nitric oxide synthase 失效
    使用咪唑和吲哚化合物作为一氧化氮合成酶的抑制剂

    公开(公告)号：US6087363A

    公开(公告)日：2000-07-11

    申请号：US356171

    申请日：1999-07-16

    Applicant: Ross E. Longley ,  Richard A. Isbrucker ,  Amy E. Wright

    Inventor： Ross E. Longley ,  Richard A. Isbrucker ,  Amy E. Wright

    IPC: A61K31/4178 ,  A61K31/497 ,  A61K31/495

    CPC classification number: A61K31/4178 ,  A61K31/497

    Abstract: Imidazole and indole compounds were found to inhibit neural nitric oxide synthase (bNOS) activity. Nortopsentin-C inhibited bNOS as well as calcineurin activities suggesting that its actions are directed against calmodulin, a co-factor common to these two enzymes. Two indole compounds, as well as dragmacidin-D, inhibited bNOS, but not calcineurin, activity. Murine macrophage viability and induced NOS (iNOS) activity in cultured cells was also unaffected by these compounds.

    Abstract translation: 发现咪唑和吲哚化合物抑制神经一氧化氮合酶（bNOS）活性。 诺芬汀C抑制bNOS以及钙调神经磷酸酶活性，表明其作用是针对钙调蛋白，这是这两种酶共同的辅因子。 两种吲哚化合物以及dragmacidin-D抑制bNOS，但不抑制钙调神经磷酸酶的活性。 培养细胞中的鼠巨噬细胞活力和诱导的NOS（iNOS）活性也不受这些化合物的影响。

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