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    Trigramin - a platelet aggregation inhibiting polypeptide
    4.
    发明授权
    Trigramin - a platelet aggregation inhibiting polypeptide 失效
    Trigramin - 一种血小板聚集抑制多肽

    公开(公告)号：US5066592A

    公开(公告)日：1991-11-19

    申请号：US584820

    申请日：1990-09-19

    申请人： Tur-Fu Huang ,  Stefan Niewiarowski ,  John C. Holt ,  Hanna Lukasiewicz

    发明人： Tur-Fu Huang ,  Stefan Niewiarowski ,  John C. Holt ,  Hanna Lukasiewicz

    IPC分类号： A61K38/00 ,  C07K14/46 ,  C12N5/08

    CPC分类号： C07K14/46 ,  A61K38/00 ,  Y10S514/822 ,  Y10S530/856

    摘要： Trigramin, a 72-amino acid polypeptide, has the following amino acid sequence: EAGEDCDCGSPANPCCDAATCKLIPGAQCGEGLCCDQCSFIEEGTVCRIARGDDLDDYCNGRSAGCPRNPFH. The molecule is a potent inhibitor of fibrinogen binding to receptors expressed on the glycoprotein IIb/IIIa complex in the membrane of platelets. Trigramin is thus a potent inhibitor of fibrinogen-induced human platelet aggregation. It is useful in inhibiting the formation of hemostatic platelet plugs.

    摘要翻译： Trigramin是一个72个氨基酸的多肽，具有以下氨基酸序列：EAGEDCDCGSPANPCCDAATCKLIPGAQCGEGLCCDQCSFIEEGTVCRIARGDDLDDYCNGRSAGCPRNPFH。 该分子是与血小板膜上的糖蛋白IIb / IIIa复合体上表达的受体结合的纤维蛋白原的有效抑制剂。 因此，Trigramin是纤维蛋白原诱导的人血小板聚集的有效抑制剂。 它可用于抑制止血血小板塞的形成。

    Disintegrin variants and their use in treating osteoporosis-induced bone loss and angiogenesis-related diseases
    5.
    发明授权
    Disintegrin variants and their use in treating osteoporosis-induced bone loss and angiogenesis-related diseases 有权
    Disintegrin变体及其在治疗骨质疏松症引起的骨丢失和血管发生相关疾病中的应用

    公开(公告)号：US07943728B2

    公开(公告)日：2011-05-17

    申请号：US12004045

    申请日：2007-12-20

    申请人： Woei-Jer Chuang ,  Wen-Mei Fu ,  Tur-Fu Huang ,  Wenya Huang ,  Chih-Hsin Tang ,  Chiu-Yueh Chen

    发明人： Woei-Jer Chuang ,  Wen-Mei Fu ,  Tur-Fu Huang ,  Wenya Huang ,  Chih-Hsin Tang ,  Chiu-Yueh Chen

    IPC分类号： A61K38/00 ,  A61K38/04 ,  C07K2/00 ,  C07K4/00 ,  C07K5/00 ,  C07K7/00 ,  C07K14/00 ,  C07K16/00 ,  C07K17/00 ,  C12P21/06 ,  C12P15/00 ,  C12N15/74 ,  A01N37/18

    CPC分类号： C07K14/46 ,  A61K38/00 ,  C07K14/745

    摘要： Disintegrin variants and pharmaceutical uses thereof are disclosed. The disintegrin variant includes an isolated polypeptide that has integrin αvβ3 receptor-antagonist activity and substantially reduced integrin αllbβ3 and/or α5β1 receptor-blocking activity as compared to a wild-type disintegrin. The variant is encoded by a modified disintegrin nucleotide sequence that encodes a modified amino acid sequence, resulting in a polypeptide having substantially reduced affinity to integrin αllbβ3 and/or α5β1 as compared to a wild-type disintegrin. The variant is useful for treatment and/or prevention of αvβ3 integrin-associated diseases in a mammal, which include osteoporosis, bone tumor or cancer growth, angiogenesis-related tumor growth and metastasis, tumor metastasis in bone, malignancy-induced hypercalcemia, angiogenesis-related eye diseases, Paget's disease, rheumatic arthritis, and osteoarthritis. The angiogenesis-related eye diseases include age-related macular degeneration, diabetic retinopathy, corneal neovascularizing diseases, ischaemia-induced neovascularizing retinopathy, high myopia, and retinopathy of prematurity.

    摘要翻译： 公开了解聚体变体及其药物用途。 去整合素变体包含与野生型去整合素相比具有整联蛋白αv＆bgr 3受体 - 拮抗剂活性和显着降低的整合素α1b和bgr3和/或α5＆bgr1受体阻断活性的分离多肽。 该变体由编码修饰的氨基酸序列的修饰的整合素核苷酸序列编码，导致与野生型去整合素相比，具有显着降低的对整联蛋白αbb和bgr3和/或α5和bgr的亲和力的多肽。 该变体可用于治疗和/或预防哺乳动物中的αv＆bgr 3整联蛋白相关疾病，其包括骨质疏松症，骨肿瘤或癌症生长，血管生成相关的肿瘤生长和转移，骨中的肿瘤转移，恶性肿瘤性高钙血症， 血管生成相关眼病，佩吉特氏病，风湿性关节炎和骨关节炎。 血管生成相关的眼睛疾病包括年龄相关性黄斑变性，糖尿病性视网膜病变，角膜新生血管性疾病，缺血诱导的新生血管性视网膜病变，高度近视和早产儿视网膜病变。

    Disintegrin variants and pharmaceutical uses thereof
    6.
    发明申请
    Disintegrin variants and pharmaceutical uses thereof 有权
    消融素变体及其药物用途

    公开(公告)号：US20080188413A1

    公开(公告)日：2008-08-07

    申请号：US12004045

    申请日：2007-12-20

    申请人： Woei-Jer Chuang ,  Wen-Mei Fu ,  Tur-Fu Huang ,  Wenya Huang ,  Chih-Hsin Tang ,  Chiu-Yueh Chen

    发明人： Woei-Jer Chuang ,  Wen-Mei Fu ,  Tur-Fu Huang ,  Wenya Huang ,  Chih-Hsin Tang ,  Chiu-Yueh Chen

    IPC分类号： A61K38/16 ,  A61K38/02 ,  A61K38/08 ,  C07K2/00 ,  C07K14/00 ,  C07K7/06 ,  C12P21/00 ,  C07H21/00 ,  A61P35/00 ,  A61P19/10 ,  A61P19/02

    CPC分类号： C07K14/46 ,  A61K38/00 ,  C07K14/745

    摘要： Disintegrin variants and pharmaceutical uses thereof are disclosed. The disintegrin variant includes an isolated polypeptide that has integrin αvβ3 receptor-antagonist activity and substantially reduced integrin αllbβ3 and/or α5β1 receptor-blocking activity as compared to a wild-type disintegrin. The variant is encoded by a modified disintegrin nucleotide sequence that encodes a modified amino acid sequence, resulting in a polypeptide having substantially reduced affinity to integrin αllbβ3 and/or α5β1 as compared to a wild-type disintegrin. The variant is useful for treatment and/or prevention of αvβ3 integrin-associated diseases in a mammal, which include osteoporosis, bone tumor or cancer growth, angiogenesis-related tumor growth and metastasis, tumor metastasis in bone, malignancy-induced hypercalcemia, angiogenesis-related eye diseases, Paget's disease, rheumatic arthritis, and osteoarthritis. The angiogenesis-related eye diseases include age-related macular degeneration, diabetic retinopathy, corneal neovascularizing diseases, ischaemia-induced neovascularizing retinopathy, high myopia, and retinopathy of prematurity.

    摘要翻译： 公开了解聚体变体及其药物用途。 去整合素变体包含与野生型去整合素相比具有整合素α1受体 - 拮抗剂活性的分离的多肽和显着降低的整联蛋白α1bβ3和/或α5β1受体阻断活性。 该变体由编码修饰的氨基酸序列的修饰的整合素核苷酸序列编码，导致与野生型去整合素相比，具有显着降低的对整联蛋白αββ和/或α5β1的整合素的多肽的多肽。 该变体可用于治疗和/或预防哺乳动物中的α2β1整联蛋白相关疾病，其包括骨质疏松症，骨肿瘤或癌症生长，血管生成相关的肿瘤生长和转移，骨中的肿瘤转移，恶性肿瘤性高钙血症，血管生成 - 相关的眼睛疾病，佩吉特氏病，风湿性关节炎和骨关节炎。 血管生成相关的眼睛疾病包括年龄相关性黄斑变性，糖尿病性视网膜病变，角膜新生血管性疾病，缺血诱导的新生血管性视网膜病变，高度近视和早产儿视网膜病变。