PROCESS FOR THE DETERMINATION OF THE PRIMARY STRUCTURE OF THE MESSENGER RNA CODING FOR THE HUMAN RECOMBINANT ENDOOLIGOPEPTIDASE A (HEOPA) [AF217798]...
    1.
    发明申请
    PROCESS FOR THE DETERMINATION OF THE PRIMARY STRUCTURE OF THE MESSENGER RNA CODING FOR THE HUMAN RECOMBINANT ENDOOLIGOPEPTIDASE A (HEOPA) [AF217798]... 审中-公开
    确定人类重组内源性Aβ(HEOPA)的信使RNA编码的主要结构的方法[AF217798]

    公开(公告)号:WO2004053052A2

    公开(公告)日:2004-06-24

    申请号:PCT/BR2003/000189

    申请日:2003-12-08

    IPC: C12N

    CPC classification number: C12N9/6421

    Abstract: This invention refers to the recombinant human endooligopeptidase (hEOPA), polynucleotide which codes for the hEOPA, polynucleotide which allow the expression of the EOPA in prokaryotes and eukaryotes, including the human beings; use of the synthetic substrates for the determination of the proteolytic activity of the hEOPA, or of its chaperon activity or its activity as soluble peptide receptor; obtaining and using of the specific antibodies and inhibitors of its oligopeptide binding activity, as agonists, competitors and antagonists, which are able to disturb its interaction and the complex formation with other proteins. The invention also refers to the application of the natural and recombinant protein, chemically or genetically modified which aim is the diagnosis and/or the application in congenital, infectious and degenerative pathologic conditions of the central nervous system, and for psychiatric and behavioral dysfunctions. It is also proposed the application of the inhibitors and competitors for the interaction of EOPA with ligands, including antibodies or their derivatives, for the treatment of tissular and neurodegenerative pathologies.

    Abstract translation: 本发明涉及编码hEOPA多核苷酸的重组人内寡肽酶(hEOPA)多核苷酸,其允许在原核生物和真核生物(包括人)中表达EOPA; 使用合成底物来测定hEOPA的蛋白水解活性,或其伴侣活性或其作为可溶性肽受体的活性; 获得和使用其寡肽结合活性的特异性抗体和抑制剂作为激动剂,竞争剂和拮抗剂,其能够干扰其相互作用和与其它蛋白质的复合物形成。 本发明还涉及化学或遗传修饰的天然和重组蛋白质的应用,其目的是诊断和/或在中枢神经系统的先天性,感染性和退行性病理状况中的应用,以及精神和行为功能障碍。 还提出抑制剂和竞争剂在EOPA与配体(包括抗体或其衍生物)的相互作用中的应用用于治疗组织和神经退行性病变。

    USO DE COMPOSTOS QUÍMICOS CAPAZES DE INIBIR A AÇÃO TÓXICA DAS ESFINGOMIE-LINASE D DO VENENO DE ARANHAS LOXOSCELES E COMPOSIÇÃO FARMACÊUTICA COMPREENDENDO OS REFERIDOS COMPOSTOS
    3.
    发明申请
    USO DE COMPOSTOS QUÍMICOS CAPAZES DE INIBIR A AÇÃO TÓXICA DAS ESFINGOMIE-LINASE D DO VENENO DE ARANHAS LOXOSCELES E COMPOSIÇÃO FARMACÊUTICA COMPREENDENDO OS REFERIDOS COMPOSTOS 审中-公开
    化学化合物的使用,可以抑制丝氨酸蛋白酶D的毒性活性,并且含有化合物的药物和药物组合物

    公开(公告)号:WO2015081407A1

    公开(公告)日:2015-06-11

    申请号:PCT/BR2014/050025

    申请日:2014-12-02

    CPC classification number: A61K31/443 A61K31/404

    Abstract: A presente invenção se refere, preferencialmente, ao uso do 4-bromo-N- [ (E) - (2-metil-lH-indol-3-il) metileneamino] benzenosulfonamida e do 4-metil-3-oxo-2- (3-piridilmetileno) benzo [3, 4-b] furan-6-il-4-clorobenzenossulfonato, (compostos 5 e 6, respectivamente), os quais são compostos capazes de inibir a ação tóxica da esfingomielinases D do veneno de Loxosceles, controlando o desenvolvimento do loxoscelismo cutâneo e sistémico; redução de hemólise, inibir a lesão cutânea, inibir a dermonecrose, inibir vias de sinalização intracelular e produção de espécies reativas de oxigénio. Além do potencial terapêutico, tais inibidores podem ser usados como ferramentas no estudo da ação de esfingomielinases e fosfolipases D. A presente invenção ainda se refere a uma composição farmacêutica para o tratamento de Loxoscelismo, redução de hemólise, inibir a lesão cutânea, inibir a dermonecrose, inibir vias de sinalização intracelular e produção de espécies reativas de oxigénio, a qual compreende os referidos compostos e um veiculo farmaceuticamente aceitável.

    Abstract translation: 本发明优选地涉及4-溴-N - [(E) - (2-甲基-1H-吲哚-3-基)亚甲基氨基]苯磺酰胺和4-甲基-3-氧代-2-(3- 吡啶基亚甲基)苯并[3,4-b]呋喃-6-基-4-氯苯磺酸盐(分别为化合物5和6),它们是可以抑制来自软骨蛇毒的鞘磷脂酶D的毒性活性的化合物,控制皮肤和 全身性粘液病 减少溶血; 抑制皮肤病变的形成; 抑制皮肤坏死; 抑制细胞内信号通路和活性氧的产生。 除了其治疗潜力之外,所述抑制剂可用于研究鞘磷脂酶和磷脂酶D的活性。本发明还涉及用于治疗粘膜松解,减少溶血,抑制皮肤损伤形成,抑制皮肤坏死的药物组合物, 抑制细胞内信号传导途径和产生活性氧,其包含所述化合物和药学上可接受的载体。

    HUMAN RECOMBINANT ENDOOLIGOPEPTIDASE A (hEOPA)
    4.
    发明申请
    HUMAN RECOMBINANT ENDOOLIGOPEPTIDASE A (hEOPA) 审中-公开
    人类重组内皮抑素A(hEOPA)

    公开(公告)号:WO2004053052A3

    公开(公告)日:2006-08-03

    申请号:PCT/BR0300189

    申请日:2003-12-08

    CPC classification number: C12N9/6421

    Abstract: This invention refers to a process for the determination of the primary structure of the mRNA coding for human endooligopeptidase A (hEOPA) and its protein sequence. In addition, the invention relates to a process for the determination of the structure of the hEOPA gene and the production of recombinant hEOPA. Furthermore, the invention relates to a process of generating antibodies against hEOPA in mice.

    Abstract translation: 本发明涉及确定编码人内寡肽酶A(hEOPA)的mRNA及其蛋白质序列的一级结构的方法。 此外,本发明涉及确定hEOPA基因的结构和重组hEOPA的产生的方法。 此外,本发明涉及在小鼠中产生针对hEOPA的抗体的方法。

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