Inhibition of cell migration with synthetic peptides
    5.
    发明授权
    Inhibition of cell migration with synthetic peptides 失效
    用合成肽抑制细胞迁移

    公开(公告)号:US5547936A

    公开(公告)日:1996-08-20

    申请号:US169743

    申请日:1993-12-17

    摘要: A method of inhibiting the invasion of cells, particularly malignant cells through an extracellular membrane by contacting the membrane-cell interface with synthetic Arg-Gly-Asp-containing peptides. In one embodiment, the invention provides peptides containing the amino acid sequence Arg-Gly-Asp-Thr, more specifically Gly-Arg-Gly-Asp-Thr-Pro, which inhibits the attachment of cells to type I collagen in addition to fibronectin and vitronectin, and a method of inhibiting the attachment of cells to type I collagen. The invention further provides an assay for quantitating the invasive quality of cells by determining the amount of such peptides necessary to prevent the cells from penetrating an extracellular membrane, such as an amniotic membrane, in vitro.

    摘要翻译: 通过使膜 - 细胞界面与合成的含有Arg-Gly-Asp的合成肽接触来抑制细胞侵入的方法,特别是恶性细胞通过细胞外膜。 在一个实施方案中,本发明提供了含有氨基酸序列Arg-Gly-Asp-Thr,更特别地Gly-Arg-Gly-Asp-Thr-Pro的肽,其除了纤连蛋白以外还抑制细胞与I型胶原的连接, 玻连蛋白,以及抑制细胞对I型胶原的附着的方法。 本发明进一步提供了一种用于通过确定在体外测定防止细胞穿透细胞外膜(例如羊膜)所必需的这种肽的量来量化细胞侵入性质量的测定法。

    Antithrombotic agents and methods of use
    9.
    发明授权
    Antithrombotic agents and methods of use 失效
    抗血栓剂和使用方法

    公开(公告)号:US5858972A

    公开(公告)日:1999-01-12

    申请号:US585281

    申请日:1996-01-11

    摘要: The present invention provides antithrombotic agents useful for the management of cardiovascular disease. The agents of the subject invention are novel cyclic peptides encompassed by the following formula:Y-X.sub.1 -X.sub.2 -G-D-X.sub.3 -X.sub.4 -X.sub.5 -Z(SEQ ID NO. 1). In the above formula, X.sub.2 and X.sub.3 are independently a hydrophobic amino acid and X.sub.4 is a positively charged amino acid. The X.sub.1 and X.sub.5 substituents are independently zero to five amino acids. The amino and carboxy terminal amino acids of a given peptide can be modified according to the substituents Y and Z, respectively. The peptides are cyclized through a bridge between the two amino acids with the peptide, excluding G, D and X.sub.3 in the formation of the bridge. Peptides encompassed by the above formula can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis and conditions resulting from the development of thrombi. Unexpectedly, the above-described agents have a higher apparent affinity for GP-IIb/IIIa at low calcium concentration, which is typical at the site of a clot, as compared to at higher calcium concentration found elsewhere throughout the whole blood stream.

    摘要翻译: 本发明提供了可用于治疗心血管疾病的抗血栓形成剂。 本发明的药剂是由下式表示的新型环肽:Y-X1-X2-G-D-X3-X4-X5-Z(SEQ ID NO.1)。 在上式中,X2和X3独立地是疏水性氨基酸,X4是带正电荷的氨基酸。 X1和X5取代基独立地为0至5个氨基酸。 给定肽的氨基和羧基末端氨基酸可以分别根据取代基Y和Z进行修饰。 肽在肽的两个氨基酸之间通过桥接环化,不包括G,D和X3在桥的形成。 上述配方所涵盖的肽可以在合适的生理学上可接受的载体中施用,以治疗血栓形成和由血栓形成引起的病症。 出乎意料的是,与在整个血液流中其他地方发现的较高钙浓度相比,上述试剂在低钙浓度下具有较高的GP-IIb / IIIa表观亲和力,这在凝块部位是典型的。