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    Sperm-specific AKAP protein genes and uses
    2.
    发明授权
    Sperm-specific AKAP protein genes and uses 失效
    精子特异性AKAP蛋白基因及用途

    公开(公告)号：US06451528B1

    公开(公告)日：2002-09-17

    申请号：US09268480

    申请日：1999-03-16

    申请人： Daniel W. Carr ,  Srinivasan Vijayaraghavan

    发明人： Daniel W. Carr ,  Srinivasan Vijayaraghavan

    IPC分类号： C12Q168

    CPC分类号： C12Q1/6876 ,  C07K14/47

    摘要： This invention provides isolated nucleic acid encoding sperm-specific protein kinase A anchoring proteins from mammalian species, recombinant expression constructs encoding said mammalian sperm-specific protein kinase A anchoring proteins, cells transformed with said constructs, and homogenous preparations of these proteins prepared using recombinant genetic techniques. The invention also provides analytic tools such as polyclonal antisera and monoclonal antibodies specific for said sperm-specific protein kinase A anchoring proteins of the invention. The invention also provides methods for isolating nucleic acid encoding mammalian sperm-specific protein kinase A anchoring proteins and recombinant genetic methods for producing said mammalian sperm-specific protein kinase A anchoring proteins of the invention. The invention particularly provides high throughput screening methods for screening compounds that can disrupt binding between protein kinase A and the sperm-specific protein kinase A anchoring protein and methods for determining and producing compounds, particularly antisense oligonucleotides, for inhibiting or preventing expression of sperm-specific protein kinase A anchoring protein in sperm, spermatids, or progenitor cells thereof. These methods are useful for development of effective, male-specific contraceptives, which are also provided by the invention.

    摘要翻译： 本发明提供编码来自哺乳动物物种的精子特异性蛋白激酶A锚定蛋白的分离核酸，编码所述哺乳动物精子特异性蛋白激酶A锚定蛋白的重组表达构建体，用所述构建体转化的细胞，以及使用重组遗传学制备的这些蛋白质的均质制剂 技术 本发明还提供了分析工具，例如对本发明的所述精子特异性蛋白激酶A锚定蛋白特异性的多克隆抗血清和单克隆抗体。 本发明还提供了用于分离编码哺乳动物精子特异性蛋白激酶A锚定蛋白的核酸和用于产生本发明的所述哺乳动物精子特异性蛋白激酶A锚定蛋白的重组遗传方法的方法。 本发明特别提供了用于筛选可破坏蛋白激酶A与精子特异性蛋白激酶A锚定蛋白之间的结合的化合物的高通量筛选方法，以及用于测定和产生化合物，特别是反义寡核苷酸，用于抑制或预防精子特异性表达的方法 蛋白激酶A锚定蛋白在精子，精子细胞或祖细胞中的表达。 这些方法对于开发本发明也提供的有效的男性特异性避孕药具是有用的。

    Contraceptive compositions and methods
    3.
    发明授权
    Contraceptive compositions and methods 失效
    避孕组合物和方法

    公开(公告)号：US6011013A

    公开(公告)日：2000-01-04

    申请号：US100789

    申请日：1998-06-18

    申请人： Daniel W. Carr ,  Srinivasan Vijayaraghavan

    发明人： Daniel W. Carr ,  Srinivasan Vijayaraghavan

    IPC分类号： A61K38/00 ,  C07K14/00 ,  A61K38/10 ,  A61K38/16 ,  C07K7/08

    CPC分类号： C07K14/001 ,  A61K38/00

    摘要： The present invention includes a pharmaceutical composition having an effective contraceptive amount of a synthetic peptide that includes an amphipathic .alpha.-helix domain that binds to an RII subunit of protein kinase A, and competitively inhibits the binding of protein kinase A to sperm A kinase anchoring proteins. Particular disclosed synthetic peptides having this activity include s-Ht31: N-Stearate-DLIEEAASRIVDAVIEQVKAAGAY (SEQ ID No. 9), s-Ht31-P: N-Stearate-DLIEEAASRPVDAVPEQVKAAGAY (SEQ ID No. 10), and s-AKAP79: N-Stearate-YETLLIETASSLVKNAIQLSIE (SEQ ID No. 11). The invention also includes methods of inhibiting sperm motility, by exposing them to an effective amount of the peptide, for example by placing the pharmaceutical composition (such as a suppository, foam, cream, or gel) in the vagina.

    摘要翻译： 本发明包括具有有效避孕量的合成肽的药物组合物，其包括结合蛋白激酶A的RII亚基的两亲性α-螺旋结构域，并且竞争性地抑制蛋白激酶A与精子A激酶锚定蛋白的结合 。 特别公开的具有这种活性的合成肽包括s-Ht31：N-硬脂酸酯-DLIEEAASRIVDAVIEQVKAAGAY（SEQ ID No.9），s-Ht31-P：N-硬脂酸酯-DLIEEAASRPVDAVPEQVKAAGAY（SEQ ID No.10）和s-AKAP79：N - 硬脂酸酯YETLLIETASSLVKNAIQLSIE（SEQ ID No.11）。 本发明还包括通过将它们暴露于有效量的肽，例如通过将药物组合物（例如栓剂，泡沫，乳膏或凝胶）放置在阴道中来抑制精子活力的方法。