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公开(公告)号：US06355610B2
公开(公告)日：2002-03-12
申请号：US09823494
申请日：2001-03-30
IPC分类号： A61K3800
摘要： Peptides are disclosed that inhibit the conversion of protease sensitive prion protein (PrPsen) to the protease resistant isoform (PrPres). These peptides comprise discrete fragments of prion proteins, and are shown to inhibit the in vitro conversion of PrPsen to PrPres in a cell-free system. Numerous peptides are disclosed that include at least two amino acid residues from the highly amyloidogenic region P113-120 of the PrP protein. None of these peptides conferred protease-resistance to the PrPsen molecules. The presence of residues 119 and 120 from the highly hydrophobic sequence AGAAAAGA (position 113 to 120) produced a particular inhibitory effect. The inhibition occurred with a high degree of specificity (e.g. with an IC50 of less than about 1000 &mgr;M).
摘要翻译： 公开了抑制蛋白酶敏感性朊病毒蛋白（PrPsen）转化为蛋白酶抗性同种型（PrPres）的肽。 这些肽包含朊病毒蛋白的离散碎片，并且显示出在无细胞系统中抑制PrPsen到PrPres的体外转化。 公开了许多肽，其包括来自PrP蛋白质的高淀粉样蛋白原性区域P113-120的至少两个氨基酸残基。 这些肽都没有赋予PrPsen分子蛋白酶抗性。 来自高疏水性序列AGAAAAGA（113至120位）的残基119和120的存在产生特别的抑制作用。 抑制发生在高度的特异性（例如，IC 50小于约1000μM）。
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公开(公告)号：US06211149B1
公开(公告)日：2001-04-03
申请号：US09128450
申请日：1998-08-03
IPC分类号： A61K3800
摘要： Peptides are disclosed that inhibit the conversion of protease sensitive prion protein (PrPsen) to the protease resistant isoform (PrPres). These peptides comprise discrete fragments of prion proteins, and are shown to inhibit the in vitro conversion of PrPsen to PrPres in a cell-free system. Numerous peptides are disclosed that include at least two amino acid residues from the highly amyloidogenic region P113-120 of the PrP protein. None of these peptides conferred protease-resistance to the PrPsen molecules. The presence of residues 119 and 120 from the highly hydrophobic sequence AGAAAAGA (position 113 to 120) produced a particular inhibitory effect. The inhibition occurred with a high degree of specificity (e.g. with an IC50 of less than about 1000 &mgr;M).
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