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公开(公告)号：US08937039B2
公开(公告)日：2015-01-20
申请号：US14081695
申请日：2013-11-15
申请人： Hao Zhang , Yang Shi , Hao Xu , Kirkwood A. Pritchard, Jr.
发明人： Hao Zhang , Yang Shi , Hao Xu , Kirkwood A. Pritchard, Jr.
CPC分类号： C07K5/0815 , A61K38/00 , C07K5/0821
摘要： The present invention provides peptide-based peroxidase inhibitors having the formula AA1-AA2-AA3, wherein AA1 is a positively charged, negatively charged or neutral amino acid, AA2 is a redox active amino acid, and AA3 is an amino acid possessing a reducing potential such that AA3 is capable of undergoing a redox reaction with a radical of amino acid AA2 or a retro or retro-inverso analog thereof. The result of such a combination is a highly effective inhibitor of peroxidase activity that has potent anti-inflammatory properties in widely diverse models of vascular disease and injury. Exemplary tripeptides effectively inhibit peroxidase mediated LDL oxidation, increase vasodilation in SCD mice, inhibit eosinophil infiltration and collagen deposition in asthma mice, inhibit acute lung injury, and decrease ischemic injury of the heart.
摘要翻译： 本发明提供具有式AA1-AA2-AA3的肽类过氧化物酶抑制剂，其中AA1为带正电荷的带负电荷或中性氨基酸，AA2为氧化还原活性氨基酸，AA3为具有还原电位的氨基酸 使得AA3能够与氨基酸AA2的基团或其逆反相或类似物进行氧化还原反应。 这种组合的结果是高度有效的过氧化物酶活性抑制剂，其在广泛多样化的血管疾病和损伤模型中具有有效的抗炎特性。 示例性三肽有效抑制过氧化物酶介导的LDL氧化，增加SCD小鼠的血管舒张，抑制哮喘小鼠嗜酸性粒细胞浸润和胶原蛋白沉积，抑制急性肺损伤，减少心脏缺血性损伤。
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公开(公告)号：US08673847B2
公开(公告)日：2014-03-18
申请号：US13500040
申请日：2010-10-05
申请人： Hao Zhang , Yang Shi , Hao Xu , Kirkwood A. Pritchard, Jr.
发明人： Hao Zhang , Yang Shi , Hao Xu , Kirkwood A. Pritchard, Jr.
摘要： The present invention provides peptide-based peroxidase inhibitors having the formula AA1-AA2-AA3, wherein AA1 is a positively charged, negatively charged or neutral amino acid, AA2 is a redox active amino acid, and AA3 is an amino acid possessing a reducing potential such that AA3 is capable of undergoing a redox reaction with a radical of amino acid AA2 or a retro or retro-inverso analog thereof. The result of such a combination is a highly effective inhibitor of peroxidase activity that has potent anti-inflammatory properties in widely diverse models of vascular disease and injury. Exemplary tripeptides effectively inhibit peroxidase mediated LDL oxidation, increase vasodilation in SCD mice, inhibit eosinophil infiltration and collagen deposition in asthma mice, inhibit acute lung injury, and decrease ischemic injury of the heart.
摘要翻译： 本发明提供具有式AA1-AA2-AA3的肽类过氧化物酶抑制剂，其中AA1为带正电荷的带负电荷或中性氨基酸，AA2为氧化还原活性氨基酸，AA3为具有还原电位的氨基酸 使得AA3能够与氨基酸AA2的基团或其逆反相或类似物进行氧化还原反应。 这种组合的结果是高度有效的过氧化物酶活性抑制剂，其在广泛多样化的血管疾病和损伤模型中具有有效的抗炎特性。 示例性三肽有效抑制过氧化物酶介导的LDL氧化，增加SCD小鼠的血管舒张，抑制哮喘小鼠嗜酸性粒细胞浸润和胶原蛋白沉积，抑制急性肺损伤，减少心脏缺血性损伤。
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