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Host Defence Cryptides from Human Apolipoproteins: Applications in Medicinal Chemistry

机译:来自人载脂蛋白的宿主防治:药用化学应用

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摘要

Several eukaryotic proteins with defined physiological roles may act as precursors of cryptic bioactive peptides released upon protein cleavage by the host and/or bacterial proteases. Based on this, the term "cryptome" has been used to define the unique portion of the proteome encompassing proteins with the ability to generate bioactive peptides (cryptides) and proteins (crypteins) upon proteolytic cleavage. Hence, the cryptotne represents a source of peptides with potential pharmacological interest. Among eukaryotic precursor proteins, human apolipoproteins play an important role, since promising bioactive peptides have been identified and characterized from apolipoproteins E, B, and A-I sequences. Human apolipoproteins derived peptides have been shown to exhibit antibacterial, anti-biofilm, antiviral, anti-inflammatory, anti-atherogenic, antioxidant, or anticancer activities in in vitro assays and, in some cases, also in in vivo experiments on animal models. The most interesting Host Defence Peptides (I IDPs) identified thus far in human apolipoproteins are described here with a focus on their biological activities applicable to biomedicine. Altogether, reported evidence clearly indicates that cryptic peptides represent promising templates for the generation of new drugs and therapeutics against infectious diseases.
机译:具有定义的生理作用的若干真核蛋白质可以充当宿主和/或细菌蛋白酶对蛋白质切割时释放的隐秘生物活性肽的前体。基于此,术语“密码组”已被用于定义包含在蛋白水解裂解上产生生物活性肽(加密)和蛋白质(加密素)的蛋白质的独特部分。因此,Cryptotne代表具有潜在的药理学兴趣的肽来源。在真核前体蛋白中,人载体蛋白在发挥重要作用,因为已经鉴定出了有望的生物活性肽,并且用脂素蛋白E,B和A-I序列表征。已经显示人载脂蛋白衍生的肽在体外测定中表现出抗菌,抗生物膜,抗炎症,抗炎,抗炎,抗氧化剂,抗血液,抗氧化剂或抗癌活性,并且在某些情况下也在动物模型的体内实验中。迄今为止鉴定的最有趣的宿主防御肽(I IDPS)在此描述于专注于适用于生物医学的生物学活性。总的来说,报告的证据表明隐秘肽代表了产生新药和治疗传染病的有前途的模板。

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