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Host Defence Cryptides from Human Apolipoproteins: Applications in Medicinal Chemistry.
Current Topics in Medicinal Chemistry ( IF 3.4 ) Pub Date : 2020-05-01 , DOI: 10.2174/1568026620666200427091454
Rosa Gaglione 1 , Elio Pizzo 2 , Eugenio Notomista 2 , Cesar de la Fuente-Nunez 3 , Angela Arciello 1, 4
Affiliation  

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 cryptome 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 (HDPs) 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.



中文翻译:

来自人类载脂蛋白的宿主防御肽:在药物化学中的应用。

具有确定的生理作用的几种真核蛋白可以充当被宿主和/或细菌蛋白酶切割后释放的隐秘生物活性肽的前体。基于此,术语“密码组”已被用于定义蛋白质组中包含蛋白质的独特部分,该蛋白质具有在蛋白水解切割后产生生物活性肽(隐)和蛋白质(隐蛋白)的能力。因此,密码学代表具有潜在药理学意义的肽的来源。在真核生物前体蛋白中,人载脂蛋白起着重要作用,因为已经从载脂蛋白E,B和AI序列中鉴定并鉴定了有希望的生物活性肽。人类载脂蛋白衍生的肽已显示具有抗菌,抗生物膜,抗病毒,抗炎,抗动脉粥样硬化,抗氧化剂或抗癌活性的体外测定,在某些情况下,还包括动物模型的体内实验。本文介绍了迄今为止在人类载脂蛋白中鉴定出的最有趣的宿主防御肽(HDP),重点是其可用于生物医学的生物学活性。总体而言,已报道的证据清楚地表明,隐肽代表了有希望的模板,用于产生抗传染病的新药和疗法。

更新日期:2020-05-01
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