proteins.

  • 文章类型: Journal Article
    “结构决定功能”是当前生物界的共识,但是与某种功能相对应的结构特征一直是科学探索的热点领域。肽是介于抗体和小分子大小之间的生物活性分子。尽管如此,肽的胃肠屏障和理化性质一直限制了肽的口服给药。因此,分析了肽修饰和渗透增强剂口服肽转化策略的主要途径。根据我们对天然口服肽结构的分析,可以通过胃肠道吸收,我们认为,基于二硫键的天然装订肽的设计策略有利于口服肽的设计。这不仅可用于天然抗胃肠消化结构蛋白的鉴定,也为新型口服多肽药物的构建提供了坚实的结构基础。
    \'Structure determines function\' is a consensus in the current biological community, but the structural characteristics corresponding to a certain function have always been a hot field of scientific exploration. A peptide is a bio-active molecule that is between the size of an antibody and a small molecule. Still, the gastrointestinal barrier and the physicochemical properties of peptides have always limited the oral administration of peptides. Therefore, we analyze the main ways oral peptide conversion strategies of peptide modification and permeation enhancers. Based on our analysis of the structure of natural oral peptides, which can be absorbed through the gastrointestinal tract, we believe that the design strategy of natural stapled peptides based on disulfide bonds is good for oral peptide design. This cannot only be used to identify anti-gastrointestinal digestive structural proteins in nature but also provide a solid structural foundation for the construction of new oral peptide drugs.
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  • 文章类型: Journal Article
    非常规的翻译后修饰(PTM)作为癌症发展和进展的关键参与者越来越受到关注。了解非常规PTM在癌症中的作用有可能彻底改变癌症诊断,预后,和治疗干预措施。这些修改,其中包括O-GlcNAcylation,谷胱甘肽酰化,巴豆酰化,包括数以百计的其他人,与癌细胞中关键细胞过程和信号通路的失调有关。这篇综述旨在提供对癌症中非常规PTM作为诊断标志物和治疗靶标的综合分析。本文包括回顾有关各种常规和非常规PTM在癌症生物学中的功能意义的最新知识。此外,本文重点介绍了分析技术的进步,比如生化分析,质谱和生物信息学工具等。,这使得能够检测和表征癌症中的非常规PTM。这些技术有助于鉴定与癌症亚型相关的特定PTM。非常规PTM作为生物标志物的潜在用途将进一步有助于更好的诊断并有助于发现有效的疗法。有关非常规PTM在广阔而迅速扩展的领域中的作用的知识将有助于癌症的检测和靶向治疗。
    Unconventional Post-Translational Modifications (PTMs) have gained increasing attention as crucial players in cancer development and progression. Understanding the role of unconventional PTMs in cancer has the potential to revolutionize cancer diagnosis, prognosis, and therapeutic interventions. These modifications, which include O-GlcNAcylation, glutathionylation, crotonylation, including hundreds of others, have been implicated in the dysregulation of critical cellular processes and signaling pathways in cancer cells. This review paper aims to provide a comprehensive analysis of unconventional PTMs in cancer as diagnostic markers and therapeutic targets. The paper includes reviewing the current knowledge on the functional significance of various conventional and unconventional PTMs in cancer biology. Furthermore, the paper highlights the advancements in analytical techniques, such as biochemical analyses, mass spectrometry and bioinformatic tools etc., that have enabled the detection and characterization of unconventional PTMs in cancer. These techniques have contributed to the identification of specific PTMs associated with cancer subtypes. The potential use of Unconventional PTMs as biomarkers will further help in better diagnosis and aid in discovering potent therapeutics. The knowledge about the role of Unconventional PTMs in a vast and rapidly expanding field will help in detection and targeted therapy of cancer.
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  • 文章类型: Journal Article
    背景:生物碱是从各种植物来源获得的重要植物成分。该研究的主要目标是使用分子对接研究评估生物碱的抗阿尔茨海默病潜力。阿尔茨海默病(AD)被认为是记忆力逐渐下降,推理,决策,朝向一个人的物理环境,和语言。
    方法:选择主要靶标即乙酰胆碱酯酶蛋白用于分子对接研究。
    结果:使用ChemDraw软件绘制了各种生物碱的结构,PDB从RCSBPDB数据库检索,并在MolergoVirtualDocker上进行了分子对接研究。潜在的生物碱被鉴定为具有抗阿尔茨海默病效力。
    结论:利血平,长春碱,麦角胺,发现和管草碱表现出潜在的抗阿尔茨海默病效力。
    BACKGROUND: Alkaloids are important phytoconstituents obtained from various plant sources. The study\'s primary goal is to assess the anti-Alzheimer potential of alkaloids using a molecular docking study. Alzheimer\'s disease (AD) is considered a gradual decline in memory, reasoning, decision-making, orientation to one\'s physical surroundings, and language.
    METHODS: The main target i.e. acetylcholinesterase proteins was selected for the molecular docking study.
    RESULTS: The structures of various alkaloids were drawn using Chem Draw Software, PDB was retrieved from the RCSB PDB database, and molecular docking study was performed on Molergo Virtual Docker. The potential alkaloids were identified with anti-Alzheimer potency.
    CONCLUSIONS: Reserpine, vinblastine, ergotamine, and tubocurarine were found to exhibit potential anti-Alzheimer potency.
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  • 文章类型: Journal Article
    背景:肝癌(LC)是中国最常见的恶性肿瘤之一,死亡率很高,排在胃癌和食管癌之后的第三大死亡原因。LncRNAFAM83H-AS1已被证实在LC的进展中发挥关键作用。然而,具体机制有待进一步调查。
    方法:进行定量实时PCR(qRT-PCR)以测量基因的转录水平。通过CCK8和集落形成测定确定增殖。进行Westernblot以检测相对蛋白表达。构建异种移植小鼠模型以研究LncRNAFAM83H-AS1对体内肿瘤生长和放射敏感性的影响。
    结果:lncRNAFAM83H-AS1的水平在LC中显著升高。FAM83H-AS1的敲低抑制LC细胞增殖和集落存活分数。FAM83HAS1的缺失增加了LC细胞对4GyX射线辐射的敏感性。在异种移植模型中,放疗联合FAM83H-AS1沉默可显着降低肿瘤体积和重量。FAM83H的过表达逆转了FAM83H-AS1缺失对LC细胞增殖和集落存活分数的影响。此外,FAM83H的过表达也恢复了异种移植模型中FAM83H-AS1的敲低或辐射引起的肿瘤体积和重量减少。
    结论:敲低lncRNAFAM83H-AS1抑制LC生长并增强LC的放射敏感性。它有可能成为LC治疗的有希望的靶标。
    BACKGROUND: Liver cancer (LC) is one of China\'s most common malignant tumors, with a high mortality rate, ranking third leading cause of death after gastric and esophageal cancer. Recent patents propose the LncRNA FAM83H-AS1 has been verified to perform a crucial role in the progression of LC. LncRNA FAM83H-AS1 has been verified to perform a crucial role in the progression of LC. However, the concrete mechanism remains to be pending further investigation.
    OBJECTIVE: This study aimed to explore the embedding mechanism of FAM83H-AS1 molecules in terms of radio sensitivity of LC and provide potentially effective therapeutic targets for LC therapy.
    METHODS: Quantitative real-time PCR (qRT-PCR) was conducted to measure the transcription levels of genes. Proliferation was determined via CCK8 and colony formation assays. Western blot was carried out to detect the relative protein expression. A xenograft mouse model was constructed to investigate the effect of LncRNA FAM83H-AS1 on tumor growth and radio-sensitivity in vivo.
    RESULTS: The levels of lncRNA FAM83H-AS1 were remarkably increased in LC. Knockdown of FAM83H-AS1 inhibited LC cell proliferation and colony survival fraction. Deletion of FAM83H-AS1 increased the sensitivity of LC cells to 4 Gy of X-ray radiation. In the xenograft model, radiotherapy combined with FAM83H-AS1 silencing significantly reduced tumor volume and weight. Overexpression of FAM83H reversed the effects of FAM83H-AS1 deletion on proliferation and colony survival fraction in LC cells. Moreover, the over-expressing of FAM83H also restored the tumor volume and weight reduction caused by the knockdown of FAM83H-AS1 or radiation in the xenograft model.
    CONCLUSIONS: Knockdown of lncRNA FAM83H-AS1 inhibited LC growth and enhanced radiosensitivity in LC. It has the potential to be a promising target for LC therapy.
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  • 文章类型: Journal Article
    BACKGROUND: Nucleus targeted drug delivery provides several opportunities for the treatment of fatal diseases such as cancer. However, the complex nucleocytoplasmic barriers pose significant challenges for delivering a drug directly and efficiently into the nucleus. Aptamers representing singlestranded DNA and RNA qualify as next-generation highly advanced and personalized medicinal agents that successfully inhibit the expression of certain proteins; possess extraordinary gene-expression for manoeuvring the diseased cell\'s fate with negligible toxicity. In addition, the precisely directed aptamers to the site of action present a tremendous potential to reach the nucleus by escaping the ensuing barriers to exhibit a better drug activity and gene expression.
    OBJECTIVE: This review epigrammatically highlights the significance of targeted drug delivery and presents a comprehensive description of the principal barriers faced by the nucleus targeted drug delivery paradigm and ensuing complexities thereof. Eventually, the progress of nucleus targeting with nucleic acid aptamers and success achieved so far have also been reviewed.
    METHODS: Systematic literature search was conducted of research published to date in the field of nucleic acid aptamers.
    CONCLUSIONS: The review specifically points out the contribution of individual aptamers as the nucleustargeting agent rather than aptamers in conjugated form.
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  • 文章类型: Journal Article
    Latex, a milky fluid found in several plants, is widely used for many purposes, and its proteins have been investigated by researchers. Many studies have shown that latex produced by some plant species is a natural source of biologically active compounds, and many of the hydrolytic enzymes are related to health benefits. Research on the characterization and industrial and pharmaceutical utility of latex has progressed in recent years. Latex proteins are associated with plants\' defense mechanisms, against attacks by fungi. In this respect, there are several biotechnological applications of antifungal proteins. Some findings reveal that antifungal proteins inhibit fungi by interrupting the synthesis of fungal cell walls or rupturing the membrane. Moreover, both phytopathogenic and clinical fungal strains are susceptible to latex proteins. The present review describes some important features of proteins isolated from plant latex which presented in vitro antifungal activities: protein classification, function, molecular weight, isoelectric point, as well as the fungal species that are inhibited by them. We also discuss their mechanisms of action.
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  • 文章类型: Journal Article
    BACKGROUND: Phosphodiesterases (PDEs) are enzymes that play a key role in terminating cyclic nucleotides signalling by catalysing the hydrolysis of 3\', 5\'- cyclic adenosine monophosphate (cAMP) and/or 3\', 5\' cyclic guanosine monophosphate (cGMP), the second messengers within the cell that transport the signals produced by extracellular signalling molecules which are unable to get into the cells. However, PDEs are proteins which do not operate alone but in complexes that made up of a many proteins.
    OBJECTIVE: This review highlights some of the general characteristics of PDEs and focuses mainly on the Protein-Protein Interactions (PPIs) of selected PDE enzymes. The objective is to review the role of PPIs in the specific mechanism for activation and thereby regulation of certain biological functions of PDEs.
    METHODS: The article discusses some of the PPIs of selected PDEs as reported in recent scientific literature. These interactions are critical for understanding the biological role of the target PDE.
    RESULTS: The PPIs have shown that each PDE has a specific mechanism for activation and thereby regulation a certain biological function.
    CONCLUSIONS: Targeting of PDEs to specific regions of the cell is based on the interaction with other proteins where each PDE enzyme binds with specific protein(s) via PPIs.
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  • 文章类型: Journal Article
    Biomacromolecules structures and their interaction between different systems have been extensively studied in the last years. Nevertheless, in the medicinal context, it has not been studied deeply. For this reason, the interest to investigate the behavior of different biomacromolecules such us proteins, organelles, phospholipids, etc. with soft materials has opened new research lines. Computational and experimental methodologies have tried to answer different questions that have been difficult to solve, due to the complexity of the phenomenon, as an example, competition between biomacromolecules and soft materials for a specific organ. In this review, we would like to demonstrate how soft materials influence the biomacromolecules structures and how to change their response, biodistribution and also biocompatibility for future applications.
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  • 文章类型: Journal Article
    We discuss the diverse biological activities, therapeutic potential, and clinical applications of peptides and proteins isolated from various yams species including Dioscorea opposita Thunb (Chinese yam), D alata, D japonica (Japanese yam), D pseudojaponica, D batatas (Korea yam), and D cayenensis. Yam peptides and proteins have many pharmacological activities including immunomodulatory, antioxidant, estrogen-stimulating, osteogenic, angiotensin I-converting enzyme inhibiting, carbonic anhydrase and trypsin inhibiting, chitinase, anti-insect, anti-dust mite, lectin, and anti-proliferative activities. Yam peptides and proteins have therapeutic potential for treating cardiovascular diseases, inflammatory diseases, cancers, aging disorders, menopause, and osteoporosis.
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  • 文章类型: Journal Article
    The genus Panax consists of a group of prized medicinal herbs. Major members of the Panax genus include P. ginseng, P. notoginseng, P. quinquefolius, and P. vietnamensis. They possess various bioactive constituents such as ginsenosides, saponins, polysaccharides and proteins. Many of them were reported to show beneficial effects on human health. Ginsenosides and saponins of ginsengs caught the sight of most researchers. Precise investigations revealed their roles on improvement of the functioning of the nervous system, cardiovascular system, and other functions. In contrast, our knowledge of the bioactive Panax proteins is relatively limited. A number of proteins from P. ginseng, the most valuable member of Panax species, have been investigated and proved to be beneficial to our body. Meanwhile, a few bioactive P. notoginseng proteins, such as ribonucleases and antifungal proteins, have been characterized and reported. We summarize herein the proteins present in P. notoginseng that have been identified, and try to compare them with those from other Panax species with a similar structure or bioactivity, and conclude whether the proteins in P. notoginseng have any distinctive features.
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