Molecular Peptide Grafting as a Tool to Create Novel Protein Therapeutics.
Molecular Peptide Grafting as a Tool to Create Novel Protein Therapeutics.
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DOI：
10.3390/molecules28052383
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发表时间：
2023-03-05
期刊：
影响因子：
--
通讯作者：
Komar AA
中科院分区：
文献类型：
--
作者：
Komar AA
肽（合成的或对应于蛋白质的离散区域）的研究促进了对蛋白质结构-活性关系的理解。短肽也可用作强有力的治疗剂。然而，许多短肽的功能活性通常显著低于其亲本蛋白质的功能活性。这（通常）是由于它们的结构组织、稳定性和溶解性降低，通常导致聚集倾向增强。已经出现了几种方法来克服这些限制，其目的是将结构约束强加到治疗性肽的主链和/或侧链中（例如分子钉合、肽主链环化和分子接枝），因此加强其生物活性构象，从而改善其溶解度、稳定性和功能活性。这篇综述提供了一个简短的总结，旨在提高短功能肽的生物活性的方法，特别关注的肽移植的方法，其中一个功能肽插入到支架分子。骨架内插入短的治疗性肽到支架蛋白中已显示出增强其活性并使其具有更稳定和生物活性的构象。
The study of peptides (synthetic or corresponding to discrete regions of proteins) has facilitated the understanding of protein structure–activity relationships. Short peptides can also be used as powerful therapeutic agents. However, the functional activity of many short peptides is usually substantially lower than that of their parental proteins. This is (as a rule) due to their diminished structural organization, stability, and solubility often leading to an enhanced propensity for aggregation. Several approaches have emerged to overcome these limitations, which are aimed at imposing structural constraints into the backbone and/or sidechains of the therapeutic peptides (such as molecular stapling, peptide backbone circularization and molecular grafting), therefore enforcing their biologically active conformation and thus improving their solubility, stability, and functional activity. This review provides a short summary of approaches aimed at enhancing the biological activity of short functional peptides with a particular focus on the peptide grafting approach, whereby a functional peptide is inserted into a scaffold molecule. Intra-backbone insertions of short therapeutic peptides into scaffold proteins have been shown to enhance their activity and render them a more stable and biologically active conformation.
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影响因子：
3.9
作者：
Daly NL;Wilson DT
通讯作者：
Wilson DT
设计蛋白质 - 蛋白质相互作用的螺旋肽抑制剂。
影响因子：
6.8
作者：
Rezaei Araghi R;Keating AE
通讯作者：
Keating AE
影响因子：
7.3
作者：
Gunasekera, Sunithi;Foley, Fiona M.;Daly, Norelle L.
通讯作者：
Daly, Norelle L.
影响因子：
8
作者：
Chen, Jieming;Sawyer, Nicholas;Regan, Lynne
通讯作者：
Regan, Lynne
影响因子：
4.1
作者：
Bechtler C;Lamers C
通讯作者：
Lamers C