摘要
背景:肽和基于肽的治疗剂是划定重要化学空间的生物分子,可将小分子与生物治疗剂(如抗体、重组蛋白和蛋白质结构域)联系起来。 简介: 环寡肽和缩肽,尤其是蓝藻衍生的噻唑啉基多肽 (CTBC),由于其独特的结构特征和有趣的生物作用,表现出广泛的药理活性,为药物发现提供了有希望的线索。 方法:在本研究中,我们全面回顾了 CTBCs 的天然来源、区分化学成分和相关的生物特征。我们分析了它们的结构特性,计算了生物学描述的作用方式,这使得 CTBCs 成为出现基于肽的前瞻性疗法不可或缺的来源。在这种情况下,还简要讨论了金属有机框架及其生物医学应用。首先,给出了基于肽的疗法的挑战、方法和临床状态。 结果:基于这些分析,CTBC 可以被评估为理想的药物靶点,这对于传统的小分子一直是一个挑战,例如那些参与蛋白质-蛋白质相互作用的小分子,或者将被开发为潜在的癌症靶向纳米材料。这些环寡肽的环化诱导降低的构象自由度有助于改善代谢稳定性和与其分子靶标的结合亲和力。几种环肽的临床成功引发了天然产物样环肽的大型文库筛选和合成,以解决未满足的医疗需求。 结论:CTBCs可以被认为是最有前途的药物发现先导化合物。采用先进的生物和生物制药策略的融合可能会使这些环肽成为未来治疗应用的潜在生物分子。
关键词: 唑啉基肽,蓝藻,噻唑啉,细胞毒性,全合成,SAR,环缩肽。
Current Medicinal Chemistry
Title:Natural Thiazoline-Based Cyclodepsipeptides from Marine Cyanobacteria: Chemistry, Bioefficiency and Clinical Aspects
Volume: 28 Issue: 38
关键词: 唑啉基肽,蓝藻,噻唑啉,细胞毒性,全合成,SAR,环缩肽。
摘要:
Background: Peptides and peptide-based therapeutics are biomolecules that demarcate a significant chemical space to bridge small molecules with biological therapeutics, such as antibodies, recombinant proteins, and protein domains.
Introduction: Cyclooligopeptides and depsipeptides, particularly cyanobacteria-derived thiazoline-based polypeptides (CTBCs), exhibit a wide array of pharmacological activities due to their unique structural features and interesting bioactions, which furnish them as promising leads for drug discovery.
Methods: In the present study, we comprehensively review the natural sources, distinguishing chemistries, and pertinent bioprofiles of CTBCs. We analyze their structural peculiarities counting the mode of actions for biological portrayals which render CTBCs as indispensable sources for emergence of prospective peptide-based therapeutics. In this milieu, metal organic frameworks and their biomedical applications are also briefly discussed. To boot, the challenges, approaches, and clinical status of peptide-based therapeutics are conferred.
Results: Based on these analyses, CTBCs can be appraised as ideal drug targets that have always remained a challenge for traditional small molecules, like those involved in protein- protein interactions or to be developed as potential cancer-targeting nanomaterials. Cyclization-induced reduced conformational freedom of these cyclooligopeptides contribute to improved metabolic stability and binding affinity to their molecular targets. Clinical success of several cyclic peptides provokes the large library-screening and synthesis of natural product-like cyclic peptides to address the unmet medical needs.
Conclusion: CTBCs can be considered as the most promising lead compounds for drug discovery. Adopting the amalgamation of advanced biological and biopharmaceutical strategies might endure these cyclopeptides to be prospective biomolecules for futuristic therapeutic applications in the coming times.
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Cite this article as:
Natural Thiazoline-Based Cyclodepsipeptides from Marine Cyanobacteria: Chemistry, Bioefficiency and Clinical Aspects, Current Medicinal Chemistry 2021; 28 (38) . https://dx.doi.org/10.2174/0929867328666210526095436
DOI https://dx.doi.org/10.2174/0929867328666210526095436 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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