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Lasso peptides: chemical approaches and structural elucidation
Organic & Biomolecular Chemistry ( IF 3.2 ) Pub Date : 2018-06-27 00:00:00 , DOI: 10.1039/c8ob01304g
Helena Martin-Gómez 1, 2, 3 , Judit Tulla-Puche 3, 4, 5, 6
Affiliation  

The discovery and development of novel constrained peptides that combine the advantages of therapeutic proteins with those of small molecules has partially prompted the re-emergence of peptides as therapeutics. In this regard, lasso peptides are characterized by both the selectivity and potency of larger protein biologics but with no or low immunogenicity, and the stability and bioavailability of small molecules. Moreover, the diverse functionality of lasso peptides and their extraordinary stability against chemical, thermal and proteolytic degradation make them attractive candidates for drug discovery. However, the chemical synthesis of lasso peptides remains a challenge due to the difficulty in building and maintaining their threaded structure. From a therapeutic point of view, these small and constrained structures would provide a new paradigm in drug discovery.

中文翻译:

套索肽:化学方法和结构阐明

结合治疗性蛋白质的优点和小分子的优点的新型受约束肽的发现和开发,部分地促使了作为治疗剂的肽的重新出现。在这方面,套索肽的特征在于较大的蛋白质生物制剂的选择性和效力,但没有或具有低的免疫原性,以及小分子的稳定性和生物利用度。此外,套索肽的各种功能及其对化学,热和蛋白水解降解的非凡稳定性使其成为药物开发的有吸引力的候选对象。然而,由于难以建立和维持其套索结构,套索肽的化学合成仍然是一个挑战。从治疗的角度来看,
更新日期:2018-06-27
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