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药物化学中的聚糖:一种未被充分利用的资源。

Glycans in Medicinal Chemistry: An Underexploited Resource.

作者信息

Fernández-Tejada Alberto, Cañada F Javier, Jiménez-Barbero Jesús

机构信息

Chemical and Physical Biology, Centro de Investigaciones Biológicas (CIB-CSIC), Ramiro de Maeztu 9, 28040 Madrid (Spain).

CIC bioGUNE: Center for Cooperative Research in Biosciences, Bizkaia Technology Park, 48160 Derio (Spain).

出版信息

ChemMedChem. 2015 Aug;10(8):1291-5. doi: 10.1002/cmdc.201500107. Epub 2015 May 14.

DOI:10.1002/cmdc.201500107
PMID:25974358
Abstract

The biological relevance of glycans as mediators of key physiological processes, including disease-related mechanisms, makes them attractive targets for a wide range of medical applications. Despite their important biological roles, especially as molecular recognition elements, carbohydrates have not been fully exploited as therapeutics mainly due to the scarcity of structure-activity correlations and their non-drug-like properties. A more detailed understanding of the complex carbohydrate structures and their associated functions should contribute to the development of new glycan-based pharmaceuticals. Recent significant progress in oligosaccharide synthesis and chemical glycobiology has renewed the interest of the medicinal chemistry community in carbohydrates. This promises to increase our possibilities to harness them in drug discovery efforts for the development of new and more effective, synthetic glycan-based therapeutics and vaccines.

摘要

聚糖作为关键生理过程(包括疾病相关机制)的介质,其生物学相关性使其成为广泛医学应用的有吸引力的靶点。尽管它们具有重要的生物学作用,尤其是作为分子识别元件,但碳水化合物尚未被充分开发用作治疗药物,主要原因是结构 - 活性关系稀缺以及它们具有非药物样性质。对复杂碳水化合物结构及其相关功能的更详细了解应有助于新型基于聚糖的药物的开发。寡糖合成和化学生物糖学最近取得的重大进展重新激发了药物化学界对碳水化合物的兴趣。这有望增加我们在药物发现工作中利用它们开发新型、更有效、基于合成聚糖的治疗药物和疫苗的可能性。

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引用本文的文献

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Biocatalyzed Synthesis of Glycostructures with Anti-infective Activity.具有抗感染活性的糖结构的生物催化合成。
Acc Chem Res. 2022 Sep 6;55(17):2409-2424. doi: 10.1021/acs.accounts.2c00136. Epub 2022 Aug 9.
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Natural and synthetic carbohydrate-based vaccine adjuvants and their mechanisms of action.天然和合成的碳水化合物基疫苗佐剂及其作用机制。
Nat Rev Chem. 2021;5(3):197-216. doi: 10.1038/s41570-020-00244-3. Epub 2021 Jan 25.
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Glycans in drug discovery.药物研发中的聚糖
Medchemcomm. 2019 Jul 26;10(10):1678-1691. doi: 10.1039/c9md00292h. eCollection 2019 Oct 1.
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Developments in Carbohydrate-Based Cancer Therapeutics.基于碳水化合物的癌症治疗学进展
Pharmaceuticals (Basel). 2019 Jun 4;12(2):84. doi: 10.3390/ph12020084.
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Imidazolium-labeled glycosides as probes to harness glycosyltransferase activity in human breast milk.咪唑鎓标记的糖苷作为利用人母乳中糖基转移酶活性的探针。
Org Biomol Chem. 2017 May 3;15(17):3575-3579. doi: 10.1039/c7ob00550d.