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腺嘌呤核苷:其衍生物的合成方法及抗肿瘤活性。

Adenosine: Synthetic Methods of Its Derivatives and Antitumor Activity.

机构信息

Laboratory of Synthesis and Biological Activity, Institute of Chemistry of Naturals Resources, University of Talca, Talca, Chile.

Center for Bioinformatics and Molecular Simulation, University of Talca, Talca, Chile.

出版信息

Mini Rev Med Chem. 2018;18(20):1684-1701. doi: 10.2174/1389557518666180516163539.

Abstract

Since 1929, several researchers have conducted studies in relation to the nucleoside of adenosine (1) mainly distribution identifying, characterizing their biological importance and synthetic chemistry to which this type of molecule has been subjected to obtain multiple of its derivatives. The receptors that interact with adenosine and its derivatives, called purinergic receptors, are classified as A1, A2A, A2B and A3. In the presence of agonists and antagonists, these receptors are involved in various physiological processes and diseases. This review describes and compares some of the synthetic methods that have been developed over the last 30 years for obtaining some adenosine derivatives, classified according to substitution processes, complexation, mating and conjugation. Finally, we mention that although the concentrations of these nucleosides are low in normal tissues, they can increase rapidly in pathophysiological conditions such as hypoxia, ischemia, inflammation, trauma and cancer. In particular, the evaluation of adenosine derivatives as adjunctive therapy promises to have a significant impact on the treatment of certain cancers, although the transfer of these results to clinical practice requires a deeper understanding of how adenosine regulates the process of tumorigenesis.

摘要

自 1929 年以来,已有多位研究人员针对腺嘌呤核苷(1)进行了相关研究,主要涉及分布鉴定、生物重要性和合成化学,此类分子经历了多种衍生化以获得多种衍生物。与腺苷及其衍生物相互作用的受体称为嘌呤能受体,分为 A1、A2A、A2B 和 A3。在激动剂和拮抗剂的存在下,这些受体参与了各种生理过程和疾病。本文综述并比较了过去 30 年来用于获得一些腺苷衍生物的一些合成方法,根据取代过程、络合、配对和共轭进行了分类。最后,我们提到尽管这些核苷在正常组织中的浓度较低,但在缺氧、缺血、炎症、创伤和癌症等病理生理条件下,其浓度会迅速升高。特别是,将腺苷衍生物作为辅助治疗进行评估有望对某些癌症的治疗产生重大影响,尽管将这些结果转化为临床实践需要更深入地了解腺苷如何调节肿瘤发生过程。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/38af/6327119/2fbba1116fea/MRMC-18-1684_F1.jpg

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