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通过氨基、胍基和咪唑基进行位点特异性功能化,实现10-23脱氧核酶的激活。

Site-specific functionalization with amino, guanidinium, and imidazolyl groups enabling the activation of 10-23 DNAzyme.

作者信息

Du Shanshan, Li Yang, Chai Zhilong, Shi Weiguo, He Junlin

机构信息

State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology Beijing 100850 China

School of Pharmaceutical Sciences, Guizhou University Guizhou 550025 China.

出版信息

RSC Adv. 2020 May 19;10(32):19067-19075. doi: 10.1039/d0ra02226h. eCollection 2020 May 14.

Abstract

10-23 DNAzyme has been extensively explored as a therapeutic and biotechnological tool, as well as in DNA computing. Faster cleavage or transformation is always needed. The present research displays a rational modification approach for a more efficient DNAzyme. In the catalytic core, amino, guanidinium and imidazolyl groups were introduced for its chemical activation through the adenine base. Among the six adenine residues, A9 is the unique residue that realizes all the positive effects; the 6-amino and 8-position of adenine and the 7-position of 8-aza-7-deaza-adenine could be used for the introduction of the functional groups. A12 is a new choice for catalytic improvement with an 8-substituent. Therefore, more active DNAzymes could be expected by this nucleobase-modified activation approach.

摘要

10-23脱氧核酶已被广泛探索作为一种治疗和生物技术工具,以及用于DNA计算。总是需要更快的切割或转化。本研究展示了一种用于更高效脱氧核酶的合理修饰方法。在催化核心中,通过腺嘌呤碱基引入氨基、胍基和咪唑基以实现其化学活化。在六个腺嘌呤残基中,A9是实现所有积极效应的独特残基;腺嘌呤的6-氨基和8位以及8-氮杂-7-脱氮腺嘌呤的7位可用于引入官能团。A12是具有8-取代基的催化改进的新选择。因此,通过这种核碱基修饰的活化方法有望获得更具活性的脱氧核酶。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bda3/9053948/3916adfc09ac/d0ra02226h-s1.jpg

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