Rational design of SAM analogues targeting SAM-II riboswitch aptamer.

Ham YW; Humphreys DJ; Choi S; Dayton DL

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Rational design of SAM analogues targeting SAM-II riboswitch aptamer.

机译：靶向SAM-II Riboswitch Aptamer的SAM类似物的理性设计。

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Riboswitches are noncoding RNA elements embedded in 5'-untranslated region of many bacterial mRNAs regulating gene expression in response to essential metabolites. They are unique from other RNA targets because they have evolved to form specific structural receptors for the purpose of binding small molecular metabolites suggesting that structure-based rational drug design approach may be used in designing metabolite mimics targeting riboswitches. We have developed a fluorescence binding assay for SAM-II riboswitch aptamer and identified an S-adenosylmethionine (SAM) analogue that selectively binds to SAM-II riboswitch aptamer with comparable binding affinity to its native metabolite using structure-based design approach.

机译：核糖开关是嵌入在许多细菌MRNA的5'-未翻译区域中的非沉积RNA元素，以应对基本的代谢物调节基因表达。它们是独特的其他RNA靶标，因为它们已经进化形成了形成特异性结构受体，以结合小分子代谢物，表明结构的合理药物设计方法可以用于设计靶向核糖开关的代谢物模拟。我们已经开发了SAM-II核糖开关适体的荧光结合测定，并鉴定了S-腺苷甲基硫氨氨酸（SAM）类似物，其选择性地结合SAM-II Riboswitch适体，利用基于结构的设计方法对其天然代谢物的相当结合亲和力。

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《Bioorganic and Medicinal Chemistry Letters》 |2011年第17期|共4页
作者
Ham YW; Humphreys DJ; Choi S; Dayton DL;
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Department of Chemistry and Biochemistry Brigham Young University Provo UT 84602 USA.;

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正文语种 eng
中图分类药学;
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1. Rational design of SAM analogues targeting SAM-II riboswitch aptamer. [J] . Ham YW, Humphreys DJ, Choi S, Bioorganic and Medicinal Chemistry Letters . 2011,第17期

机译：靶向SAM-II Riboswitch Aptamer的SAM类似物的理性设计。
2. A magnesium-induced triplex pre-organizes the SAM-II riboswitch [J] . Susmita Roy, Heiko Lammert, Ryan L. Hayes, PLoS Computational Biology . 2017,第3期

机译：镁诱导的Triplex预组织Sam-II Riboswitch
3. Folding of SAM-II riboswitch explored by replica-exchange molecular dynamics simulation [J] . Xu Xue, Wang Yongjun, Li Zhihong Journal of Theoretical Biology . 2015,第Null期

机译：复制-交换分子动力学模拟探索SAM-II核糖开关的折叠
4. Identification of target analogues of E3 ubiquitin ligase involved in the incidence of breast cancer: A rational drug designing approach [C] . Shreya Kumari, Priyanka Narad, Abhishek Sengupta International Conference on Bioinformatics and Systems Biology . 2018

机译：鉴定参与乳腺癌发病的E3泛素连接酶的靶类似物：一种合理的药物设计方法
5. High resolution optical tweezers for single molecule studies of hierarchical folding in the pbuE riboswitch aptamer. [D] . Foster, Daniel. 2010

机译：高分辨率光学镊子，用于pbuE核糖开关适体中的分层折叠的单分子研究。
6. Structure-guided design of fluorescent S-adenosylmethionine analogs for a high-throughput screen to target SAM-I riboswitch RNAs [O] . Scott F. Hickey, Ming C. Hammond -1

机译：荧光S-腺苷甲硫氨酸类似物的结构导向设计用于高通量筛选靶向SAM-1核糖开关RNA
7. Structure-Guided Design of Fluorescent S-Adenosylmethionine Analogs for a High-Throughput Screen to Target SAM-I Riboswitch RNAs [O] . Hickey Scott F., Hammond Ming C. 2014

机译：荧光S-腺苷甲硫氨酸类似物的结构导向设计，用于高通量筛选，靶向SAM-I Riboswitch RNA。
8. Riboswitch-Mediated Aptamer Binding for Imaging and Therapy (RABIT): A Novel Technique to Selectively Target an Intracelluar Ligand Specific for Ovarian Cancer. [R] . Kolodny, G. M., Yisraeli, J. 2015

机译：用于成像和治疗的核糖开关介导的适体结合（RaBIT）：选择性靶向卵巢癌特异性细胞内配体的新技术。

Rational design of SAM analogues targeting SAM-II riboswitch aptamer.

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