1-Ethyl-guanosin | 39707-98-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-Ethyl-guanosin
• 英文别名: 2-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1-ethylpurin-6-one
• CAS: 39707-98-7
• 化学式: C₁₂H₁₇N₅O₅
• 分子量: 311.297
• InChiKey: XDMQEVQNZKMYNM-IOSLPCCCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  146
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• Nucleic acid drug for inducing skipping of variant exon of CD44 gene and increasing expression of normal type CD44 mRNA
  申请人：KNC LABORATORIES CO., LTD.

  公开号：US10174319B2

  公开（公告）日：2019-01-08

  Insertion of variant exons of CD44 gene of cancer stem cells into its mRNA is inhibited whereupon the cancer stem cells lose their properties so that they are rendered sensitive to anticancer agents and radiation, possibly leading to cancer treatment. A drug for cancer treatment, comprising an antisense oligonucleotide capable of inducing skipping of variant exon(s) of CD44 gene to thereby increase expression of normal CD44 mRNA, a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof. An oligonucleotide of 20-23 bp having the entirety or a part of any one of the nucleotide sequences as shown in SEQ ID NOS: 1 to 19, a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof. A drug for inducing skipping of at least one variant exon selected from the group consisting of variant exons 8, 9 and 10 of CD44 gene, comprising the above-described oligonucleotide, a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof.

  癌症干细胞CD44基因的变异外显子插入其mRNA的过程受到抑制，从而使癌症干细胞失去其特性，使其对抗癌剂和辐射敏感，可能导致癌症治疗。 一种治疗癌症的药物，包括能够诱导跳过 CD44 基因变异外显子从而增加正常 CD44 mRNA 表达的反义寡核苷酸、其药学上可接受的盐、其溶液或其原药。具有 SEQ ID NOS: 1 至 19 中所示核苷酸序列的全部或部分的 20-23 bp 的寡核苷酸、其药学上可接受的盐、其溶液或其原药。一种用于诱导至少一个选自 CD44 基因变异外显子 8、9 和 10 所组成的组中的变异外显子的跳过的药物，包括上述寡核苷酸、其药学上可接受的盐、其溶液或其原药。
• Inhibition of viruses
  申请人：Medical Research Council

  公开号：US20030130226A1

  公开（公告）日：2003-07-10

  Disclosed is a pharmaceutical composition comprising a ribonucleoside analogue in accordance with general formula I or II as herein defined, in admixture with a physiologically acceptable excipient diluent or carrier.

  本发明公开了一种药物组合物，该组合物包含符合本文定义的通式 I 或 II 的核糖核苷类似物，并与生理上可接受的赋形剂稀释剂或载体混合。
• Screening assay for hepatitis C virus antiviral agents
  申请人：——

  公开号：US20030148267A1

  公开（公告）日：2003-08-07

  The invention includes methods of identifying compounds that increase the mutation rate of hepatitis C virus. The invention can be used to screen libraries of test compounds, including both nucleoside analogs and non-nucleoside analogs. The methods include: 1) contacting a test cell with a candidate compound, wherein the test cell contains a nucleic acid molecule comprising an infectious hepatitis C viral genome, a ribozyme, and an inducible promoter operably linked to the first and second nucleotide sequences, the ribozyme being configured to remove a 3′ sequence unnecessary for replication of the infectious hepatitis C viral genome from a transcript initiated by the inducible promote; and 2) the detection of an increase in hepatitis C virus quasispecies produced by the cell in the presence of the candidate compound. Detection of an increase in quasispecies can be accomplished by, e.g., sequencing HCV nucleic acid molecules isolated from the test cell.

  本发明包括鉴定可提高丙型肝炎病毒变异率的化合物的方法。本发明可用于筛选试验化合物库，包括核苷类似物和非核苷类似物。方法包括1）将候选化合物与试验细胞接触，其中试验细胞含有核酸分子，该核酸分子包含传染性丙型肝炎病毒基因组、核糖核酸酶和与第一和第二核苷酸序列可操作连接的可诱导启动子，核糖核酸酶被配置为从由可诱导启动子启动的转录本中移除复制传染性丙型肝炎病毒基因组所必需的 3′序列；2）检测细胞在候选化合物存在下产生的丙型肝炎病毒准种的增加。例如，可通过对从试验细胞中分离出的丙型肝炎病毒核酸分子进行测序来检测准种的增加。
• Induction of viral mutation by incorporation of miscoding ribonucleoside analogs into viral RNA
  申请人：——

  公开号：US20030119764A1

  公开（公告）日：2003-06-26

  The present invention is directed to the identification and use of ribonucleoside analogs to induce the mutation of an RNA virus, including BVDV, HIV and HCV, or a virus which otherwise replicates through an RNA intermediate. The increase in the mutation rate of the virus results in reduced viability of progeny generations of the virus, thereby inhibiting viral replication. In addition to these methods and related compositions, the invention provides methods and combinatorial chemistry libraries for screening ribonucleoside analogs for mutagenic potential.

  本发明涉及核糖核苷类似物的鉴定和使用，以诱导 RNA 病毒（包括 BVDV、HIV 和 HCV）或以其他方式通过 RNA 中间体复制的病毒发生变异。病毒变异率的增加会导致病毒后代的存活率降低，从而抑制病毒复制。除了这些方法和相关组合物之外，本发明还提供了筛选核糖核苷类似物诱变潜力的方法和组合化学文库。
• Mutagenesis methods using ribavirin and/or RNA replicases
  申请人：Coia Gregory

  公开号：US20050266453A1

  公开（公告）日：2005-12-01

  The use of RNA-replicases for introducing mutations into and selecting for improved RNA molecules is described. The use of ribavirin, or a derivative/analogue thereof, in methods for introducing one or more mutations during replication or transcription of a target nucleic acid molecule is also described. These methods can be used to screen for nucleic acids, or proteins encoded thereby, with altered or new activity. Also provided are kits comprising ribavirin, or a derivative/analogue thereof, for use in mutagenesis procedures.

  介绍了利用 RNA 复制酶将突变引入 RNA 分子并选择改良 RNA 分子的方法。还介绍了在目标核酸分子的复制或转录过程中使用利巴韦林或其衍生物/类似物引入一种或多种突变的方法。这些方法可用于筛选具有改变的或新的活性的核酸或其编码的蛋白质。还提供了包含利巴韦林或其衍生物/类似物的试剂盒，用于诱变程序。