alpha-thio-UTP

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷
• 英文名称: alpha-thio-UTP
• 英文别名: UTPαS；UTPalphaS；[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphinothioyl] phosphono hydrogen phosphate
• 化学式: C₉H₁₅N₂O₁₄P₃S
• 分子量: 500.21
• InChiKey: BWPNYQWDXHLOGU-NOUWQNLYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.1
• 重原子数：
  29
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  274
• 氢给体数：
  7
• 氢受体数：
  15

反应信息

• 作为产物：
  描述：

  2,3-di-O-acetyluridine 在 吡啶 、 氨 、 tris(tetra-n-butylammonium) hydrogen pyrophosphate 、 sulfur 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 乙腈 为溶剂， 反应 20.0h， 生成 alpha-thio-UTP
  参考文献：
  名称：

  Synthesis of Nucleoside α-Thiotriphosphates via an Oxathiaphospholane Approach^†

  摘要：

  Nucleoside 5 '-O-(alpha-thiotriphosphates) were obtained in reactions of the appropriate nucleoside 5 '-O-(2-thio-1,3,2-oxathiaphospholanes) with pyrophosphate in the presence of DBU. The presented method allows also for preparation of alpha-seleno congeners and corresponding a-modified diphosphates.

  DOI：

  10.1021/ol050617r

文献信息

• [EN] NUCLEOSIDE 5'-PHOSPHOROTHIOATE ANALOGUES AND USES THEREOF<br/>[FR] ANALOGUES DE NUCLÉOSIDE 5'-PHOSPHOROTHIOATE ET LEURS UTILISATIONS
  申请人：UNIV BAR ILAN

  公开号：WO2013132489A1

  公开（公告）日：2013-09-12

  The invention provides particular mono- and dinucleoside 5'-phosphorothioate analogues, more particularly mono- or di- adenosine or uridine 5'-di- or tri- phosphorothioate analogues in which at least one of the bridging oxygen atoms of the phosphorothioate is replaced by a group such as -CH2-, and at least one of the non- bridging atoms or negatively-charged atoms of the phosphorothioate is either a sulfur atom or a sulfur ion; and pharmaceutical compositions thereof. These compounds are useful for treatment of neurodegenerative diseases or disorders such as Alzheimer's disease.

  该发明提供了特定的单核苷酸和二核苷酸5'-磷硫酸酯类似物，更具体地说是单腺苷或尿苷5'-二磷硫酸酯类似物或三磷硫酸酯类似物，其中磷硫酸酯的桥氧原子之一被类似于-CH2-的基团取代，并且磷硫酸酯的非桥接原子或负电荷原子之一是硫原子或硫离子；以及其药物组合物。这些化合物可用于治疗神经退行性疾病或障碍，如阿尔茨海默病。
• Sensitization of cancer cells to therapy using siNA targeting genes from the 1p and 19q chromosomal regions
  申请人：INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)

  公开号：EP1884569A1

  公开（公告）日：2008-02-06

  The invention relates to the identification of genes involved in resistance of cancer cells to therapy, to short nucleic acid molecules which inhibit the expression of these genes by RNA interference and to their use as adjuvant in cancer therapy, to sensitize cancer cells to conventional anticancer agents ; said short nucleic acid molecules are double-stranded short interfering nucleic acid molecules comprising a sense and an antisense region, wherein the sense region comprises a nucleotide sequence that is selected from the group consisting of: the sequences SEQ ID NO: 15, 11, 13, 14, 30, 31, 38, 46, 64 and 70 and the sequences having at least 70 % identity, preferably at least 80 % identity, more preferably at least 90 % identity with said sequences, and the antisense region comprises a nucleotide sequence that is complementary to the sense region.

  本发明涉及癌细胞抗药性基因的鉴定、通过RNA干扰抑制这些基因表达的短核酸分子及其在癌症治疗中作为辅助剂的用途，以使癌细胞对常规抗癌剂敏感；所述短核酸分子是由有义区和反义区组成的双链短干扰核酸分子，其中有义区包括选自以下组成的组的核苷酸序列：SEQ ID NO: 15、11、13、14、30、31、38、46、64和70：序列 SEQ ID NO：15、11、13、14、30、31、38、46、64 和 70 以及与上述序列具有至少 70% 的同一性，优选至少 80% 的同一性，更优选至少 90% 的同一性的序列，而反义区包括与有义区互补的核苷酸序列。
• Reversible siRNA-based silencing of mutated and endogenous wild-type huntingtin gene and its application for the treatment of Huntington's disease
  申请人：Commissariat à l'Energie Atomique

  公开号：EP2014769A1

  公开（公告）日：2009-01-14

  Isolated double-stranded short interfering nucleic acid molecules inhibiting the expression of endogenous wild-type and exogenous human mutated huntingtin genes in cells of a non-human mammal which are expressing both said huntingtin genes, and their application for the treatment of Huntington's disease as well as to study Huntington's disease in rodent models

  分离的双链短干扰核酸分子，可抑制表达上述两种亨廷丁基因的非人类哺乳动物细胞中内源性野生型亨廷丁基因和外源性人类突变亨廷丁基因的表达，及其在亨廷顿症治疗和啮齿动物模型亨廷顿症研究中的应用
• Sensizitation of cancer cells to therapy using sina targeting genes from the 1p and 19q chromosomal regions
  申请人：UNIVERSITE JOSEPH FOURIER (GRENOBLE 1)

  公开号：EP2336320A1

  公开（公告）日：2011-06-22

  The invention relates to the identification of genes involved in resistance of cancer cells to therapy, to short nucleic acid molecules which inhibit the expression of these genes by RNA interference and to their use as adjuvant in cancer therapy, to sensitize cancer cells to conventional anticancer agents ; said short nucleic acid molecules are double-stranded short interfering nucleic acid molecules comprising a sense and an antisense region, wherein the sense region comprises a nucleotide sequence that is selected from the group consisting of: the sequences SEQ ID NO: 15, 11, 13, 14, 30, 31, 38, 46, 64 and 70 and the sequences having at least 70 % identity, preferably at least 80 % identity, more preferably at least 90 % identity with said sequences, and the antisense region comprises a nucleotide sequence that is complementary to the sense region.

  本发明涉及癌细胞抗药性基因的鉴定、通过RNA干扰抑制这些基因表达的短核酸分子及其在癌症治疗中作为辅助剂的用途，以使癌细胞对常规抗癌剂敏感；所述短核酸分子是由有义区和反义区组成的双链短干扰核酸分子，其中有义区包括选自以下组成的组的核苷酸序列：SEQ ID NO: 15、11、13、14、30、31、38、46、64和70：序列 SEQ ID NO：15、11、13、14、30、31、38、46、64 和 70 以及与上述序列具有至少 70% 的同一性，优选至少 80% 的同一性，更优选至少 90% 的同一性的序列，而反义区包括与有义区互补的核苷酸序列。
• Metabolically stabilized double stranded mRNA
  申请人：University of Iowa Research Foundation

  公开号：US11007213B2

  公开（公告）日：2021-05-18

  Double stranded mRNA (ds mRNA), e.g., produced in vitro, where one strand encodes a protein of interest and the other strand is hydrogen bonded to at least a portion of the coding region for the protein, as well as methods of making and using the ds mRNA, are provided.

  提供了双链 mRNA（ds mRNA），例如在体外产生的双链 mRNA（ds mRNA），其中一条链编码感兴趣的蛋白质，另一条链与蛋白质编码区的至少一部分氢键结合，还提供了制造和使用 ds mRNA 的方法。