N-(2,5-dioxopyrrolidin-1-yl)-4-formylbenzamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(2,5-dioxopyrrolidin-1-yl)-4-formylbenzamide
• 化学式: C₁₂H₁₀N₂O₄
• 分子量: 246.22
• InChiKey: RMTLMTYIGIOBQR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  83.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] ANTIBODY DRUG CONJUGATES FOR THE TREATMENT OF IMMUNE CONDITIONS<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT POUR LE TRAITEMENT D'ÉTATS IMMUNITAIRES
  申请人：CALIFORNIA INST BIOMEDICAL RES

  公开号：WO2016115218A1

  公开（公告）日：2016-07-21

  Disclosed herein are antibody kinase inhibitor conjugates. The antibody kinase inhibitor conjugates may be used to treat conditions such as autoimmune diseases and cancers.

  本文披露了抗体激酶抑制剂偶联物。这些抗体激酶抑制剂偶联物可用于治疗自身免疫疾病和癌症等疾病。
• ENCAPSULATED PARTICLES
  申请人：nanoComposix, Inc.

  公开号：US20160250612A1

  公开（公告）日：2016-09-01

  The disclosed technology relates generally to material systems which include a plurality of particles and methods of making the same. The particles have a core and a shell which encapsulates the core and has at least one atomic element not included in the core. The cores of the particles have a median maximum dimension that is less than 10 microns and a median of at least one axial dimension that is between 10 nm and 500 nm. The shells of the particles have a median thickness that is less than 100 nm, a silicon concentration that is between 10% and 50% on the basis of the weight of the shells, and an aluminum concentration that is between 0.01% and 5% on the basis of the weight of the shells.

  披露的技术通常涉及包括多个粒子的材料系统及其制备方法。这些粒子具有一个核心和一个包覆核心的壳层，壳层中至少包含一个不包括在核心中的原子元素。这些粒子的核心具有一个中位数最大尺寸小于10微米，一个中位数至少一个轴向尺寸在10纳米到500纳米之间。这些粒子的壳层具有一个中位数厚度小于100纳米，硅浓度在壳层重量基础上介于10％和50％之间，铝浓度在壳层重量基础上介于0.01％和5％之间。
• DEVELOPMENT OF NOVEL MACROMOLECULE TRANSDUCTION DOMAIN WITH IMPROVED CELL PERMEABILITY AND METHOD FOR USING SAME
  申请人：Procell Therapeutics Inc.

  公开号：EP2784081A1

  公开（公告）日：2014-10-01

  The present invention relates to an improved macromolecule transduction domain (MTD), which facilitates permeating the cell membrane of a biologically active molecule, having enhanced cell permeability. Specifically, an improved MTD according to the present invention, compared to an existing MTD, can transmit various types of biologically active molecule from inside the body and inside a test tube more effectively, and thus can be effectively used in a method to genetically alter a biologically active molecule so as to have cell permeability or in a method to transport a biologically active molecule into a cell, or the like. Additionally, the improved MTD can be very useful in development of new drugs and incrementally modified drugs as uses of the improved MTD are possible in drug delivery systems, recombinant protein vaccines or DNA/RNA therapeutic agents, gene or protein therapies, and pharmacologically or medically useful protein production or medical, pharmacological and pharmaceutical compositions.

  本发明涉及一种改进的大分子转导结构域（MTD），它有利于生物活性分子渗透细胞膜，具有更强的细胞渗透性。具体地说，与现有的 MTD 相比，根据本发明改进的 MTD 可以更有效地从体内和试管内转运各种生物活性分子，因此可以有效地用于遗传改变生物活性分子以使其具有细胞渗透性的方法，或用于将生物活性分子转运到细胞内的方法等。此外，改进型MTD在新药和增量改良药物的开发中也非常有用，因为改进型MTD可用于给药系统、重组蛋白疫苗或DNA/RNA治疗剂、基因或蛋白疗法、药理学或医学上有用的蛋白生产或医疗、药理学和药物组合物中。
• SOLID-PHASE IMMOBILIZATION OF MICROBIAL TRANSGLUTAMINASE MTG ON MICROBEADS FOR PROTEIN CONJUGATION
  申请人：PAUL SCHERRER INSTITUT

  公开号：EP3272864A1

  公开（公告）日：2018-01-24

  Site-specific modification of proteins with microbial transglutaminase (MTG) is a powerful and versatile strategy for a controlled modification of proteins under physiological conditions. We present evidence that solid-phase microbead-immobilization can be used to site-specifically and efficiently attach different functional molecules important for further downstream applications to proteins of therapeutic relevance including scFV, Fab-fragment and antibodies. We demonstrate that MTG remained firmly immobilized with no detectable column bleeding and that enzyme activity was sustained during continuous operation, which allowed for a convenient recycling of the enzyme, thus going beyond solution-phase MTG conjugation. In addition it is showed that immobilized MTG shows enhanced selectivity towards a certain residue in the presence of several reactive residues which are all targeted if the conjugation was carried out in solution.

  用微生物转谷氨酰胺酶（MTG）对蛋白质进行位点特异性修饰是在生理条件下对蛋白质进行可控修饰的一种强大而多用途的策略。我们提出的证据表明，固相微珠固定化技术可用于定点、高效地将对进一步下游应用非常重要的不同功能分子附着到具有治疗意义的蛋白质上，包括 scFV、Fab 片段和抗体。我们的研究表明，MTG 被牢牢固定，没有检测到色谱柱渗漏，而且在连续操作过程中酶的活性得以保持，从而方便了酶的再循环，超越了溶液相 MTG 连接。此外，研究还表明，如果在溶液中进行缀合，固定化的 MTG 会在存在多个反应残基的情况下对某个残基显示出更强的选择性，而这些反应残基都是缀合的目标。
• METHOD FOR THE DETECTION AND/OR QUANTIFICATION OF LUPIN BETA-CONGLUTIN ALLERGEN PROTEINS
  申请人：Consejo Superior de Investigaciones Científicas (CSIC)

  公开号：EP3514166A1

  公开（公告）日：2019-07-24

  The present invention provides an improved antibody, method and kit for the specific detection and/or quantification of the main allergen proteins of lupin seeds, namely beta-conglutins, preferably in foodstuffs. The method of the invention is preferably based on an ELISA assay and the antibody used has been designed against an epitope that is shared by at least seven isoforms of the beta-conglutin proteins of the Lupinus angustifolius species and at least one isoform of the Lupinis albus species. Thus, the method of the invention is highly specific and sensitive, so that it may detect and quantify even lupin traces present in food samples which might elicit allergic reactions in sensitized consumers.

  本发明提供了一种改进的抗体、方法和试剂盒，用于特异性检测和/或定量羽扇豆种子的主要过敏原蛋白，即β-凝集素，最好是食品中的β-凝集素。本发明的方法最好以 ELISA 检测法为基础，所使用的抗体是针对至少七种 Lupinus angustifolius 种的β-凝集素蛋白同工型和至少一种 Lupinis albus 种的β-凝集素蛋白同工型所共有的表位设计的。因此，本发明的方法具有高度的特异性和灵敏性，甚至可以检测和量化食品样品中可能引起过敏消费者过敏反应的羽扇豆痕量。