2-Amino-3-benzyl-succinic acid | 99477-50-6

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 英文名称: 2-Amino-3-benzyl-succinic acid
• 英文别名: 3-azaniumyl-2-benzyl-4-hydroxy-4-oxobutanoate
• CAS: 99477-50-6
• 化学式: C₁₁H₁₃NO₄
• 分子量: 223.229
• InChiKey: KMVYGTIPJNGNRD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2
• 重原子数：
  16
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  101
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-Amino-3-benzyl-succinic acid 在 磷酸吡哆醛 、 Pseudomonas dacunhae L-aspartateb β-decarboxylase R37A/T382G 作用下， 以 aq. buffer 为溶剂， 生成 L-高苯丙氨酸 、 (2R)-2-amino-3-benzylbutanedioic acid
  参考文献：
  名称：

  假单胞菌L-天冬氨酸β-脱羧酶的L-高苯丙氨酸合成的结构指导工程

  摘要：

  假单胞菌L-天冬氨酸β-脱羧酶（AspBDC）的结构指导工程导致了一个双突变体（R37A / T382G），其比活性朝目标底物3（R）-的比活性显着提高了15,400倍，达到216 mU / mg。 L-天冬氨酸苄酯。通过使用该变体作为生物催化剂，开发了一种酶促合成L-高苯丙氨酸的新策略，可在12小时内提供75％的产物收率。我们的结果强调了工程化的AspBDC在生物催化合成药物Relavent和增值非天然L-氨基酸方面的潜力

  DOI：

  10.1039/d0cc05871h

文献信息

• 3-alkylaryl aspartate compounds and their use for selective enhancement of synaptic transmission
  申请人：Esslinger S. Christopher

  公开号：US20070142467A1

  公开（公告）日：2007-06-21

  The present invention provides an L-aspartate derivative compound represented by the following structure wherein Ar represents an aromatic group; L represents a linking moiety; R represents hydrogen, alkyl, aryl, or heteroaryl; and indicates that the stereochemistry at the 3-position can be R or S. The compounds of the invention are useful for selectively inhibiting EAAT3 and for enhancing synaptic transmission. Additionally, the inventive compounds can be used to treat a patient suffering from Alzheimers disease or a neuropathy or a neurodegenerative disease in which L-glutamate transporter activity is involved in the onset of the disease.

  本发明提供了一种由以下结构表示的L-天冬氨酸衍生物化合物 其中Ar代表芳香基团；L代表连接基团；R代表氢、烷基、芳基或杂环芳基；和 表示3位的立体化学可以是R或S。本发明的化合物对选择性抑制EAAT3和增强突触传递具有用处。此外，这些创新性化合物可用于治疗患有阿尔茨海默病或神经病或神经退行性疾病的患者，其中L-谷氨酸转运蛋白活性参与了疾病的发病。
• Amphiphilic Block Copolymer And Preparation Method Thereof And Micellar Drug-Loading System Formed By Same With Antitumor Drug
  申请人：LIU Ke

  公开号：US20150283246A1

  公开（公告）日：2015-10-08

  The present invention relates to a novel amphiphilic block copolymer and the preparation method thereof, as well as a micellar drug-loaded system formed by said copolymer and an anti-tumor drug. Said amphiphilic block copolymer comprises a hydrophilic segment and a hydrophobic segment, and the end group of said hydrophobic segment is end-capped with a hydrophobic group. Methoxypolyethylene glycol (or polyethylene glycol)-polyester block copolymer which has recognized safety is used as a fundamental material of the amphiphilic block copolymer of the present invention, and the terminal hydroxyl group of the polyester segment is modified with a hydrophobic group, whereby the compatibility between the drug molecule and the hydrophobic segments of the block copolymer is improved, and the interaction therebetween is enhanced. Moreover, a larger space for accommodating the drug molecules is provided. Said micelles are more effective in restricting the drug molecules inside the micellar core and preventing the drug from dissolved out of the micelles. Therefore, a drug-loaded micelle with high stability is obtained.

  本发明涉及一种新型的两亲性嵌段共聚物及其制备方法，以及由该共聚物和抗肿瘤药物形成的微胶束药物载药系统。该两亲性嵌段共聚物包括亲水性段和疏水性段，疏水性段的末端基团被疏水基团封端。本发明的两亲性嵌段共聚物的基础材料采用了已经被认可为安全的甲氧基聚乙二醇（或聚乙二醇）-聚酯嵌段共聚物，并且聚酯段的末端羟基被疏水基团修饰，从而提高了药物分子与嵌段共聚物的疏水性段之间的相容性和相互作用，同时提供了更大的容纳药物分子的空间。这些微胶束更有效地限制了药物分子在微胶束核心内的扩散和溶解，因此获得了高稳定性的药物载药微胶束。
• AMPHIPHILIC BLOCK COPOLYMER AND PREPARATION METHOD THEREOF AND MICELLAR DRUG-LOADING SYSTEM FORMED BY SAME WITH ANTITUMOR DRUG
  申请人：Suzhou Nanomedicine R&D Co., Ltd.

  公开号：EP2913353A1

  公开（公告）日：2015-09-02

  The present invention relates to a novel amphiphilic block copolymer and the preparation method thereof, as well as a micellar drug-loaded system formed by said copolymer and an anti-tumor drug. Said amphiphilic block copolymer comprises a hydrophilic segment and a hydrophobic segment, and the end group of said hydrophobic segment is end-capped with a hydrophobic group. Methoxypolyethylene glycol (or polyethylene glycol)-polyester block copolymer which has recognized safety is used as a fundamental material of the amphiphilic block copolymer of the present invention, and the terminal hydroxyl group of the polyester segment is modified with a hydrophobic group, whereby the compatibility between the drug molecule and the hydrophobic segments of the block copolymer is improved, and the interaction therebetween is enhanced. Moreover, a larger space for accommodating the drug molecules is provided. Said micelles are more effective in restricting the drug molecules inside the micellar core and preventing the drug from dissolved out of the micelles. Therefore, a drug-loaded micelle with high stability is obtained.

  本发明涉及一种新型两亲嵌段共聚物及其制备方法，以及由所述共聚物和抗肿瘤药物形成的胶束载药体系。所述两亲嵌段共聚物包括亲水段和疏水段，所述疏水段的端基被疏水基团封端。本发明采用安全性得到认可的甲氧基聚乙二醇（或聚乙二醇）-聚酯嵌段共聚物作为两亲性嵌段共聚物的基本材料，聚酯段的末端羟基被疏水基团修饰，从而改善了药物分子与嵌段共聚物的疏水段之间的相容性，增强了它们之间的相互作用。此外，还提供了更大的容纳药物分子的空间。所述胶束能更有效地将药物分子限制在胶束核心内，并防止药物从胶束中溶解出来。因此，药物胶束具有很高的稳定性。
• CYCLIC PRODRUGS OF PEPTIDES AND PEPTIDE NUCLEIC ACIDS HAVING IMPROVED METABOLIC STABILITY AND CELL MEMBRANE PERMEABILITY
  申请人：THE UNIVERSITY OF KANSAS

  公开号：EP0830372B1

  公开（公告）日：2001-10-10
• COMPOSITIONS AND METHODS FOR THE DIAGNOSIS AND TREATMENT OF DISEASES OF THE LIVER
  申请人：Viscient Biosciences, Inc.

  公开号：US20200241005A1

  公开（公告）日：2020-07-30

  Provided herein are novel molecular markers and targets of liver disease, including NAFLD, NASH, liver fibrosis and related conditions. Also provided herein are methods of screening for modulators of such molecular markers and targets for the treatment of diseases of the liver as well as the modulators useful for treating such disease. Also provided are novel molecular markers useful for diagnosing diseases of the liver, including, NAFLD, NASH, liver fibrosis and related conditions, and for monitoring the progression and treatment of such disease of the liver.