马尿酰精氨酸 | 744-46-7

• 物质功能分类: 生物化工 - 氨基酸及其衍生物 - 精氨酸类衍生物
• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 马尿酰精氨酸
• 英文名称: N-benzoylglycyl-L-arginine
• 英文别名: hippuryl-L-arginine；Bz-Gly-Arg；N^α-(N-benzoyl-glycyl)-L-arginine；N^α-(N-Benzoyl-glycyl)-L-arginin；N2-(N-benzoylglycyl)-L-arginine；N3α-hippuryl-L-arginine；(2S)-2-[(2-benzamidoacetyl)amino]-5-(diaminomethylideneazaniumyl)pentanoate
• CAS: 744-46-7
• 化学式: C₁₅H₂₁N₅O₄
• 分子量: 335.363
• InChiKey: GFLCPYUSPYXNBV-NSHDSACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  24
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  160
• 氢给体数：
  5
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  马尿酰精氨酸 在 N-甲基吗啉 、 盐酸 、 氯甲酸乙酯 作用下， 以 四氢呋喃 、 乙醚 为溶剂， 反应 0.22h， 生成 N-苯甲酰基甘氨酸甲酯
  参考文献：
  名称：

  快速反应释放肽的羧基末端残基

  摘要：

  肽恶唑酮在含有稀酸（例如0.02M HCl）的醇中的醇解作用可在室温下10分钟内以30-70％的收率得到C端氨基酸和缩短的肽的酯。这与发现肽恶唑酮可与烷基氯甲酸酯在3分钟内形成的发现一起，可快速去除肽C端残基。

  DOI：

  10.1016/0040-4039(96)01716-9
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 钯 、 溶剂黄146 作用下， 生成 马尿酰精氨酸
  参考文献：
  名称：

  Folk; Gladner, Journal of Biological Chemistry, 1958, vol. 231, p. 379,388

  摘要：

  DOI：

文献信息

• Peptidyl Arginine Deiminase Type IV Inhibitor
  申请人：Sato Mamoru

  公开号：US20070276040A1

  公开（公告）日：2007-11-29

  A compound represented by the general formula (I) or a salt thereof is provided: wherein R 1 , R 2 and R 3 each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, provided that at least one of R 1 , R 2 and R 3 does not represent a hydrogen atom; R 4 represents an amino group which has a substituent; and R 5 represents a carboxyl group which may have a substituent. Also provided is a peptidylarginine deiminase 4 inhibitor. The inhibitor can be used for the prevention and/or treatment of diseases associated with peptidylarginine deiminases (e.g., rheumatoid arthritis and multiple sclerosis).

  提供了由通式（I）表示的化合物或其盐： 其中，R1、R2和R3分别独立地表示氢原子或具有1至3个碳原子的烷基，但至少其中一个不表示氢原子；R4表示具有取代基的氨基；R5表示可能具有取代基的羧基。还提供了一种肽精氨酰基脱氨酶4抑制剂。该抑制剂可用于预防和/或治疗与肽精氨酰基脱氨酶相关的疾病（例如，类风湿性关节炎和多发性硬化症）。
• New carboxypeptidase A-gamma, process for preparing and pharmaceutical preparation containing same
  申请人：Eisai Co., Ltd.

  公开号：EP0060520A1

  公开（公告）日：1982-09-22

  A new species of carboxypeptidase Aγ, a process for preparation thereof and a pharmaceutical preparation containing same are disclosed. The new species of carboxypeptidase has an amino-terminal sequence with the primary structural formula of: Asn-Tyr-Ala-Thr-Tyr-His-Thr-Leu-Glu-Glu-Ile-Tyr-Asp-Phe-Met-Asp-IIe-Leu-Val-Ala-Glu-His-Pro-Gln-Leu-, and possesses physicochemical and enzymochemical properties which partly differ from known carboxypepti- dases. The new species of carboxypeptidase A. has been extracted from porcine pancreas. The process for preparing the new enzyme species comprises adding mammalian duodenum or an extract of mammalian duodenum to the porcine pancreas, thereby performing activation. Carboxypeptidase A according to the invention serves as a pharmaceutical in aiding protein digestion in the digestive tract.

  本发明公开了一种新品种的羧肽酶 Aγ、其制备方法以及含有该新品种的药物制剂。新品种羧肽酶的氨基末端序列的一级结构式为 Asn-Tyr-Ala-Thr-Tyr-His-Thr-Leu-Glu-Glu-Ile-Tyr-Asp-Phe-Met-Asp-IIe-Leu-Val-Ala-Glu-His-Pro-Gln-Leu-，具有与已知羧肽酶部分不同的物理化学和酶化学性质。 羧肽酶 A 的新品种是从猪胰腺中提取的。制备新品种酶的工艺包括向猪胰腺中加入哺乳动物十二指肠或哺乳动物十二指肠提取物，从而进行活化。 根据本发明，羧肽酶 A 可作为药物帮助消化道消化蛋白质。
• PEPTIDYL ARGININE DEIMINASE TYPE IV INHIBITOR
  申请人：Yokohama City University

  公开号：EP1717224A1

  公开（公告）日：2006-11-02

  A compound represented by the general formula (I) or a salt thereof is provided: wherein R1, R2 and R3 each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, provided that at least one of R1, R2 and R3 does not represent a hydrogen atom; R4 represents an amino group which has a substituent; and R5 represents a carboxyl group which may have a substituent. Also provided is a peptidylarginine deiminase 4 inhibitor. The inhibitor can be used for the prevention and/or treatment of diseases associated with peptidylarginine deiminases (e.g., rheumatoid arthritis and multiple sclerosis).

  提供了通式 (I) 所代表的化合物或其盐： 其中R1、R2和R3各自独立地代表氢原子或具有1至3个碳原子的烷基，条件是R1、R2和R3中至少有一个不代表氢原子；R4代表具有取代基的氨基；R5代表可能具有取代基的羧基。还提供了一种肽精氨酸脱氨酶 4 抑制剂。该抑制剂可用于预防和/或治疗与肽基精氨酸脱氨酶有关的疾病（如类风湿性关节炎和多发性硬化症）。
• Regulatable promoter
  申请人：LONZA LTD.

  公开号：US10301634B2

  公开（公告）日：2019-05-28

  A method of producing a protein of interest (POI) by culturing a recombinant eukaryotic cell line comprising an expression construct comprising a regulatable promoter and a nucleic acid molecule encoding a POI under the transcriptional control of said promoter, comprising the steps a) cultivating the cell line with a basal carbon source repressing the promoter, b) cultivating the cell line with a limited amount of a supplemental carbon source de-repressing the promoter to induce production of the POI at a transcription rate or at least 15% as compared to the native pGAP promoter, and c) producing and recovering the POI; and further an isolated regulatable promoter and a respective expression system.

  一种通过培养重组真核细胞系生产感兴趣的蛋白质（POI）的方法，该细胞系包含表达构建体，该表达构建体包含可调启动子和在所述启动子转录控制下编码POI的核酸分子，该方法包括以下步骤 a) 用抑制启动子的基础碳源培养细胞系、b) 用一定量的补充碳源培养细胞系，去抑制启动子，以诱导产生 POI，其转录率至少为原生 pGAP 启动子的 15%，以及 c) 产生并回收 POI；以及一种分离的可调节启动子和相应的表达系统。
• Constitiutive promoter
  申请人：Lonza Ltd.

  公开号：US10428123B2

  公开（公告）日：2019-10-01

  The invention relates to an isolated nucleic acid sequence comprising a promoter, which is a native sequence of Pichia pastoris comprising the nucleic acid sequence of pCS1 of SEQ ID 1, or a functionally active variant thereof which is a size variant, a mutant or hybrid of SEQ ID 1, or a combination thereof, expression constructs and recombinant host cells comprising the promoter, and a method of producing a protein of interest under the control of the promoter. It further relates to a method to identify a constitutive promoter from eukaryotic cells, and an isolated nucleic acid sequence comprising a promoter which when operatively linked to a nucleotide sequence encoding a protein of interest directs the expression thereof in a host cell at an expression level that is higher than under control of the native pGAP promoter at high and low growth rates.

  本发明涉及一种包含启动子的分离核酸序列，该启动子是由SEQ ID 1的pCS1核酸序列组成的Pichia pastoris的原生序列，或其功能活性变体，即SEQ ID 1的大小变体、突变体或杂交体，或其组合，还涉及包含该启动子的表达构建体和重组宿主细胞，以及在该启动子控制下生产感兴趣的蛋白质的方法。本发明还涉及一种从真核细胞中鉴定组成型启动子的方法，以及一种包含启动子的分离核酸序列，当该启动子与编码感兴趣的蛋白质的核苷酸序列操作性连接时，可指导其在宿主细胞中的表达，其表达水平在高生长率和低生长率下均高于在原生 pGAP 启动子控制下的表达水平。