L-Prolyl-L-leucin-anhydrid | 18625-25-7

• 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
• 英文名称: L-Prolyl-L-leucin-anhydrid
• 英文别名: Leucine-proline anhydride；[(2S)-2-amino-4-methylpentanoyl] (2S)-pyrrolidine-2-carboxylate
• CAS: 18625-25-7
• 化学式: C₁₁H₂₀N₂O₃
• 分子量: 228.291
• InChiKey: QEDMGXHHRXIZDW-IUCAKERBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  16
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  81.4
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• STRUCTURAL MIMETICS OF PROLINE-RICH PEPTIDES AND THEIR USE
  申请人：FORSCHUNGSVERBUND BERLIN E.V.

  公开号：US20140100217A1

  公开（公告）日：2014-04-10

  The present invention provides a compound comprising a general formula 1: In general formula 1, X is at least one of O and S. A is a ring bridge. Y 1 is at least one of H, alkyl, fluoroalkyl, aryl and heteroaryl. Z 1 , Z 2 , Z 3 are, individually or alternatively, at least one of H, carbonyl, OH, O-alkyl, O-acyl, N—R 1 R 2 (where R 1 or R 2 are, individually or alternatively, at least one of H, alkyl, acyl, and sulfonyl), alkyl, acyl, fluoroalkyl, aryl, and heteroaryl. R 1 is at least one of alkyl, acyl, alkoxycarbonyl, aryloxycarbonyl, and aminocarbonyl. R 2 is at least one of H, alkyl, aryl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aminocarbonyl, aryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminoacyl and peptidyl. The present invention furthermore relates to the use of the compound as a pharmaceutical active compound, and to the use of the pharmaceutical active compound to treat bacterial diseases, neurodegenerative diseases and tumors.

  本发明提供了一个包含一般式1的化合物： 在一般式1中，X至少是O和S中的一个。A是一个环桥。Y1至少是H、烷基、氟烷基、芳基和杂环芳基中的一个。Z1、Z2、Z3分别或交替地至少是H、羰基、OH、O-烷基、O-酰基、N—R1R2（其中R1或R2分别或交替地至少是H、烷基、酰基和磺酰基中的一个）、烷基、酰基、氟烷基、芳基和杂环芳基中的一个。R1至少是烷基、酰基、烷氧羰基、芳氧羰基和氨基羰基中的一个。R2至少是H、烷基、芳基、烷基羰基、芳基羰基、烷氧羰基、氨基羰基、芳氧羰基、烷基磺酰基、芳基磺酰基、氨基酰基和肽基中的一个。本发明还涉及将该化合物用作药物活性化合物的用途，以及将药物活性化合物用于治疗细菌性疾病、神经退行性疾病和肿瘤的用途。
• DNA VACCINE BASED ON B7-1-PE40KDEL EXOTOXIN FUSION GENE AND USE THEREOF
  申请人：Affiliated Hospital of Academy of Military Medical Sciences, PLA

  公开号：EP2628802A1

  公开（公告）日：2013-08-21

  The present invention relates to the fields of immunology and molecular biology and related to a B7-1-PE40KDEL exotoxin fusion gene-based DNA vaccine and the use thereof. Specifically, the DNA vaccine contains a recombinant expression vector, and the vector contains exotoxin fusion gene B7-1-PE40KDEL, which is effectively ligated into selected eukaryotic expression vectors, such as pcDNA3.1/Zeo(+), pWLNEO, pSV2CAT, pOG44, pXT1, pSG, pSVK3, pBPV, pMSG, pSVL, and adenovirus. The invention also relates to the exotoxin fusion gene B7-1-PE40KDEL, the encoded exotoxin fusion protein, a recombinant expression vector that contains the exotoxin fusion gene, and compositions that contain the recombinant expression vector. The DNA vaccine in this invention has a good effect on the treatment or prevention of allogeneic tissue/organ transplant rejection and hematopoietic stem cell transplantation rejection such as GVHD.

  本发明涉及免疫学和分子生物学领域，与一种基于B7-1-PE40KDEL外毒素融合基因的DNA疫苗及其使用有关。具体地说，该DNA疫苗含有重组表达载体，载体中含有外毒素融合基因B7-1-PE40KDEL，该基因被有效地连接到选定的真核表达载体中，如pcDNA3.1/ZEO(+)、pWLNEO、pSV2CAT、pOG44、pXT1、pSG、pSVK3、pBPV、pMSG、pSVL和腺病毒。本发明还涉及外毒素融合基因 B7-1-PE40KDEL、编码的外毒素融合蛋白、含有外毒素融合基因的重组表达载体以及含有重组表达载体的组合物。本发明中的DNA疫苗对治疗或预防异体组织/器官移植排斥反应和造血干细胞移植排斥反应（如GVHD）具有良好的效果。
• MUTANT RECEPTORS AND THEIR USE IN A NUCLEAR RECEPTOR-BASED INDUCIBLE GENE EXPRESSION SYSTEM
  申请人：Intrexon Corporation

  公开号：EP3219204A1

  公开（公告）日：2017-09-20

  This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field gene expression. More specifically, this invention relates to novel substitution mutant receptors and their use in a nuclear receptor-based inducible gene expression system and methods of modulating the expression of a gene in a host cell for applications such as gene therapy, large scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.

  本发明涉及生物技术或基因工程领域。具体来说，本发明涉及基因表达领域。更具体地说，本发明涉及新型置换突变受体及其在基于核受体的诱导基因表达系统中的应用，以及调节宿主细胞中基因表达的方法，应用领域包括基因治疗、蛋白质和抗体的大规模生产、基于细胞的高通量筛选测定、功能基因组学和转基因生物的性状调控。
• Markers for detection of gastric cancer
  申请人：Pacific Edge Limited

  公开号：US10024859B2

  公开（公告）日：2018-07-17

  Early detection of tumors is a major determinant of survival of patients suffering from tumors, including gastric tumors. Members of the GTM gene family can be differentially expressed in gastric tumor tissue, and thus can be used as markers for the detection of gastric and other types of cancer. The present invention provides for novel GTMs for the detection of tumors, including gastric tumors, and in particular human zymogen granule protein 16 (ZG16). The GTMs can be used in isolation or together with other known GTMs to provide for novel signatures to be used in the detection of tumors, including gastric tumors.

  早期发现肿瘤是决定包括胃肿瘤在内的肿瘤患者生存期的重要因素。GTM 基因家族成员可在胃肿瘤组织中差异表达，因此可用作检测胃癌和其他类型癌症的标记物。本发明提供了用于检测包括胃肿瘤在内的肿瘤的新型 GTMs，特别是人zymogen granule protein 16 (ZG16)。这些 GTMs 可单独使用，也可与其他已知的 GTMs 一起使用，以提供用于检测包括胃肿瘤在内的肿瘤的新型特征。
• Method for producing target substance
  申请人：AJINOMOTO CO., INC.

  公开号：US10155952B2

  公开（公告）日：2018-12-18

  A method for producing a target substance is provided. A target substance is produced by culturing a coryneform bacterium, which is able to produce a target substance, and which also has an improved ability to assimilate xylose as a result of the introduction of a mutation into a coding region and/or an expression control region of the NCgl2954 gene on the chromosome of the bacterium. The culture is conducted in a medium containing xylose, and the target substance can be collected from the medium.

  本发明提供了一种生产目标物质的方法。目标物质的生产是通过培养一种能够生产目标物质的棒状杆菌来实现的，由于在该细菌染色体上的 NCgl2954 基因的编码区和/或表达控制区引入了突变，该细菌同化木糖的能力也得到了提高。在含有木糖的培养基中进行培养，可从培养基中收集目标物质。