N6-(2-碘乙酰基)-L-赖氨酸 | 90764-56-0

• 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: N6-(2-碘乙酰基)-L-赖氨酸
• 英文名称: (+)-S-2-amino-6-iodoacetamidohexanoic acid
• 英文别名: N(sup 6)-(Iodoacetyl)-L-lysine；(2S)-2-amino-6-[(2-iodoacetyl)amino]hexanoic acid
• CAS: 90764-56-0
• 化学式: C₈H₁₅IN₂O₃
• 分子量: 314.123
• InChiKey: PEVDSQTZJOGTKZ-LURJTMIESA-N

物化性质

• 熔点：
  183-185 °C
• 沸点：
  500.0±45.0 °C(Predicted)
• 密度：
  1.706±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.1
• 重原子数：
  14
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  92.4
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-硝基苯酯碘乙酸 、 L-赖氨酸盐酸盐 在 sodium hydroxide 作用下， 以 四氢呋喃 为溶剂， 反应 5.0h， 以78%的产率得到N6-(2-碘乙酰基)-L-赖氨酸
  参考文献：
  名称：

  Regioselective Synthesis of (+) -S-2-Amino-5-iodoacetamidopentanoic and (+) -S-2-amino-6-iodoacetamidohexanoic Acids

  摘要：

  Mild reaction conditions were developed for the preparation of the active-site-directed irreversible enzime inhibitors (+)-S-2-amino-5-iodoacetamidopentanoic acid and (+)-S-2-amino-6-iodoacetamidohexanoic acid.

  DOI：

  10.1080/00397919108020837

文献信息

• HIV protease inhibitors based on amino acid derivatives
  申请人：——

  公开号：US20020151546A1

  公开（公告）日：2002-10-17

  A compound selected from the group consisting of a compound of formula I 1 a compound of formula II 2 and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R 1 , R 2 , Cx, n, R 3 , R 4 , R 5 , Y are as defined in the specification.

  从以下组中选择的化合物，其中化合物I的化合物，化合物II的化合物，以及当化合物I和II的化合物包括其氨基团的药用可接受铵盐，其中R1、R2、Cx、n、R3、R4、R5、Y的定义如规范中所述。
• [EN] A GENETICALLY ENCODED, PHAGE-DISPLAYED CYCLIC PEPTIDE LIBRARY AND METHODS OF MAKING THE SAME<br/>[FR] BANQUE DE PEPTIDES CYCLIQUES CODÉS GÉNÉTIQUEMENT ET EXPRIMÉS EN SURFACE DE PHAGES, ET MÉTHODES DE PRODUCTION DE CELLE-CI
  申请人：TEXAS A & M UNIV SYS

  公开号：WO2020236146A1

  公开（公告）日：2020-11-26

  Embodiments of the present disclosure pertain to methods of selecting cyclic peptides that bind to a target by transforming a phage display library with a plurality of nucleic acids into bacterial host cells, where the nucleic acids include phage coat protein genes with a combinatorial region that encodes at least one cysteine and at least one non-canonical amino acid. The transformation results in the production of phage particles with phage coat proteins where the cysteine and the non-canonical amino acid couple to one another to form a cyclic peptide library. Phage particles are then screened against the desired target to select bound cyclic peptides. Amino acid sequences of the selected cyclic peptides are then identified. Additional embodiments pertain to methods of constructing a phage display library that encodes the cyclic peptides. Further embodiments of the present disclosure pertain to the produced cyclic peptides, phage display libraries and phage particles.

  本公开的实施例涉及一种选择循环肽结合靶标的方法，该方法通过将具有编码至少一个半胱氨酸和至少一个非规范氨基酸的组合区域的噬菌体外壳蛋白基因的核酸库转化为细菌宿主细胞来实现。转化导致产生带有噬菌体外壳蛋白的噬菌体颗粒，其中半胱氨酸和非规范氨基酸耦合形成循环肽库。然后，对所需的靶标筛选噬菌体颗粒以选择结合的循环肽。然后确定所选择的循环肽的氨基酸序列。本公开的其他实施例涉及构建编码循环肽的噬菌体外显库的方法。本公开的其他实施例涉及所产生的循环肽、噬菌体外显库和噬菌体颗粒。
• Hiv protease inhibitors based on amino acid derivatives
  申请人：Ambrilia Biopharma Inc.

  公开号：EP1803706A1

  公开（公告）日：2007-07-04

  The present application refers to a compound selected from the group consisting of a compound of formula I wherein the compounds No. 1 to 10, respectively, are defined as follows The compounds are useful in the treatment of HIV and HTLV infections.

  本申请涉及的化合物选自由式 I 所组成的组 其中 1 号至 10 号化合物分别定义如下 这些化合物可用于治疗 HIV 和 HTLV 感染。
• Use of L-arginine optionally combined with magnesium for the treatment of sickle cell disease and/or pulmonary hypertension
  申请人：Children's Hospital & Research Center at Oakland

  公开号：EP2397128A1

  公开（公告）日：2011-12-21

  The invention features methods and compositions for treatment of conditions associated with decreased nitric oxide bioavailability, such as a condition associated with elevated arginase activity, using an arginine-based therapy, including combination therapy with an arginase inhibitor and/or magnesium

  本发明的特点是使用基于精氨酸的疗法，包括与精氨酸酶抑制剂和/或镁的联合疗法，来治疗与一氧化氮生物利用率降低有关的病症，如与精氨酸酶活性升高有关的病症的方法和组合物。
• ARGINASE AS BIOMARKER AND DRUG TARGET FOR PCOS
  申请人：Johann Wolfgang Goethe-Universität Frankfurt am Main

  公开号：EP3696281A1

  公开（公告）日：2020-08-19

  The invention is based on the surprising finding that in women with polycystic ovary syndrome (PCOS) an increased activity and/or expression of arginase is detected. The invention uses therefore various arginase associated biomarkers as indicators for the occurrence with the disease. More importantly the invention describes genetic variations associated with increased arginase expression/activity, and further being associated with PCOS. Hence, the invention provides enzymatic, immunological, and genetic diagnostic approaches for the detection and monitoring of PCOS in a subject. Furthermore the invention shows that the causal link of PCOS and arginase activity and hence provides the use of arginase inhibitors as a treatment approach.

  本发明基于一个惊人的发现，即在患有多囊卵巢综合症（PCOS）的妇女体内，发现精氨酸酶的活性和/或表达量增加。因此，本发明使用各种与精氨酸酶相关的生物标志物作为疾病发生的指标。更重要的是，本发明描述了与精氨酸酶表达/活性增加相关的遗传变异，并进一步与多囊卵巢综合症相关。因此，本发明提供了用于检测和监测受试者多囊卵巢综合症的酶学、免疫学和遗传学诊断方法。此外，本发明还表明了多囊卵巢综合症与精氨酸酶活性之间的因果关系，因此提供了使用精氨酸酶抑制剂的治疗方法。