Leu-Leu-Glu | 20274-83-3

• 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: Leu-Leu-Glu
• 英文别名: (2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]pentanedioic acid
• CAS: 20274-83-3
• 化学式: C₁₇H₃₁N₃O₆
• 分子量: 373.4
• InChiKey: QNBVTHNJGCOVFA-AVGNSLFASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.8
• 重原子数：
  26
• 可旋转键数：
  12
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.76
• 拓扑面积：
  159
• 氢给体数：
  5
• 氢受体数：
  7

文献信息

• Compounds for enzyme inhibition
  申请人：Bennett K. Mark

  公开号：US20060088471A1

  公开（公告）日：2006-04-27

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus, such as a detectable label. Along with therapeutic utilities, these peptide based compounds can be used in assays useful for screening, monitoring, diagnostic and/or dosing purposes.

  基于肽的化合物包括含杂原子的三元环，能够高效且选择性地抑制N-末端亲核试剂（Ntn）水解酶的特定活性。所述化合物可以不同程度地抑制具有多种活性的Ntn的活性。例如，20S蛋白酶体的类胰蛋白酶样和PGPH活性可以通过这些创新性化合物进行选择性抑制。基于肽的化合物包括至少三个肽单元、环氧或氮杂环和N-末端的功能化，例如可检测标记。除了治疗用途外，这些基于肽的化合物还可用于筛选、监测、诊断和/或剂量目的的检测中。
• Compounds for proteasome enzyme inhibition
  申请人：Proteolix, Inc.

  公开号：EP2100899A2

  公开（公告）日：2009-09-16

  The present invention relates to a method for determining the activity of a proteasome inhibitor, comprising (a) obtaining a biological sample that has been treated with a proteasome inhibitor; (b) separating inhibitor-bound proteasome subunits from unbound proteasome subunits; (c) determining the amount of inhibitor-bound proteasome subunits, unbound proteasome subunits, or both, wherein a change in the amount of inhibitor bound proteasome subunits is indicative of proteasome inhibitor activity.

  本发明涉及一种确定蛋白酶体抑制剂活性的方法，该方法包括：(a) 获得用蛋白酶体抑制剂处理过的生物样本；(b) 将抑制剂结合的蛋白酶体亚基与未结合的蛋白酶体亚基分离；(c) 确定抑制剂结合的蛋白酶体亚基、未结合的蛋白酶体亚基或两者的量，其中抑制剂结合的蛋白酶体亚基量的变化表明蛋白酶体抑制剂的活性。
• Enzyme inhibition
  申请人：Yale University

  公开号：US20040266664A1

  公开（公告）日：2004-12-30

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.

  包括含杂原子的三元环的肽基化合物能有效地、选择性地抑制 N 端亲核（Ntn）水解酶的特定活性。具有多种活性的 Ntn 的活性可受到所述化合物不同程度的抑制。例如，本发明化合物可选择性地抑制 20S 蛋白酶体的糜蛋白酶样活性和 PGPH 活性。肽基化合物包括一个邻近环官能团的退电子基团，肽包括至少三个肽单元。除其他治疗作用外，肽基化合物还具有抗炎和抑制细胞增殖的作用，涉及这些化合物的治疗应用。
• LABELED COMPOUNDS FOR PROTEASOME INHIBITION
  申请人：Proteolix, Inc.

  公开号：EP1805208A2

  公开（公告）日：2007-07-11
• COMPOUNDS FOR ENZYME INHIBITION
  申请人：Bennett Mark K.

  公开号：US20090215093A1

  公开（公告）日：2009-08-27

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus, such as a detectable label. Along with therapeutic utilities, these peptide based compounds can be used in assays useful for screening, monitoring, diagnostic and/or dosing purposes.