Leu-Val-Tyr

• 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-Val-Tyr
• 英文别名: (2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoic acid
• 化学式: C₂₀H₃₁N₃O₅
• 分子量: 393.5
• InChiKey: MSFITIBEMPWCBD-ULQDDVLXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  28
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  142
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• Compounds for enzyme inhibition
  申请人：Zhou Han-Jie

  公开号：US20070105786A1

  公开（公告）日：2007-05-10

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles

  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与蛋白酶体相关的N-末端亲核（Ntn）水解酶的特定活性。这些基于肽的化合物包括环氧化物或氮杂环丙烷，并在N-末端进行官能化。除了其他治疗用途外，预计这些基于肽的化合物将显示抗炎性能和抑制细胞增殖。由于它们的生物利用度特性，这些基于肽的蛋白酶体抑制剂可以通过口服给药进行。
• [EN] COMPOUNDS FOR PROTEASOME ENZYME INHIBITION<br/>[FR] COMPOSES POUR L'INHIBITION ENZYMATIQUE DU PROTEASOME
  申请人：PROTEOLIX INC

  公开号：WO2006017842A1

  公开（公告）日：2006-02-16

  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 activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

  肽基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。这些具有多种活性的Ntn的活性可以被所描述的化合物差异性地抑制。例如，创蛋白酶样活性的20S蛋白酶可以通过这种创新的化合物被选择性地抑制。这些肽基化合物包括环氧化物或氮杂环，以及N-末端的官能化。除了其他治疗用途外，这些肽基化合物预计具有抗炎性和细胞增殖抑制作用。
• Compounds for Proteasome Enzyme Inhibition
  申请人：Onyx Therapeutics, Inc.

  公开号：EP2564834A2

  公开（公告）日：2013-03-06

  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 activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

  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。肽基化合物包括环氧化物或氮丙啶，以及 N 端的官能化。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。
• Compounds For Enzyme Inhibition
  申请人：Onyx Therapeutics, Inc.

  公开号：EP2623113A2

  公开（公告）日：2013-08-07

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.

  肽基化合物包括含杂原子的三元环，能有效并选择性地抑制与蛋白酶体相关的 N-末端亲核（Ntn）水解酶的特定活性。肽基化合物包括环氧化物或氮丙啶，并在 N 端进行了官能化。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。由于这些肽基蛋白酶体抑制剂具有生物利用度高的特点，因此可以口服给药。
• COMPOUNDS FOR PROTEASOME ENZYME INHIBITION
  申请人：Onyx Therapeutics, Inc.

  公开号：EP1781688B1

  公开（公告）日：2011-01-19