Cbz-Arg-Arg-pNA

• 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: Cbz-Arg-Arg-pNA
• 英文别名: Z-Arg-Arg-NA；Z-Arg-Arg-pNA；benzyl N-[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-5-(diaminomethylideneamino)-1-(4-nitroanilino)-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
• 化学式: C₂₆H₃₆N₁₀O₆
• 分子量: 584.635
• InChiKey: UMXUPKWQORIVFR-SFTDATJTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  42
• 可旋转键数：
  16
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  271
• 氢给体数：
  7
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  Cbz-Arg-Arg-pNA 在 papain 、 1,4-二巯基-2,3-丁二醇 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 4-硝基苯胺
  参考文献：
  名称：

  Selective chromogenic and fluorogenic peptide substrates for the assay of cysteine peptidases in complex mixtures

  摘要：

  This study describes the design, synthesis, and use of selective peptide substrates for cysteine peptidases of the Cl papain family, important in many biological processes. The structure of the newly synthesized substrates is Glp-Xaa-Ala-Y (where Glp = pyroglutamyl; Xaa = Phe or Val; and Y = pNA [p-nitroanilide], AMC [4-amino-7-methylcoumaride], or AFC [4-amino-7-trifluoromethyl-coumaridel]). Substrates were synthesized enzymatically to guarantee selectivity of the reaction and optical purity of the target compounds, simplifying the scheme of synthesis and isolation of products. The hydrolysis of the synthesized substrates was evaluated by C1 cysteine peptidases from different organisms and with different functions, including plant enzymes papain, bromelain, ficin, and mammalian lysosomal cathepsins B and L. The new substrates were selective for C1 cysteine peptidases and were not hydrolyzed by serine, aspartic, or metallo peptidases. We demonstrated an application of the selectivity of the synthesized substrates during the chromatographic separation of a multicomponent set of digestive peptidases from a beetle, Tenebrio molitor. Used in combination with the cysteine peptidase inhibitor E-64, these substrates were able to differentiate cysteine peptidases from peptidases of other classes in midgut extracts from T. molitor larvae and larvae of the genus Tribolium; thus, they are useful in the analysis of complex mixtures containing peptidases from different classes. Published by Elsevier Inc.

  DOI：

  10.1016/j.ab.2013.12.032

文献信息

• Nanoparticle drug conjugates
  申请人：Memorial Sloan Kettering Cancer Center

  公开号：US10111963B2

  公开（公告）日：2018-10-30

  Described herein are nanoparticle drug conjugates (NDCs), which, in certain embodiments, comprise a non-toxic, multi-modality, clinically proven silica-based nanoparticle platform with covalently attached drug molecules/moieties. The nanoparticle drug conjugates (NDCs) demonstrate imaging capability and targeting ligands which efficiently clear through the kidneys. Furthermore, the conjugates incorporate therapeutic agents for cancer detection, prevention, and/or treatment.

  本文描述的是纳米颗粒药物共轭物（NDCs），在某些实施方案中，它包括无毒、多模态、经临床验证的硅基纳米颗粒平台与共价连接的药物分子/分子。纳米颗粒药物共轭物（NDCs）具有成像能力和靶向配体，能有效地通过肾脏清除。此外，这些共轭物还含有用于癌症检测、预防和/或治疗的治疗剂。
• NANOPARTICLE DRUG CONJUGATES
  申请人：Memorial Sloan Kettering Cancer Center

  公开号：EP3148591B1

  公开（公告）日：2020-03-11