(BOC2Lys)2Lys

• 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: (BOC2Lys)2Lys
• 英文别名: 2,6-Bis[2,6-bis[(2-methylpropan-2-yl)oxycarbonylamino]hexanoylamino]hexanoic acid
• 化学式: C₃₈H₇₀N₆O₁₂
• 分子量: 803.007
• InChiKey: PPQHRAJBZUBKRC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  56
• 可旋转键数：
  29
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  249
• 氢给体数：
  7
• 氢受体数：
  12

反应信息

• 作为反应物：
  描述：

  (BOC2Lys)2Lys 在 三氟乙酸 作用下， 反应 2.0h， 生成 2,6-Bis(2,6-diaminohexanoylamino)hexanoic acid
  参考文献：
  名称：

  Synthesis and characterization of ramose tetralactosyl-lysyl-chitosan-5-fluorouracil and its in vitro release

  摘要：

  为了提高药物负载量并实现良好的释放效果，本文采用了树枝状方法，选择壳聚糖作为载体，以5-氟尿嘧啶（5-Fu）作为模型药物。成功合成了树枝状壳聚糖-赖氨酸-5-Fu(3)和树枝状四乳糖基-赖氨酸-壳聚糖-5-Fu(6)，然后对(6)的体外释放进行了研究。结果显示，(3)和(6)的药物负载量分别为9.17%和1.63%（w/w）。研究了(6)在pH 7.4磷酸盐缓冲液和pH 1.2 HCl-KCl溶液中的体外释放行为。在碱性和酸性介质中，(6)维持零级释放的时间分别为64小时和24小时，184小时的总释放率分别为71.97%和82.34%。整个释放阶段表现平稳，相同时间下碱性环境中的累积释放浓度低于酸性环境。

  DOI：

  10.1007/s11164-011-0473-x
• 作为产物：
  描述：

  DL-赖氨酸 在 4-二甲氨基吡啶 、 N-羟基丁二酰亚胺 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 sodium hydroxide 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 31.0h， 生成 (BOC2Lys)2Lys
  参考文献：
  名称：

  Synthesis and characterization of ramose tetralactosyl-lysyl-chitosan-5-fluorouracil and its in vitro release

  摘要：

  为了提高药物负载量并实现良好的释放效果，本文采用了树枝状方法，选择壳聚糖作为载体，以5-氟尿嘧啶（5-Fu）作为模型药物。成功合成了树枝状壳聚糖-赖氨酸-5-Fu(3)和树枝状四乳糖基-赖氨酸-壳聚糖-5-Fu(6)，然后对(6)的体外释放进行了研究。结果显示，(3)和(6)的药物负载量分别为9.17%和1.63%（w/w）。研究了(6)在pH 7.4磷酸盐缓冲液和pH 1.2 HCl-KCl溶液中的体外释放行为。在碱性和酸性介质中，(6)维持零级释放的时间分别为64小时和24小时，184小时的总释放率分别为71.97%和82.34%。整个释放阶段表现平稳，相同时间下碱性环境中的累积释放浓度低于酸性环境。

  DOI：

  10.1007/s11164-011-0473-x

文献信息

• A reduction-responsive liposomal nanocarrier with self-reporting ability for efficient gene delivery
  作者：Bing Wang、Ji Zhang、Yan-Hong Liu、Wei Zhang、Ya-Ping Xiao、Rui-Mo Zhao、Xiao-Qi Yu

  DOI：10.1039/c8tb00392k

  日期：——

  A naphthalimide-sulfonamide-based bioreducible liposomal carrier is prepared for real-time self-reporting the reduction-responsive process in gene delivery via the generated fluorescence signal.

  一种基于萘酰亚胺磺酰胺的可生物还原的脂质体载体被制备，用于实时自报告基因传递中的还原响应过程，通过产生的荧光信号。
• Compounds
  申请人：SmithKline Beecham p.l.c.

  公开号：US06835712B1

  公开（公告）日：2004-12-28

  Spermine:peptide-based surfactant compounds are disclosed. The compounds are based on a spermine backbone with peptide groups and optionally hydrocarbyl groups linked thereto. Uses of the spermine:peptide-based surfactant compounds and methods for their production are also disclosed.

  本发明公开了基于精胺骨架的肽类表面活性剂化合物。该化合物基于精胺骨架，具有肽基团和可选择地与之连接的烃基团。本发明还公开了使用该精胺：肽类表面活性剂化合物的方法以及它们的制备方法。
• Multifunctional amphiphilic peptide dendrimer as nonviral gene vectors for effective cancer therapy via combined gene/photodynamic therapies
  作者：Xu-Ying Liu、Xi Zhang、Jing-Bo Yang、Cheng-Yan Wu、Qian Wang、Zhong-Lin Lu、Quan Tang

  DOI：10.1016/j.colsurfb.2022.112651

  日期：2022.9

  highest transfection efficiency up to 5.7-fold as compared with Lipo2000 in HeLa cells. Meanwhile, rapid endocytosis, successful endo/lysosomal escape, gene release and rapid nuclear delivery of DNA revealed the superiority of liposomes TTC-L-KKK/DOPE during gene delivery process. More importantly, efficient reactive oxygen species (ROS) generation by TTC-L-KKK/DOPE led to effective PDT, thus improving

  基因疗法对治疗基因相关疾病具有很大的前景。然而，安全和成功的临床应用迫切需要进一步推进构建有效的递送系统。在此，三种两亲性肽树枝状大分子 ( TTC - L- KRR/KKK/KHH )，含有天然氨基酸残基（赖氨酸K、精氨酸R和组氨酸H）和经烷基修饰的基于 AIE 的光敏剂（四苯基乙烯噻吩改性氰基丙烯酸酯，TTC）链 ( L )，已被设计和制备用于通过以下方式提高治疗效力基因疗法（GT）和光动力疗法（PDT）的结合。所有三种化合物都具有典型的聚集诱导发射 (AIE) 特性和超低临界胶束浓度 (CMC)。由两亲性肽树枝状大分子和二油酰磷脂酰乙醇胺（DOPE）组成的脂质体可以有效地将DNA结合成大小合适、形态规则、生物相容性好的纳米颗粒。其中，脂质体TTC- L- KKK/DOPE在HeLa细胞中的转染效率最高，是Lipo2000的5.7倍。同时，快速的内吞作用、成功的内/溶酶体逃逸、基因释放和DNA的快速核递送揭示了脂质体TTC
• Specially-Made Lipid-Based Assemblies for Improving Transmembrane Gene Delivery: Comparison of Basic Amino Acid Residue Rich Periphery
  作者：Qian Jiang、Dong Yue、Yu Nie、Xianghui Xu、Yiyan He、Shiyong Zhang、Ernst Wagner、Zhongwei Gu

  DOI：10.1021/acs.molpharmaceut.5b00967

  日期：2016.6.6

  Cationic lipid based assemblies provide a promising platform for effective gene condensation into nano sized particles, and the peripheral properties of the assemblies are vital for complexation and interaction with physical barriers. Here, we report three cationic twin head lipids, and each of them contains a dioleoyl-glutamate hydrophobic tail and a twin polar head of lysine, arginine, or histidine. Such lipids were proven to self-assemble in aqueous solution with well-defined nanostructures and residual amino-, guanidine-, or imidazole-rich periphery, showing strong buffering capacity and good liquidity. The assemblies with arginine (RL) or lysine (KL) periphery exhibited positive charges (similar to+35 mV) and complete condensation of pDNA into nanosized complexes (similar to 120 nm). In contrast, assemblies composed of histidine-rich lipids (HL) showed relatively low cationic electric potential (similar to+10 mV) and poor DNA binding ability. As expected, the designed RL assemblies with guanidine-rich periphery enhanced the in vitro gene transfection up to 190-fold as compared with the golden standard PEI25k and Lipofectamine 2000, especially in the presence of serum. Meanwhile, interaction with cell and endo/lysosome membrane also revealed the superiority of RL complexes, that the guanidine-rich surface efficiently promoted transmembrane process in cellular internalization and endosomal disruption. More importantly, RL complexes also succeeded beyond others in vivo with significantly (similar to 7-fold) enhanced expression in HepG2 tumor xenografts in mice, as well as stronger green fluorescence protein imaging in isolated tumors and tumor frozen sections.
• POLYMERIC BIOLUBRICANTS FOR MEDICAL USE
  申请人：Grinstaff Mark W.

  公开号：US20110243883A1

  公开（公告）日：2011-10-06

  The present invention provides branched polymers which can be used as lubricants or shock absorbers in vivo. For example, the inventive polymers can be used as viscosupplements, viscoelastics, tissue space fillers, and/or anti-adhesive agents. Also provided are pharmaceutical compositions comprising the inventive polymers and methods of using them including, for example, in the treatment of arthritic and sport-injured knee joints; in reconstruction or cosmetic procedures, intervertebral disc repair, treatment of vocal cord problems, treatment of urinary incontinence, and prevention of adhesion formation following abdominal or gynecological surgery.