1,2-Diheptadecanoyl-sn-glycero-3-phosphoethanolamine

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 甘油磷脂
• 英文名称: 1,2-Diheptadecanoyl-sn-glycero-3-phosphoethanolamine
• 英文别名: [(2R)-3-[2-aminoethoxy(hydroxy)phosphoryl]oxy-2-heptadecanoyloxypropyl] heptadecanoate
• 化学式: C₃₉H₇₈NO₈P
• 分子量: 720.024
• InChiKey: YSFFAUPDXKTJMR-DIPNUNPCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  13.5
• 重原子数：
  49
• 可旋转键数：
  41
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.95
• 拓扑面积：
  139
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  α-D-mannopyranosyl-2-glycolaldehyde 、 1,2-Diheptadecanoyl-sn-glycero-3-phosphoethanolamine 在 sodium cyanoborohydride 、 溶剂黄146 作用下， 以 甲醇 、 氯仿 、 二甲基亚砜 为溶剂， 反应 30.0h， 以53%的产率得到Heptadecanoic acid (R)-1-heptadecanoyloxymethyl-2-(hydroxy-{2-[2-((2S,3S,4S,5S,6R)-3,4,5-trihydroxy-6-hydroxymethyl-tetrahydro-pyran-2-yloxy)-ethylamino]-ethoxy}-phosphoryloxy)-ethyl ester
  参考文献：
  名称：

  Probing Low Affinity and Multivalent Interactions with Surface Plasmon Resonance:  Ligands for Concanavalin A

  摘要：

  The affinities of the carbohydrate-binding protein concanavalin A (Con A) for mono- and multivalent ligands were measured by surface plasmon resonance (SPR) detection. Assessing protein-carbohydrate affinities is typically difficult due to weak affinities observed and the complications that arise from the importance of multivalency in these interactions. We describe a convenient method to rapidly evaluate the inhibitory constants for a panel of different ligands, both monovalent and multivalent, for low-affinity receptors, such as the carbohydrate-binding protein Con A. A nonnatural, mannose-substituted glycolipid was synthesized, and self-assembled monolayers of varying carbohydrate density were generated. The synthetic surfaces bind Con A. Competition experiments that employed monovalent ligands in solution yielded K-i values similar to equilibrium binding constants obtained in titration microcalorimetry experiments. In addition, this assay could be used to examine various polymeric ligands of defined lengths, generated by ring-opening metathesis polymerization (ROMP). This study demonstrates the utility of this method for rapidly screening ligands that engage in low affinity interactions with their target receptors. Our results emphasize that those molecules that can simultaneously occupy two or more saccharide binding sites within a lectin oligomer are effective inhibitors of protein-carbohydrate interactions.

  DOI：

  10.1021/ja9818506

文献信息

• [EN] BRANCHED PEG MOLECULES AND RELATED COMPOSITIONS AND METHODS<br/>[FR] MOLÉCULES DE PEG RAMIFIÉ, COMPOSITIONS ET PROCÉDÉS ASSOCIÉS
  申请人：PHASERX INC

  公开号：WO2018126084A1

  公开（公告）日：2018-07-05

  Disclosed are branched PEG molecules, including branched PEG-lipids and branched-PEG proteins, as well as related compositions and methods for making branched PEG molecules. Also disclosed are related compositions, systems, and methods for in vivo delivery of therapeutic and diagnostic agents.

  揭示了分支聚乙二醇（PEG）分子，包括分支PEG-脂质和分支PEG-蛋白质，以及制备分支PEG分子的相关组合物和方法。还公开了相关的组合物、系统和方法，用于体内传递治疗和诊断试剂。
• Functional associative coatings for nanoparticles
  申请人：Hainfeld James F.

  公开号：US20080089836A1

  公开（公告）日：2008-04-17

  Described herein are nanoparticles that are coated with a bilayer of molecules formed from surface binding molecules and amphiphatic molecules. The bilayer coating self assembles on the nanoparticles from readily available materials/molecules. The modular design of the bilayer coated nanoparticles provides a means for readily and efficiently optimizing the properties of the bilayer coated nanoparticle compositions. Also described herein are uses of such nanoparticles in medicine, laboratory techniques, industrial and commerical applications.

  本文描述了一种纳米颗粒，其表面涂覆有由表面结合分子和两亲分子形成的双层分子层。该双层涂层可以自组装在纳米颗粒上，使用易得的材料/分子。双层涂层纳米颗粒的模块化设计提供了一种方便和高效地优化其性质的方法。此外，本文还描述了这种纳米颗粒在医学、实验室技术、工业和商业应用中的用途。
• Liposomal formulation of nonglycosidic ceramides and uses thereof
  申请人：LUDWIG INSTITUTE FOR CANCER RESEARCH LTD.

  公开号：US10039715B2

  公开（公告）日：2018-08-07

  The invention provides liposomes containing nonglycosidic ceramides within their bilayers, and compositions thereof. These liposomes activate murine iNKT cells and induce dendritic cell (DC) maturation, both in vitro and in vivo at an efficacy that is comparable to their corresponding soluble nonglycosidic ceramides. Also provided are methods for treating diseases using the liposomes and compositions of the invention.

  本发明提供了在其双层内含有非糖苷类神经酰胺的脂质体及其组合物。这些脂质体可在体外和体内激活小鼠 iNKT 细胞并诱导树突状细胞（DC）成熟，其功效与相应的可溶性非糖苷神经酰胺相当。此外，还提供了使用本发明脂质体和组合物治疗疾病的方法。
• Combinations of mRNAs encoding immune modulating polypeptides and uses thereof
  申请人：ModernaTX, Inc.

  公开号：US10172808B2

  公开（公告）日：2019-01-08

  The disclosure relates to compositions and methods for the preparation, manufacture and therapeutic use of combinations of immunomodulatory polynucleotides (e.g., mRNAs) encoding an immune response primer polypeptide (e.g., an interleukin 23 (IL-23) polypeptide or an interleukin 36γ (IL-36-gamma) polypeptide), and an immune response co-stimulatory signal polypeptide (e.g., an OX40L polypeptide).

  本公开涉及免疫调节多核苷酸（如mRNA）编码免疫应答引物多肽（如白细胞介素23（IL-23）多肽或白细胞介素36γ（IL-36-γ）多肽）和免疫应答共刺激信号多肽（如OX40L多肽）组合的制备、制造和治疗使用的组合物和方法。
• MRNA combination therapy for the treatment of cancer
  申请人：ModernaTX, Inc.

  公开号：US10335486B2

  公开（公告）日：2019-07-02

  The present disclosure relates to the use of nucleic acid (e.g., mRNA) combination therapies for the treatment of cancer. The disclosure provides compositions, and methods for their preparation, manufacture, and therapeutic use, wherein those compositions comprise at least two polynucleotides (e.g., mRNAs) in combination wherein the at least two polynucleotides are selected from the group consisting of (i) a polynucleotide encoding an immune response primer (e.g., IL23), (ii) a polynucleotide encoding an immune response co-stimulatory signal (e.g., OX40L), (iii) a polynucleotide encoding a checkpoint inhibitor (e.g., an anti CTLA-4 antibody), and, (iv) a combination thereof. The therapeutic methods disclosed herein comprise, e.g., the administration of a combination therapy disclosed herein for the treatment of cancer, e.g., by reducing the size of a tumor or inhibiting the growth of a tumor, in a subject in need thereof. In some aspects, the combination therapies disclosed herein disclosed are administered intratumorally.

  本公开涉及使用核酸（如mRNA）组合疗法治疗癌症。本公开提供了组合物及其制备、制造和治疗使用的方法，其中这些组合物包括至少两种组合在一起的多核苷酸（如mRNA），其中至少两种多核苷酸选自由以下组成的组(i)编码免疫应答引物的多核苷酸（如IL23），(ii)编码免疫应答引物的多核苷酸（如IL23），(iii)编码免疫应答引物的多核苷酸（如IL23），(iv)编码免疫应答引物的多核苷酸（如IL23）、IL23），(ii) 编码免疫应答共刺激信号（如 OX40L）的多核苷酸，(iii) 编码检查点抑制剂（如抗 CTLA-4 抗体）的多核苷酸，以及 (iv) 其组合。本文公开的治疗方法包括，例如，在有需要的受试者中施用本文公开的用于治疗癌症的组合疗法，例如，通过减小肿瘤大小或抑制肿瘤生长。在某些方面，本文公开的组合疗法是肿瘤内给药。