H-Cys-Gly-Asn-Lys-Arg-Thr-Arg-Gly-Cys-OH | 524916-43-6

• 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: H-Cys-Gly-Asn-Lys-Arg-Thr-Arg-Gly-Cys-OH
• 英文别名: CGNKRTRGC；LyP-1；(2R)-2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[2-[[(2R)-2-amino-3-sulfanylpropanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-3-sulfanylpropanoic acid
• CAS: 524916-43-6
• 化学式: C₃₆H₆₇N₁₇O₁₂S₂
• 分子量: 994.167
• InChiKey: PBVSAMVZJCJUHU-SLQNPQMPSA-N

物化性质

• 密度：
  1.60±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -10.8
• 重原子数：
  67
• 可旋转键数：
  34
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  516
• 氢给体数：
  19
• 氢受体数：
  18

反应信息

• 作为反应物：
  描述：

  H-Cys-Gly-Asn-Lys-Arg-Thr-Arg-Gly-Cys-OH 、 盐酸多柔比星 在 乙二胺四乙酸 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N-hydroxysulfosuccinimide sodium salt 、 sodium chloride 作用下， 以 二甲基亚砜 、 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  Design and In Vitro Evaluation of Bispecific Complexes and Drug Conjugates of Anticancer Peptide, LyP-1 in Human Breast Cancer

  摘要：

  ox-DSPL-LyP-1复合物在体外实验中显示出良好的疗效。

  DOI：

  10.1007/s11095-016-2066-2

文献信息

• Design and In Vitro Evaluation of Bispecific Complexes and Drug Conjugates of Anticancer Peptide, LyP-1 in Human Breast Cancer
  作者：Selin Seda Timur、Prashant Bhattarai、Reyhan Neslihan Gürsoy、İmran Vural、Ban-An Khaw

  DOI：10.1007/s11095-016-2066-2

  日期：2017.2

  LyP-1, a nine-amino-acid tumor homing peptide, selectively binds to its cognate receptor, p32. Overexpression of p32 in certain tumors should allow use of LyP-1 as a targeting agent for the delivery of therapeutic or diagnostic agents. Peptide conjugates are developed for enhanced pre-targeting of MDA-MB-231 breast cancer cells with peptide-antibody bispecific complexes and targeting with multiple-drug/-fluorophore-conjugated nano-polymers. LyP-1-anti-DTPA bispecific antibody complexes (LyP-1-bsAbCx) were generated by conjugation of anti-DTPA antibody and LyP-1. LyP-1–doxorubicin (Dox), Dox-DTPA-succinyl-polylysine (Dox-DSPL), Dox-DSPL-LyP-1, DTPA-Dox-poly glutamic acid (D-Dox-PGA) or DTPA-rhodamine conjugated polylysine (DSPL-RITC) were prepared. In vitro therapeutic efficacy and targeting by immunofluorescence in MDA-MB-231 breast cancer cells were assessed with Dox-LyP-1. Immunofluorescence visualization of cancer cells was evaluated after pretargeting with LyP-1-bsAbCx and targeting with DSPL-RITC. Cytotoxicity of Dox-LyP-1 conjugates was significantly greater than free doxorubicin (p < 0.0001). For fluorescent-labeled LyP-1, internalization occurred in 30 min in tumor cells. Fluorescence intensity of two-step targeted cells showed that pretargeting with LyP-1-bsAbC, followed by targeting with DSPL-RITC was greater than non-pretargeted DSPL-RITC (p < 0.05). Peptide-conjugates are effective targeting agents for MDA-MB-231 breast cancer cells in culture. LyP-1-bsAbCx and Dox-LyP-1 conjugates may allow development of novel targeted cancer therapy and diagnosis.

  ox-DSPL-LyP-1复合物在体外实验中显示出良好的疗效。