Cys-Gly-Cys | 246231-57-2

• 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: Cys-Gly-Cys
• 英文别名: Cysteinyl glycyl cysteine；(2R)-2-[[2-[[(2R)-2-amino-3-sulfanylpropanoyl]amino]acetyl]amino]-3-sulfanylpropanoic acid
• CAS: 246231-57-2
• 化学式: C₈H₁₅N₃O₄S₂
• 分子量: 281.357
• InChiKey: URDUGPGPLNXXES-WHFBIAKZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.1
• 重原子数：
  17
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  124
• 氢给体数：
  6
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  Fmoc-L-丙氨酸 、 Fmoc-L-Cys(Trt)-PEG-PS 、 alkaline earth salt of/the/ methylsulfuric acid 生成 Cys-Gly-Cys
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Targeting of tumor vasculature using radiolabelled antibody L19 against fibronectin ED-B
  申请人：Philogen S.p.A.

  公开号：EP1514561A1

  公开（公告）日：2005-03-16

  A specific binding member that binds human ED-B, wherein the specific binding member is labelled with an isotope selected from the group consisting of 76Br, 77Br, 123I, 124I, 131I and 211At and comprises an antigen-binding site that comprises an antibody VH domain and an antibody VL domain, wherein the antibody VH domain is selected from the group consisting of the L19 VH domain, and a VH domain comprising a VH CDR1, a VH CDR2 and a VH CDR3, wherein the VH CDR3 is the L19 VH CDR3 of SEQ ID NO. 3, the VH CDR1 is optionally L19 VH CDR1 of SEQ ID NO. 1, and the VH CDR2 is optionally L19 VH CDR2 of SEQ ID NO. 2; and wherein the antibody VL domain is optionally selected from the group consisting of the L19 VL domain, and a VL domain comprising a VL CDR1, a VL CDR2 and a VL CDR3, wherein the VL CDR3 is the L19 VL CDR3 of SEQ ID NO. 6, the VL CDR1 is optionally L19 VL CDR1 of SEQ ID NO. 4, and the VL CDR2 is optionally L19 VL CDR2 of SEQ ID NO. 5; the L19 VH domain and L19 VL domain sequences being disclosed in Pini et al. (1998) J. Biol. Chem. 273: 21769-21776; wherein the specific binding member comprises a mini-immunoglobulin comprising said antibody VH domain and antibody VL domain fused to εS2-CH4 and dimerized or comprises a whole IgG1 antibody molecule; also methods and uses employing such a specific binding member.

  一种结合人类ED-B的特异结合成员，其中该特异结合成员标记有从76Br、77Br、123I、124I、131I和211At组成的同位素中选择的一种，并包括一个包含抗原结合位点的抗体VH结构域和抗体VL结构域，其中抗体VH结构域选自L19 VH结构域组，以及包括VH CDR1、VH CDR2和VH CDR3的VH结构域，其中VH CDR3是序列ID号为3的L19 VH CDR3，VH CDR1可以选择序列ID号为1的L19 VH CDR1，VH CDR2可以选择序列ID号为2的L19 VH CDR2；抗体VL结构域可以选择自L19 VL结构域组，以及包括VL CDR1、VL CDR2和VL CDR3的VL结构域，其中VL CDR3是序列ID号为6的L19 VL CDR3，VL CDR1可以选择序列ID号为4的L19 VL CDR1，VL CDR2可以选择序列ID号为5的L19 VL CDR2；L19 VH结构域和L19 VL结构域序列在Pini等人（1998）J. Biol. Chem. 273: 21769-21776中披露；其中该特异结合成员包括一个包含所述抗体VH结构域和抗体VL结构域的迷你免疫球蛋白融合到εS2-CH4并二聚化，或包括一个完整的IgG1抗体分子；还包括采用此类特异结合成员的方法和用途。
• [EN] IMMUNOCYTOKINE COMBINATION THERAPY<br/>[FR] POLYTHÉRAPIE PAR IMMUNOCYTOKINE
  申请人：PHILOGEN SPA

  公开号：WO2018154517A1

  公开（公告）日：2018-08-30

  This invention relates ιο methods and compositions, in a combination therapy, for treatment of neoplastic disease, including tenors and cancer, wherein an immunocytokine arid a small molecule drug conjugate which comprises a moiety capable of binding to a tumor-associated target, e.g., capable of binding to carbonic anhydrase IX (CAIX)S are administered. In preferred embodiments, the immunocytokine comprises an antibody targeting the ED~B or ED~A domain of fibronectin and interleakin-2, and the small molecule drug conjugate comprises a ligand moiety capable of binding to CAIX, a tinker, and a cytotoxic drug.

  该发明涉及一种用于治疗肿瘤性疾病的方法和组合疗法，包括肿瘤和癌症，其中给予一种免疫细胞因子和一种小分子药物结合物，该结合物包括能够结合到肿瘤相关靶标的部分，例如能够结合到碳酸酐酶IX（CAIX）的部分。在首选实施例中，免疫细胞因子包括靶向纤维连接蛋白的ED-B或ED-A结构域的抗体和白细胞介素-2，小分子药物结合物包括能够结合到CAIX的配体部分、一个连接物和一个细胞毒性药物。
• Selective targeting of tumor vasculature using antibody molecules
  申请人：Borsi Laura

  公开号：US20060057146A1

  公开（公告）日：2006-03-16

  The present invention relates to selectively targeting tumoral vasculature in vivo using a human recombinant scFv, L19, to the angiogenesis marker ED-B domain of fibronectin. In preferred embodiments, a complete human IgG1 is employed having the variable regions of L19. In other embodiments is employed a mini-immunoglobulin generated by fusing the scFv L19 to the constant CH4 domain of a secretory IgE isoform that naturally contains a cysteine in its COOH terminal and which forms a covalently linked dimer. Different in vivo behaviour of the antibody formats is exploitable for different diagnostic and/or therapeutic purposes, depending on clinical needs and disease. The antibody molecules may be labelled as described.

  本发明涉及使用人重组单链抗体（scFv）L19，针对纤维连接素的血管生成标记ED-B区域，有选择性地靶向体内的肿瘤血管。在优选实施例中，采用完整的人IgG1，其具有L19的可变区域。在其他实施例中，采用将scFv L19与分泌型IgE同工型的常数CH4结合形成的迷你免疫球蛋白，其在COOH末端天然含有半胱氨酸并形成共价连接的二聚体。抗体格式的不同体内行为可用于不同的诊断和/或治疗目的，具体取决于临床需求和疾病。抗体分子可以如所述标记。
• Selective targeting of tumor vasculature using radiolabelled antibody molecules
  申请人：Borsi Laura

  公开号：US20050074401A1

  公开（公告）日：2005-04-07

  A specific binding member that binds human ED-B, wherein the specific binding member is labelled with an isotope selected from the group consisting of 76 Br, 77 Br, 123 I, 124 I, 131 I and 211 At and comprises an antigen-binding site that comprises an antibody VH domain and an antibody VL domain, wherein the antibody VH domain is selected from the group consisting of the L19 VH domain, and a VH domain comprising a VH CDR1, a VH CDR2 and a VH CDR3, wherein the VH CDR3 is the L19 VH CDR3 of SEQ ID NO. 3, the VH CDR1 is optionally L19 VH CDR1 of SEQ ID NO. 1, and the VH CDR2 is optionally L19 VH CDR2 of SEQ ID NO. 2; and wherein the antibody VL domain is optionally selected from the group consisting of the L19 VL domain, and a VL domain comprising a VL CDR1, a VL CDR2 and a VL CDR3, wherein the VL CDR3 is the L19 VL CDR3 of SEQ ID NO. 6, the VL CDR1 is optionally L19 VL CDR1 of SEQ ID NO. 4, and the VL CDR2 is optionally L19 VL CDR2 of SEQ ID NO. 5; the L19 VH domain and L19 VL domain sequences being disclosed in Pini et al. (1998) J. Biol. Chem . 273: 21769-21776; wherein the specific binding member comprises a mini-immunoglobulin comprising said antibody VH domain and antibody VL domain fused to ε S2 -CH4 and dimerized or comprises a whole IgG1 antibody molecule; also methods and uses employing such a specific binding member.

  一种特定的结合成员，结合人类ED-B，其中该特定的结合成员标记有从76Br，77Br，123I，124I，131I和211At组成的同位素，包括一个抗原结合位点，该位点包括一个抗体VH域和一个抗体VL域，其中抗体VH域选自L19 VH域和包括VH CDR1、VH CDR2和VH CDR3的VH域，其中VH CDR3是SEQ ID NO. 3的L19 VH CDR3，VH CDR1是可选的SEQ ID NO. 1的L19 VH CDR1，VH CDR2是可选的SEQ ID NO. 2的L19 VH CDR2；其中抗体VL域可选自L19 VL域和包括VL CDR1、VL CDR2和VL CDR3的VL域，其中VL CDR3是SEQ ID NO. 6的L19 VL CDR3，VL CDR1是可选的SEQ ID NO. 4的L19 VL CDR1，VL CDR2是可选的SEQ ID NO. 5的L19 VL CDR2；L19 VH域和L19 VL域序列披露于Pini等人的(1998)J. Biol. Chem. 273: 21769-21776中；其中该特定的结合成员包括将所述抗体VH域和抗体VL域融合到εS2-CH4并二聚化的mini-免疫球蛋白或包括整个IgG1抗体分子的抗体分子；还包括使用该特定的结合成员的方法和用途。
• SELECTIVE TARGETING OF TUMOR VASCULATURE USING RADIOLABELLED ANTIBODY MOLECULES
  申请人：Borsi Laura

  公开号：US20090214423A1

  公开（公告）日：2009-08-27

  A specific binding member that binds human ED-B, wherein the specific binding member is labelled with an isotope selected from the group consisting of 76 Br, 77 Br, 123 I, 124 I, 131 I and 211 At and comprises an antigen-binding site that comprises an antibody VH domain and an antibody VL domain, wherein the antibody VH domain is selected from the group consisting of the L19 VH domain, and a VH domain comprising a VH CDR1, a VH CDR2 and a VH CDR3, wherein the VH CDR3 is the L19 VH CDR3 of SEQ ID NO. 3, the VH CDR1 is optionally L19 VH CDR1 of SEQ ID NO. 1, and the VH CDR2 is optionally L19 VH CDR2 of SEQ ID NO. 2; and wherein the antibody VL domain is optionally selected from the group consisting of the L19 VL domain, and a VL domain comprising a VL CDR1, a VL CDR2 and a VL CDR3, wherein the VL CDR3 is the L19 VL CDR3 of SEQ ID NO. 6, the VL CDR1 is optionally L19 VL CDR1 of SEQ ID NO. 4, and the VL CDR2 is optionally L19 VL CDR2 of SEQ ID NO. 5; the L19 VH domain and L19 VL domain sequences being disclosed in Pini et al. (1998) J. Biol. Chem . 273: 21769-21776; wherein the specific binding member comprises a mini-immunoglobulin comprising said antibody VH domain and antibody VL domain fused to ε S2 -CH4 and dimerized or comprises a whole IgG1 antibody molecule; also methods and uses employing such a specific binding member.

  一种特定结合成员，结合人源ED-B，其中该特定结合成员标记有从76Br、77Br、123I、124I、131I和211At组成的同位素，并且包括一个抗原结合位点，该位点包括一个抗体VH区域和一个抗体VL区域，其中抗体VH区域被选择于L19 VH区域和包括VH CDR1、VH CDR2和VH CDR3的VH区域之一，其中VH CDR3是SEQ ID NO. 3的L19 VH CDR3，VH CDR1是可选的SEQ ID NO. 1的L19 VH CDR1，VH CDR2是可选的SEQ ID NO. 2的L19 VH CDR2；抗体VL区域可选自L19 VL区域和包括VL CDR1、VL CDR2和VL CDR3的VL区域之一，其中VL CDR3是SEQ ID NO. 6的L19 VL CDR3，VL CDR1是可选的SEQ ID NO. 4的L19 VL CDR1，VL CDR2是可选的SEQ ID NO. 5的L19 VL CDR2；L19 VH区域和L19 VL区域序列在Pini et al. (1998) J. Biol. Chem. 273: 21769-21776中披露；其中特定结合成员包括将该抗体VH区域和抗体VL区域融合到εS2-CH4并二聚化的小型免疫球蛋白，或包括整个IgG1抗体分子；还涉及使用该特定结合成员的方法和用途。