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1. 发明申请

WO2010047509A3 ANTI-DR5 ANTIBODY WITH IMPROVED AFFINITY AND STABILITY, AND COMPOSITION FOR CANCER PREVENTION OR TREATMENT INCLUDING SAME 审中-公开
公开(公告)号：WO2010047509A3
公开(公告)日：2010-10-21
申请号：PCT/KR2009006036
申请日：2009-10-20
申请人： AJOU UNIV IND ACAD COOP FOUND , KIM YONG SUNG , KWON MYUNG HEE , LEE SEUNG HYUN , PARK KYUNG JIN
发明人： KIM YONG SUNG , KWON MYUNG HEE , LEE SEUNG HYUN , PARK KYUNG JIN
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , C12N15/13
CPC分类号： C07K16/2878 , A61K2039/505 , C07K2317/56 , C07K2317/565
摘要： The present invention relates to an anti-DR5 antibody with improved affinity and stability that specifically binds to the death receptor 5 (DR5) to destroy cancer cells effectively and the composition for cancer prevention or treatment including the same. The anti-DR5 antibody of the present invention causes mutageneses on the amino acid residues of VH-CDR2 and VH-CDR3 within the heavy chain variable region and the amino acid residue of VL-CDR3 within the light chain variable region of HW1 which is the known anti-DR5 antibody, and replaces the framework within the heavy chain variable region from a VH6 subtype to a VH3 subtype and replaces the framework within the light chain variable region with the framework part of Vk1 or Vk3 so that affinity and stability are improved over the known anti-DR5 antibody, HW1. In addition, the anti-DR5 antibody of the present invention effectively induces cell death with respect to TRAIL-sensitive cancer cells that express DR5 and TRAIL-resistant cancer cells that express DR5 by autophagy so that it may be usefully employed in preventing or treating cancers caused by DR5 expression.

2. 发明申请

WO2010047509A9 ANTI-DR5 ANTIBODY WITH IMPROVED AFFINITY AND STABILITY, AND COMPOSITION FOR CANCER PREVENTION OR TREATMENT INCLUDING SAME 审中-公开
标题翻译：具有改善的亲和力和稳定性的抗DR5抗体，以及用于癌症预防或治疗的组合物，包括相同的
公开(公告)号：WO2010047509A9
公开(公告)日：2010-09-02
申请号：PCT/KR2009006036
申请日：2009-10-20
申请人： AJOU UNIV IND ACAD COOP FOUND , KIM YONG SUNG , KWON MYUNG HEE , LEE SEUNG HYUN , PARK KYUNG JIN
发明人： KIM YONG SUNG , KWON MYUNG HEE , LEE SEUNG HYUN , PARK KYUNG JIN
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , C12N15/13
CPC分类号： C07K16/2878 , A61K2039/505 , C07K2317/56 , C07K2317/565
摘要： The present invention relates to an anti-DR5 antibody with improved affinity and stability that specifically binds to the death receptor 5 (DR5) to destroy cancer cells effectively and the composition for cancer prevention or treatment including the same. The anti-DR5 antibody of the present invention causes mutageneses on the amino acid residues of VH-CDR2 and VH-CDR3 within the heavy chain variable region and the amino acid residue of VL-CDR3 within the light chain variable region of HW1 which is the known anti-DR5 antibody, and replaces the framework within the heavy chain variable region from a VH6 subtype to a VH3 subtype and replaces the framework within the light chain variable region with the framework part of Vk1 or Vk3 so that affinity and stability are improved over the known anti-DR5 antibody, HW1. In addition, the anti-DR5 antibody of the present invention effectively induces cell death with respect to TRAIL-sensitive cancer cells that express DR5 and TRAIL-resistant cancer cells that express DR5 by autophagy so that it may be usefully employed in preventing or treating cancers caused by DR5 expression.
摘要翻译：本发明涉及特异性结合死亡受体5（DR5）以有效破坏癌细胞的具有改善的亲和力和稳定性的抗DR5抗体，并且涉及用于癌症预防或治疗的组合物以及包含其的组合物。本发明的抗DR5抗体对重链可变区内的VH-CDR2和VH-CDR3的氨基酸残基和HW1的轻链可变区内的VL -CDR3的氨基酸残基进行诱变，并将重链可变区内的框架从VH6亚型替换为VH3亚型并用Vk1或Vk3的框架部分置换轻链可变区内的框架，从而改善了亲和性和稳定性已知的抗DR5抗体HW1。此外，本发明的抗DR5抗体相对于表达DR5和TRAIL抗性癌细胞的TRAIL敏感性癌细胞，通过自噬来有效地诱导细胞死亡，从而其可有效用于预防或治疗癌症由DR5表达引起。

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