公开(公告)号：US07374767B2

公开(公告)日：2008-05-20

申请号：US10499458

申请日：2002-12-04

申请人： Silvio Ernesto Perea Rodriguez ,  Osvaldo Reyes Acosta ,  Nelson Francisco Santiago Vispo ,  Yaquelin Puchades Izaguirre ,  Ricardo Silva Rodriguez ,  Alejandro Moro Soria ,  Alicia Santos Savio ,  Luis Javier González López ,  Belkis González Barrios

发明人： Silvio Ernesto Perea Rodriguez ,  Osvaldo Reyes Acosta ,  Nelson Francisco Santiago Vispo ,  Yaquelin Puchades Izaguirre ,  Ricardo Silva Rodriguez ,  Alejandro Moro Soria ,  Alicia Santos Savio ,  Luis Javier González López ,  Belkis González Barrios

IPC分类号： A61K39/12

CPC分类号： C07K14/005 ,  A61K38/00 ,  A61K48/00 ,  C07K7/06 ,  C07K2319/10 ,  C12N7/00 ,  C12N2710/20022 ,  C12N2710/20032

摘要： This invention is related to the Molecular Pharmacology field and especially to the development of peptides useful for treating epithelial tumors and mainly those associated to oncogenic types of HPVs. The main objective of this invention is to identify peptides whose structure permits to block the Casein Kinase II (CKII) phosphorylation domain by direct interaction with such a site. In the present invention it is shown eleven cyclic peptides with different aminoacid sequences which inhibit the CKII phosphorylation in vitro, exhibit cytotoxicity on HPV-16 transformed cells (CaSki) and also increase the sensitivity of these cells to the cytostatic effect of interferon (IFN). Furthermore, the invention relates to the use of these peptides conjugated or fused to other peptides and chemical compounds which penetrates into cells as well as with the use of both peptide and chemical mimetic molecules.

摘要翻译： 本发明涉及分子药理学领域，特别涉及可用于治疗上皮肿瘤和主要与致癌型HPV相关的肽的发展。 本发明的主要目的是鉴定其结构允许通过与这种位点的直接相互作用阻断酪蛋白激酶II（CKII）磷酸化结构域的肽。 在本发明中，显示了11种具有不同氨基酸序列的环肽，其在体外抑制CKII磷酸化，对HPV-16转化细胞（CaSki）表现出细胞毒性，并且还增加了这些细胞对干扰素（IFN）的细胞抑制作用的敏感性， 。 此外，本发明涉及这些肽与其它肽和化合物共轭或融合的用途，这些肽和化合物可以渗入细胞以及使用肽和化学模拟分子。

公开(公告)号：US20060233742A1

公开(公告)日：2006-10-19

申请号：US10499458

申请日：2002-12-04

申请人： Silvio Rodriguez ,  Osvaldo Reyes Acosta ,  Nelson Santiago Vispo ,  Yaquelin Puchades Izaguirre ,  Ricardo Silva Rodriguez ,  Alejandro Moro Soria ,  Alicia Santos Savio ,  Luis González López ,  Belkis González Barrios

发明人： Silvio Rodriguez ,  Osvaldo Reyes Acosta ,  Nelson Santiago Vispo ,  Yaquelin Puchades Izaguirre ,  Ricardo Silva Rodriguez ,  Alejandro Moro Soria ,  Alicia Santos Savio ,  Luis González López ,  Belkis González Barrios

IPC分类号： A61K38/19 ,  A61K38/10 ,  A61K38/12 ,  A61K38/21

CPC分类号： C07K14/005 ,  A61K38/00 ,  A61K48/00 ,  C07K7/06 ,  C07K2319/10 ,  C12N7/00 ,  C12N2710/20022 ,  C12N2710/20032

摘要： This invention is related to the Molecular Pharmacology field and especially to the development of peptides useful for treating epithelial tumors and mainly those associated to oncogenic types of HPVs. The main objective of this invention is to identify peptides whose structure permits to block the Casein Kinase II (CKII) phosphorylation domain by direct interaction with such a site. In the present invention it is shown eleven cyclic peptides with different aminoacid sequences which inhibit the CKII phosphorylation in vitro, exhibit cytotoxicity on HPV-16 transformed cells (CaSki) and also increase the sensitivity of these cells to the cytostatic effect of interferon (IFN). Furthermore, the invention relates to the use of these peptides conjugated or fused to other peptides and chemical compounds which penetrates into cells as well as with the use of both peptide and chemical mimetic molecules.

摘要翻译： 本发明涉及分子药理学领域，特别涉及可用于治疗上皮肿瘤和主要与致癌型HPV相关的肽的发展。 本发明的主要目的是鉴定其结构允许通过与这种位点的直接相互作用阻断酪蛋白激酶II（CKII）磷酸化结构域的肽。 在本发明中，显示了11种具有不同氨基酸序列的环肽，其在体外抑制CKII磷酸化，对HPV-16转化细胞（CaSki）表现出细胞毒性，并且还增加了这些细胞对干扰素（IFN）的细胞抑制作用的敏感性， 。 此外，本发明涉及这些肽与其它肽和化合物共轭或融合的用途，这些肽和化合物可以渗入细胞以及使用肽和化学模拟分子。