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    • 9. 发明申请
    • ASSESSING LEVELS OF O6-ALKYLGUANINE-DNA ALKYLTRANSFERASE IN VIVO
    • 评估VIVO中O6-氨基嘌呤-DNA烷基转移酶的水平
    • WO0185221A3
    • 2002-08-15
    • PCT/US0115370
    • 2001-05-14
    • UNIV DUKE
    • ZALUTSKY MICHAEL RCOLVIN MICHAELVAIDYANATHAN GANESAN
    • A61K51/04
    • A61K51/0491A61K51/04
    • Radiolabeled O6-derivatized guanine molecules can be used to form radiolabeled AGT molecules which can be detected in vivo assessment of AGT levels is useful for optimizing the efficacy of chemotherapy. In addition, assessing AGT levels in tumors in vivo permits selection of patients most likely to benefit from such chemotherapy and enables clinicians to monitor the effect of known and potential chemotherapeutic agents. In particular, methods have been developed for the efficient syntheses of [18F]FBG and [131I]IBG, both of which bind specifically to purified AGT. These two radiolabeled O6 benzylguanine analogues can be used to assess levels of AGT in vivo.
    • 放射性标记的O6衍生的鸟嘌呤分子可用于形成放射性标记的AGT分子,其可以在体内检测AGT水平的评估用于优化化疗的功效。 此外,在体内评估肿瘤中的AGT水平允许选择最有可能受益于这种化学疗法的患者,并使临床医生能够监测已知和潜在的化学治疗剂的作用。 特别地,已经开发了用于[18F] FBG和[131I] IBG的有效合成的方法,两者都特异性结合纯化的AGT。 这两种放射性标记的O6苄基鸟嘌呤类似物可用于评估体内AGT的水平。
    • 10. 发明申请
    • RADIOCONJUGATION OF INTERNALIZING ANTIBODIES
    • 内分泌抗体的放射免疫
    • WO0032240B1
    • 2001-03-01
    • PCT/US9928167
    • 1999-11-30
    • UNIV DUKE
    • ZALUTSKY MICHAEL R
    • A61K49/00A61K51/10
    • A61K49/0058A61K51/1093
    • Antibodies to cell surface ligands such as EGFRvIII can be used to therapeutically or diagnosticallly deliver a radiolabel to tumor cells with high selectivity. The utility of radioconjugated internalizing antibodies is limited, however, by release of the label and its reuptake into normal cells. The invention provides new technology for radioconjugation of internalizing antibodies which reduces the release of label and improves retention of radioconjugated antibodies in lysosomes, where radiation is more effectively and selectively delivered to the nucleus of tumor cells.
    • 细胞表面配体如EGFRvIII的抗体可用于治疗或诊断性地以高选择性向肿瘤细胞递送放射性标记。 然而,放射性缀合的内化抗体的效用是有限的,但是通过释放标记物并将其再吸收到正常细胞中。 本发明提供了用于内化抗体的放射性缀合的新技术,其减少标记的释放并改善放射性缀合的抗体在溶酶体中的保留,其中辐射被更有效地选择性递送到肿瘤细胞的核。