Herceptin-Geldanamycin Immunoconjugates
نویسندگان
چکیده
منابع مشابه
Herceptin-geldanamycin immunoconjugates: pharmacokinetics, biodistribution, and enhanced antitumor activity.
The efficacy of monoclonal antibodies (mAbs) as single agents in targeted cancer therapy has proven to be limited. Arming mAbs with a potent toxic drug could enhance their activity. Here we report that conjugating geldanamycin (GA) to the anti-HER2 mAb Herceptin improved the activity of Herceptin. The IC(50)s of the immunoconjugate H-GA were 10-200-fold lower than that of Herceptin in antiproli...
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BACKGROUND HER2 is a membrane receptor whose overexpression is strongly associated with poor prognosis in breast carcinomas. Inhibition of HER2 activity can reduce tumor growth, which led to the development of Herceptin, an anti-HER2 monoclonal antibody (MAb) that is already in clinical use. However, the objective response rate to Herceptin monotherapy is quite low. HER2 activity can also be in...
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PROLOGUE This paper discusses the scientific rationale, synthesis, therapeutic utility and clinical limitations of cancer chemotherapy with antineoplastic drugs or toxins covalently linked to monoclonal antibodies directed against tumor cell antigens. Chemical issues that must be considered when designing an effective antineoplastic immunoconjugate or immunotoxin (including purity, functional g...
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A new crystalline antimicrobial compound, geldanamycin, has been discovered in the culture nitrates of Streptomyces hygroscopicus var. geldanus var. nova. Geldanamycin is moderately active in vitro against protozoa, bacteria and fungi. It is also active against L-1210 and KB cells growing in culture and against the parasite Syphacia ohlevata, in vivo. The fermentation, assay, chromatography and...
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Trastuzumab (Herceptin), a humanized monoclonal antibody, is a cancer drug developed to target the human epidermal receptor (HER) 2, which is overexpressed in some cancer cells. Cutaneous side effects, such as folliculitis, xerosis, and alopecia have not been reported with therapies targeting HER2, in spite of the frequent observances of such with the therapies targeting the epidermal growth fa...
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ژورنال
عنوان ژورنال: Cancer Research
سال: 2004
ISSN: 0008-5472,1538-7445
DOI: 10.1158/0008-5472.can-03-2485