Doxorubicin immunoconjugates containing bivalent, lysosomally-Cleavable dipeptide linkages

التفاصيل البيبلوغرافية
العنوان: Doxorubicin immunoconjugates containing bivalent, lysosomally-Cleavable dipeptide linkages
المؤلفون: Michael A. Walker, Shilpa Radia, Dalton King, Shirley J. Lasch, David Willner, Hofstead Sandra J, Gene M. Dubowchik, Harold Mastalerz, Raymond A. Firestone, Pamela A. Trail
المصدر: Bioorganic & Medicinal Chemistry Letters. 12:1529-1532
بيانات النشر: Elsevier BV, 2002.
سنة النشر: 2002
مصطلحات موضوعية: Immunoconjugates, Lung Neoplasms, medicine.drug_class, Stereochemistry, media_common.quotation_subject, Clinical Biochemistry, Pharmaceutical Science, Peptide, Monoclonal antibody, Biochemistry, Cathepsin B, Inhibitory Concentration 50, chemistry.chemical_compound, Drug Discovery, Tumor Cells, Cultured, medicine, Humans, Doxorubicin, Sulfhydryl Compounds, Internalization, Molecular Biology, media_common, chemistry.chemical_classification, Binding Sites, Dipeptide, Organic Chemistry, Antibodies, Monoclonal, Stereoisomerism, Biological activity, Dipeptides, Immunoconjugate, chemistry, Chromatography, Gel, Molecular Medicine, Lysosomes, Dimerization, Half-Life, Conjugate, medicine.drug
الوصف: Bivalent doxorubicin (DOX)-dipeptides ( 16a – c ) were prepared and conjugated to the monoclonal antibody BR96. The dipeptides are cleaved by lysosomal proteases following internalization of the resulting immunoconjugates. Conjugate 18b demonstrated antigen-specific in vitro tumor cell killing activity (IC 50 =0.2 μM) that was equipotent to DOX with a near doubling of drug molecules/MAb. Size exclusion chromatography showed 18b to be a noncovalent dimer that was formed immediately upon conjugation.
تدمد: 0960-894X
DOI: 10.1016/s0960-894x(02)00194-4
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::933401d420d7b01374ef7d812e2fa84b
https://doi.org/10.1016/s0960-894x(02)00194-4
Rights: CLOSED
رقم الانضمام: edsair.doi.dedup.....933401d420d7b01374ef7d812e2fa84b
قاعدة البيانات: OpenAIRE
الوصف
تدمد:0960894X
DOI:10.1016/s0960-894x(02)00194-4