Regular ArticleAdriamycin Conjugates of Human Transferrin Bind Transferrin Receptors and Kill K562 and HL60-Cells
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Transferrin and transferrin receptors update
2019, Free Radical Biology and MedicineCitation Excerpt :For example, single-chain fragments of the variable region targeting TfR1 with flexible linkers for conjugation with drugs have been developed, and clinical trials are being conducted to evaluate the safety and efficacy of these constructs in patients with cancer, demonstrating promising results [158]. Various Tf conjugates are used in drug and gene delivery systems [159]; among them, doxorubicin conjugated with Tf was shown to be selectively toxic to a variety of cancer cells [160–164]. This system may be effective for brain tumors because TfR1 is expressed on the blood brain barrier and is often over expressed in brain tumors.
The transferrin receptor and the targeted delivery of therapeutic agents against cancer
2012, Biochimica et Biophysica Acta - General SubjectsCitation Excerpt :ADR is a widely used chemotherapy in treating many forms of cancer, but ultimately exhibits severe side effects, including cardiotoxicity, myelosuppression, nephrotoxicity, extravasation, and bone marrow depression due to quick diffusion throughout the body [22]. To circumvent the adverse affects of ADR, it has been chemically conjugated to Tf in an effort to deliver it directly to cancer cells expressing high levels of TfR [23–26], resulting in an effectual tissue distribution, a prolonged half-life of ADR in blood, and controlled release from Tf [25]. This Tf–ADR conjugate has shown cytotoxicity in vitro against a variety of malignant human cell lines, including Lovo (colorectal adenocarcinoma), H-MESO-1 (mesothelioma), Hep2 (liver carcinoma), HL-60 (promyelocytic leukemia), K562 (erythroleukemia), HeLa (cervical adenocarcinoma), U-937 (histiocytic lymphoma), LXFL (lung carcinoma), and MDA-MB-428 (breast cancer) and the murine fibroblast cell line L929 [23–25,27–30].
Inhibition of transferrin iron release increases in vitro drug carrier efficacy
2007, Journal of Controlled ReleaseCitation Excerpt :DT was selected as a cytotoxin since the effective concentration range of DT (IC50 ~ 0.1 nM) [7] is consistent with the concentration range in which increases in cellular association were observed in the cellular trafficking assay (0.1 and 1 nM, Fig. 4). This is in contrast to cytotoxins such as adriamycin, whose effective concentration range is considerably higher (IC50 ~ 1 μM) [27]. Thus, oxalate Tf conjugates with these cytotoxins would not be expected to display increased efficacy, since differences in cellular association between oxalate Tf and native Tf diminish as concentrations rise to 10 nM (Fig. 4C).
The transferrin receptor part II: Targeted delivery of therapeutic agents into cancer cells
2006, Clinical ImmunologyTumor targeting based on the effect of enhanced permeability and retention (EPR) and the mechanism of receptor-mediated endocytosis (RME)
2004, International Journal of PharmaceuticsCancer nanomedicine: emergence, expansion, and expectations
2023, SN Applied Sciences