Proceedings of the National Academy of Sciences - PNAS, 2005-08, Vol.102 (34), p.12095-12100
2005
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Details
- Autor(en) / Beteiligte
- Titel
- A Role for Transferrin Receptor in Triggering Apoptosis When Targeted with Gambogic Acid
- Ist Teil von
- Proceedings of the National Academy of Sciences - PNAS, 2005-08, Vol.102 (34), p.12095-12100
- Ort / Verlag
- United States: National Academy of Sciences
- Erscheinungsjahr
- 2005
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Transferrin receptor (TfR) has been shown to be significantly overexpressed in different types of cancers. We discovered TfR as a target for gambogic acid (GA), used in traditional Chinese medicine and a previously undiscovered link between TfR and the rapid activation of apoptosis. The binding site of GA on TfR is independent of the transferrin binding site, and it appears that GA potentially inhibits TfR internalization. Down-regulation of TfR by RNA interference decreases sensitivity to GA-induced apoptosis, further supporting TfR as the primary GA receptor. In summary, GA binding to TfR induces a unique signal leading to rapid apoptosis of tumor cells. These results suggest that GA may provide an additional approach for targeting the TfR and its use in cancer therapy.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0027-8424eISSN: 1091-6490DOI: 10.1073/pnas.0406731102Titel-ID: cdi_pubmed_primary_16103367
- Format
- –
- Schlagworte
- Acids, Antibodies, Apoptosis, Apoptosis - drug effects, Apoptosis - physiology, Binding Sites, Biological Sciences, Cancer, Cell Line, Tumor, Cell lines, Cells, DNA Primers, Down regulation, Drug therapy, Drugs, Chinese Herbal - pharmacology, Drugs, Chinese Herbal - therapeutic use, Epithelial cells, Fluorescent Antibody Technique, Gene Expression Regulation, Neoplastic - drug effects, Human umbilical vein endothelial cells, Humans, Immunohistochemistry, Internalization, Microscopy, Electron, Neoplasms - drug therapy, Receptors, Receptors, Transferrin - metabolism, Reverse Transcriptase Polymerase Chain Reaction, Ribonucleic acid, RNA, RNA Interference, Small interfering RNA, T lymphocytes, Tumors, Xanthones - pharmacology, Xanthones - therapeutic use