PUBLICATION
A Macrocyclic Ruthenium(III) Complex Inhibits Angiogenesis with Down-Regulation of Vascular Endothelial Growth Factor Receptor-2 and Suppresses Tumor Growth In Vivo
- Authors
- Kwong, W.L., Lam, K.Y., Lok, C.N., Lai, Y.T., Lee, P.Y., Che, C.M.
- ID
- ZDB-PUB-161008-1
- Date
- 2016
- Source
- Angewandte Chemie (International ed. in English) 55(43): 13524-13528 (Journal)
- Registered Authors
- Keywords
- VEGFRs, angiogenesis, anti-cancer, ruthenium
- MeSH Terms
-
- Angiogenesis Inhibitors/chemistry
- Angiogenesis Inhibitors/pharmacology*
- Animals
- Antineoplastic Agents/chemistry
- Antineoplastic Agents/pharmacology*
- Cell Line, Tumor
- Cell Proliferation/drug effects
- Coordination Complexes/chemistry
- Coordination Complexes/pharmacology*
- Dose-Response Relationship, Drug
- Down-Regulation/drug effects
- Drug Screening Assays, Antitumor
- Female
- Human Umbilical Vein Endothelial Cells/drug effects
- Humans
- Macrocyclic Compounds/chemistry
- Macrocyclic Compounds/pharmacology*
- Mammary Neoplasms, Experimental/drug therapy
- Mammary Neoplasms, Experimental/pathology
- Mice
- Mice, Nude
- Neovascularization, Pathologic/drug therapy*
- Neovascularization, Pathologic/pathology
- Ruthenium/chemistry
- Ruthenium/pharmacology*
- Structure-Activity Relationship
- Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors*
- Vascular Endothelial Growth Factor Receptor-2/metabolism
- Zebrafish
- PubMed
- 27717148 Full text @ Angew. Chem. Int. Ed. Engl.
Citation
Kwong, W.L., Lam, K.Y., Lok, C.N., Lai, Y.T., Lee, P.Y., Che, C.M. (2016) A Macrocyclic Ruthenium(III) Complex Inhibits Angiogenesis with Down-Regulation of Vascular Endothelial Growth Factor Receptor-2 and Suppresses Tumor Growth In Vivo. Angewandte Chemie (International ed. in English). 55(43):13524-13528.
Abstract
A macrocyclic ruthenium(III) complex [RuIII (N2 O2 )Cl2 ]Cl (Ru-1) is reported as an inhibitor of angiogenesis and an anti-tumor compound. The complex is relatively non-cytotoxic towards endothelial and cancer cell lines in vitro, but specifically inhibited the processes of angiogenic endothelial cell tube formation and cancer cell invasion. Moreover, compared with known anti-cancer ruthenium complexes, Ru-1 is distinct in that it suppressed the expression of vascular endothelial growth factor receptor-2 (VEGFR2), and the associated downstream signaling that is crucial to tumor angiogenesis. In addition, in vivo studies showed that Ru-1 inhibited angiogenesis in a zebrafish model and suppressed tumor growth in nude mice bearing cancer xenografts.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping