The DOI matches its Crossref record; 4 of the 4 references it cites were found in a registry or an index.
The biology of the combretastatins as tumour vascular targeting agents
Open accessAbstract
Summary: The tumour vasculature is an attractive target for therapy. Combretastatin A‐4 (CA‐4) and A‐1 (CA‐1) are tubulin binding agents, structurally related to colchicine, which induce vascular‐mediated tumour necrosis in animal models. CA‐1 and CA‐4 were isolated from the African bush willow, Combretum caffrum, and several synthetic analogues are also now available, such as the Aventis Pharma compound, AVE8062. More soluble, phosphated, forms of CA‐4 (CA‐4‐P) and CA‐1 (CA‐1‐P) are commonly used for in vitro and in vivo studies. These are cleaved to the natural forms by endogenous phosphatases and are taken up into cells. The lead compound, CA‐4‐P, is currently in clinical trial as a tumour vascular targeting agent. In animal models, CA‐4‐P causes a prolonged and extensive shut‐down of blood flow in established tumour blood vessels, with much less effect in normal tissues. This paper reviews the current understanding of the mechanism of action of the combretastatins and their therapeutic potential.
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Microtubules and signal transduction
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Endothelial-cell proliferation in experimental tumours
Denekamp, J., & Hobson, B. (1982) · British Journal of Cancer · doi:10.1038/bjc.1982.263 · Cited by 237
Cited by
Microtubules as a target for anticancer drugs
Jordan, M. A., & Wilson, L. (2004) · Nature Reviews Cancer · doi:10.1038/nrc1317 · Cited by 4,000
Anti‐mitotic activity of colchicine and the structural basis for its interaction with tubulin
Bhattacharyya, B., Panda, D., Gupta, S., & Banerjee, M. (2008) · Medicinal Research Reviews · doi:10.1002/med.20097 · Cited by 499
SuFEx Click Chemistry Enabled Late-Stage Drug Functionalization
Liu, Z., Li, J., Li, S., Li, G., Sharpless, K. B., & Wu, P. (2018) · Journal of the American Chemical Society · doi:10.1021/jacs.7b12788 · Cited by 319
Horin, L. J., Sonnett, M., Li, B., & Mitchison, T. J. (2025) · doi:10.1101/2025.01.22.632572 · Cited by 4
Metadata
- Authors
- TOZER, G. M., KANTHOU, C., PARKINS, C. S., & HILL, S. A.
- Venue
- International Journal of Experimental Pathology
- Publisher
- Wiley
- Published
- 2002-02
- Volume
- 83
- Issue
- 1
- Pages
- 21-38
- ISSN
- 0959-9673 (ISSN-L)
- 1365-2613
- OpenAlex
- W1725865716
- Cited by
- 335
- References
- 4
- FWCI
- 5.62
- Type
- journal article
- Language
- en
- Open access
- green
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