期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 19, 页码 8685-8711出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00463
关键词
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资金
- Spanish Ministerio de Economia y Competitividad [SAF2012-39760-C02-01, SAF2015-64629-C21-R]
- Comunidad de Madrid [BIPEDD2, P2010/BMD-2457]
- Fondo Social Europeo (FSE)
- JAE Predoc Programme
The unique characteristics of the tumor vasculature offer the possibility to selectively target tumor growth and vascularization using tubulin-destabilizing agents. Evidence accumulated with combretastatin A-4 (CA-4) and its prodrug CA-4P support the therapentic value of compound's sharing this mechanism of action. However, the chemical instability and poor solubility of CA-4 demand alternative compounds that are able to surmount these limitations. This Perspective illustrates the different classes of compounds that behave similar to CA-4, analyzes their binding mode to alpha beta-tubulin according to recently available structural complexes, and includes described approaches to improve their delivery. In addition, dissecting the mechanism of action of CA-4 and analogues allows a closer insight into the, advantages and drawbacks associated with these tubulin-destabilizing agents that behave as vascular disrupting agents (VDAs).
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