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Title

Blocking Blood Flow to Solid Tumors by Destabilizing Tubulin : An Approach to Targeting Tumor Growth (Perspective)

AuthorsPeréz-Pérez, María-Jesús ; Priego, Eva María ; Bueno, Oskía; Martins, Maria Solange; Canela, María-Dolores ; Liekens, Sandra
Issue Date27-Jun-2016
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 59 : 8685−8711 (2016)
AbstractThe 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 therapeutic value of compounds 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 αβ- 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).
Publisher version (URL)http://dx.doi.org/10.1021/acs.jmedchem.6b00463
URIhttp://hdl.handle.net/10261/138559
DOI10.1021/acs.jmedchem.6b00463
ISSN0022-2623
E-ISSN1520-4804
Appears in Collections:(IQM) Artículos
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