Title: Blocking blood flow to solid tumors by destabilizing tubulin: An approach to targeting tumor growth
Authors: Pérez-Pérez, María-Jesús ×
Priego, Eva-María
Bueno, Oskía
Martins, Maria Solange
Canela, María-Dolores
Liekens, Sandra #
Issue Date: Oct-2016
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:59 issue:19 pages:8685-8711
Abstract: 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 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).
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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