Combinatorial Chemistry & High Throughput Screening

Rathnam Chaguturu 
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Chemogenomics and Cancer Chemotherapy: Cell-Based Assays to Screen for Small Molecules that Impair Microtubule Dynamics

Author(s): Laurence Lafanechere.

Abstract:

Microtubules are still a promising target for new therapeutic agents. Thus, there is a continuous interest for compounds able to modify microtubule assembly, either by interacting directly with tubulin, or by interacting with microtubules regulators. Because of its dynamic characteristics, the microtubule cytoskeleton is a suitable target for small molecules that rapidly diffuse in the cell cytoplasm. Moreover, compounds targeting the microtubule cytoskeleton have proved to be valuable tools for basic research in cell biology. In this paper, after a short presentation of the apparent molecular pathways involved in the anticancer effect of agents that interfere with microtubules functions, the potentials and impact of chemogenomics and cell-based assays in the discovery of new therapeutic compounds and of new regulators of the microtubule cytoskeleton are described.

Keywords: Microtubules, tubulin post-translational modifications, cell-based assays, anti-cancer drugs, high content screening

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Article Details

VOLUME: 11
ISSUE: 8
Year: 2008
Page: [617 - 623]
Pages: 7
DOI: 10.2174/138620708785739943
Price: $58