期刊
INTERDISCIPLINARY SCIENCES-COMPUTATIONAL LIFE SCIENCES
卷 2, 期 2, 页码 169-174出版社
SPRINGER HEIDELBERG
DOI: 10.1007/s12539-010-0076-z
关键词
tubulin; colchicine derivatives; generation; isotype sequence; binding energy
资金
- NSERC
- Alberta's Advanced Education and Technology
- Allard Foundation
- Alberta Cancer Board
Cytoskeletal proteins, such as tubulin, are a primary target for many successful anti-cancer drugs. The expression of several beta-tubulin isotypes in normal and cancerous cells provides a platform upon which to construct chemotherapeutic agents capable of differentiating between them. To test this hypothesis, we have previously designed several colchicine derivatives and computationally probed them for affinity to the beta-tubulin isotypes. Subsequent synthesis and cytotoxicity assays produced a small set of promising compounds exhibiting IC50 values approximately 30 fold lower than values previously reported for colchicine. Here we describe the creation and testing of these first-generation colchicine derivatives and discuss the subsequent design and preliminary computational screening of a novel set of second-generation derivatives using the most promising first-generation derivatives as scaffolds.
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