Discovery of small molecule inhibitors that interact with γ‐tubulin (original) (raw)
2012, Chemical Biology & …
Recent studies have shown an overexpression of ctubulin in human glioblastomas and glioblastoma cell lines. As the 2-year survival rate for glioblastoma is very poor, potential benefit exists for discovering novel chemotherapeutic agents that can inhibit c-tubulin, which is known to form a ring complex that acts as a microtubule nucleation center. We present experimental evidence that colchicine and combretastatin A-4 bind to c-tubulin, which are to our knowledge the first drug-like compounds known to interact with c-tubulin. Molecular dynamics simulations and docking studies were used to analyze the hypothesized c-tubulin binding domain of these compounds. The suitability of the potential binding modes was evaluated and suggests the subsequent rational design of novel targeted inhibitors of c-tubulin.
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