Cancer is a leading cause of death worldwide. The control of metastasis is one of the most important issues in cancer research. The design of novel antimetastatic drugs is of great importance and so is the understanding of the molecular mechanisms and key components driving tumor growth and metastasis. Over-expressed in various cancers, fascin has emerged as a promising target for the treatment of cancer metastasis. Migrastatin, a potent inhibitor of tumor cell migration, has been employed as a lead compound in the development of series of analogs with enhanced tumor cell migration inhibitory properties. The identification of fascin as a macroketone (migrastatin analog) target provided new insights for drug discovery. In the present work, X-ray crystal structural and molecular modeling studies were performed to reveal the molecular and structural basis for the antimetastatic effects of these compounds. The biochemical, structural and molecular modeling results will be presented.

Structural and chemical basis for the antimetastatic properties of a series of migrastatin analogs

243rd National Meeting (2012)

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