Anti-cancer drug design targeting a novel tertiary structure of ras oncogene product

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GTP-bound form of ras oncogene product Ras exhibits dynamic equilibrium between two interconverting conformations, "inactive" state 1 and "active" state 2. Based on a novel tertiary structure of Ras-GTP, we have performed in silico and in vitro screening for low molecular weight compounds which inhibit Ras function. Consequently, we have succeeded in identification of several hit compounds which specifically bind and inhibit Ras function in vitro and in vivo.