Article
In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction.
Proceedings of the National Academy of Sciences of the United States of America - 14 May 2013
Shima Fumi, Yoshikawa Yoko, Ye Min, Araki Mitsugu, Matsumoto Shigeyuki, Liao Jingling, Hu Lizhi, Sugimoto Takeshi, Ijiri Yuichi, Takeda Azusa, Nishiyama Yuko, Sato Chie, Muraoka Shin, Tamura Atsuo, Osoda Tsutomu, Tsuda Ken-ichiro, Miyakawa Tomoya, Fukunishi Hiroaki, Shimada Jiro, Kumasaka Takashi, Yamamoto Masaki, Kataoka Tohru
Abstract excerpt
Mutational activation of the Ras oncogene products (H-Ras, K-Ras, and N-Ras) is frequently observed in human cancers, making them promising anticancer drug targets. Nonetheless, no effective strategy has been available for the development of Ras inhibitors, partly owing to the absence of well-defined surface pockets suitable for drug binding. Only recently, such pockets have been found in the crystal structures...
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