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- W63497172 abstract "Ras proteins, particularly their active GTP-bound forms (Ras·GTP), were thought “undruggable” owing to the absence of apparent drug-accepting pockets in their crystal structures. Only recently, such pockets have been found in the crystal structures representing a novel Ras·GTP conformation. We have conducted an in silico docking screen targeting a pocket in the crystal structure of M-RasP40D·GTP and obtained Kobe0065, which, along with its analogue Kobe2602, inhibits binding of H-Ras·GTP to c-Raf-1. They inhibit the growth of H-rasG12V-transformed NIH3T3 cells, which are accompanied by downregulation of not only MEK/ERK but also Akt, RalA, and Sos, indicating the blockade of interaction with multiple effectors. Moreover, they exhibit antitumor activity on a xenograft of human colon carcinoma carrying K-rasG12V. The nuclear magnetic resonance structure of a complex of the compound with H-RasT35S·GTP confirms its insertion into the surface pocket. Thus, these compounds may serve as a novel scaffold for the development of Ras inhibitors with higher potency and specificity." @default.
- W63497172 created "2016-06-24" @default.
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- W63497172 date "2013-01-01" @default.
- W63497172 modified "2023-09-27" @default.
- W63497172 title "Discovery of Small-Molecule Ras Inhibitors that Display Antitumor Activity by Interfering with Ras·GTP–Effector Interaction" @default.
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- W63497172 doi "https://doi.org/10.1016/b978-0-12-420146-0.00001-9" @default.
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