Article
Drug-drug conjugates of MEK and Akt inhibitors for RAS-mutant cancers.
Bioorganic & medicinal chemistry - 15 Mar 2024
Fujita Hikaru, Arai Sachiko, Arakawa Hiroshi, Hamamoto Kana, Kato Toshiyuki, Arai Tsubasa, Nitta Nanaka, Hotta Kazuki, Hosokawa Natsuko, Ohbayashi Takako, Takahashi Chiaki, Inokuma Yasuhide, Tamai Ikumi, Yano Seiji, Kunishima Munetaka, Watanabe Yoshihiro
Abstract excerpt
Controlling RAS mutant cancer progression remains a significant challenge in developing anticancer drugs. Whereas Ras G12C-covalent binders have received clinical approval, the emergence of further mutations, along with the activation of Ras-related proteins and signals, has led to resistance to Ras binders. To discover novel compounds to overcome this bottleneck, we focused on the concurrent and sustained...
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