Article
Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.
Science translational medicine - 14 Jun 2017
Plenker Dennis, Riedel Maximilian, Brägelmann Johannes, Dammert Marcel A, Chauhan Rakhee, Knowles Phillip P, Lorenz Carina, Keul Marina, Bührmann Mike, Pagel Oliver, Tischler Verena, Scheel Andreas H, Schütte Daniel, Song Yanrui, Stark Justina, Mrugalla Florian, Alber Yannic, Richters André, Engel Julian, Leenders Frauke, Heuckmann Johannes M, Wolf Jürgen, Diebold Joachim, Pall Georg, Peifer Martin, Aerts Maarten, Gevaert Kris, Zahedi René P, Buettner Reinhard, Shokat Kevan M, McDonald Neil Q, Kast Stefan M, Gautschi Oliver, Thomas Roman K, Sos Martin L
Abstract excerpt
Oncogenic fusion events have been identified in a broad range of tumors. Among them, RET rearrangements represent distinct and potentially druggable targets that are recurrently found in lung adenocarcinomas. We provide further evidence that current anti-RET drugs may not be potent enough to induce durable responses in such tumors. We report that potent inhibitors, such as AD80 or ponatinib, that stably bind in...
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