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Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.
Cheung YY, Yu H, Xu K, Zou B, Wu M, McManus OB, Li M, Lindsley CW, Hopkins CR. Cheung YY, et al. Among authors: xu k. J Med Chem. 2012 Aug 9;55(15):6975-9. doi: 10.1021/jm300700v. Epub 2012 Jul 26. J Med Chem. 2012. PMID: 22793372 Free PMC article.
Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.
Mattmann ME, Yu H, Lin Z, Xu K, Huang X, Long S, Wu M, McManus OB, Engers DW, Le UM, Li M, Lindsley CW, Hopkins CR. Mattmann ME, et al. Among authors: xu k. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5936-41. doi: 10.1016/j.bmcl.2012.07.060. Epub 2012 Aug 2. Bioorg Med Chem Lett. 2012. PMID: 22910039 Free PMC article.
Capmatinib is an effective treatment for MET-fusion driven pediatric high-grade glioma and synergizes with radiotherapy.
Zuckermann M, He C, Andrews J, Bagchi A, Sloan-Henry R, Bianski B, Xie J, Wang Y, Twarog N, Onar-Thomas A, Ernst KJ, Yang L, Li Y, Zhu X, Ocasio JK, Budd KM, Dalton J, Li X, Chepyala D, Zhang J, Xu K, Hover L, Roach JT, Chan KC, Hofmann N, McKinnon PJ, Pfister SM, Shelat AA, Rankovic Z, Freeman BB 3rd, Chiang J, Jones DTW, Tinkle CL, Baker SJ. Zuckermann M, et al. Among authors: xu k. Mol Cancer. 2024 Jun 7;23(1):123. doi: 10.1186/s12943-024-02027-6. Mol Cancer. 2024. PMID: 38849845
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