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Page 1
SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance.
Jensen-Pergakes K, Tatlock J, Maegley KA, McAlpine IJ, McTigue M, Xie T, Dillon CP, Wang Y, Yamazaki S, Spiegel N, Shi M, Nemeth A, Miller N, Hendrickson E, Lam H, Sherrill J, Chung CY, McMillan EA, Bryant SK, Palde P, Braganza J, Brooun A, Deng YL, Goshtasbi V, Kephart SE, Kumpf RA, Liu W, Patman RL, Rui E, Scales S, Tran-Dube M, Wang F, Wythes M, Paul TA. Jensen-Pergakes K, et al. Among authors: tran dube m. Mol Cancer Ther. 2022 Jan;21(1):3-15. doi: 10.1158/1535-7163.MCT-21-0620. Epub 2021 Nov 4. Mol Cancer Ther. 2022. PMID: 34737197
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
Cui JJ, Tran-Dubé M, Shen H, Nambu M, Kung PP, Pairish M, Jia L, Meng J, Funk L, Botrous I, McTigue M, Grodsky N, Ryan K, Padrique E, Alton G, Timofeevski S, Yamazaki S, Li Q, Zou H, Christensen J, Mroczkowski B, Bender S, Kania RS, Edwards MP. Cui JJ, et al. J Med Chem. 2011 Sep 22;54(18):6342-63. doi: 10.1021/jm2007613. Epub 2011 Aug 18. J Med Chem. 2011. PMID: 21812414
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.
Cui JJ, McTigue M, Nambu M, Tran-Dubé M, Pairish M, Shen H, Jia L, Cheng H, Hoffman J, Le P, Jalaie M, Goetz GH, Ryan K, Grodsky N, Deng YL, Parker M, Timofeevski S, Murray BW, Yamazaki S, Aguirre S, Li Q, Zou H, Christensen J. Cui JJ, et al. J Med Chem. 2012 Sep 27;55(18):8091-109. doi: 10.1021/jm300967g. Epub 2012 Sep 10. J Med Chem. 2012. PMID: 22924734
Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats.
Cui JJ, Shen H, Tran-Dubé M, Nambu M, McTigue M, Grodsky N, Ryan K, Yamazaki S, Aguirre S, Parker M, Li Q, Zou H, Christensen J. Cui JJ, et al. J Med Chem. 2013 Sep 12;56(17):6651-65. doi: 10.1021/jm400926x. Epub 2013 Aug 29. J Med Chem. 2013. PMID: 23944843
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.
Bagal SK, Andrews M, Bechle BM, Bian J, Bilsland J, Blakemore DC, Braganza JF, Bungay PJ, Corbett MS, Cronin CN, Cui JJ, Dias R, Flanagan NJ, Greasley SE, Grimley R, James K, Johnson E, Kitching L, Kraus ML, McAlpine I, Nagata A, Ninkovic S, Omoto K, Scales S, Skerratt SE, Sun J, Tran-Dubé M, Waldron GJ, Wang F, Warmus JS. Bagal SK, et al. Among authors: tran dube m. J Med Chem. 2018 Aug 9;61(15):6779-6800. doi: 10.1021/acs.jmedchem.8b00633. Epub 2018 Jul 27. J Med Chem. 2018. PMID: 29944371
Cu-Catalyzed Hydroboration of Benzylidenecyclopropanes: Reaction Optimization, (Hetero)Aryl Scope, and Origins of Pathway Selectivity.
Medina JM, Kang T, Erbay TG, Shao H, Gallego GM, Yang S, Tran-Dubé M, Richardson PF, Derosa J, Helsel RT, Patman RL, Wang F, Ashcroft CP, Braganza JF, McAlpine I, Liu P, Engle KM. Medina JM, et al. Among authors: tran dube m. ACS Catal. 2019 Dec 6;9(12):11130-11136. doi: 10.1021/acscatal.9b03557. Epub 2019 Oct 29. ACS Catal. 2019. PMID: 32617185 Free PMC article.
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