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161 results

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Page 1
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers.
Smith CR, Aranda R, Bobinski TP, Briere DM, Burns AC, Christensen JG, Clarine J, Engstrom LD, Gunn RJ, Ivetac A, Jean-Baptiste R, Ketcham JM, Kobayashi M, Kuehler J, Kulyk S, Lawson JD, Moya K, Olson P, Rahbaek L, Thomas NC, Wang X, Waters LM, Marx MA. Smith CR, et al. Among authors: christensen jg. J Med Chem. 2022 Feb 10;65(3):1749-1766. doi: 10.1021/acs.jmedchem.1c01900. Epub 2022 Jan 18. J Med Chem. 2022. PMID: 35041419 Free article.
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 pyrroloaminopyrazoles as novel PAK inhibitors.
Guo C, McAlpine I, Zhang J, Knighton DD, Kephart S, Johnson MC, Li H, Bouzida D, Yang A, Dong L, Marakovits J, Tikhe J, Richardson P, Guo LC, Kania R, Edwards MP, Kraynov E, Christensen J, Piraino J, Lee J, Dagostino E, Del-Carmen C, Deng YL, Smeal T, Murray BW. Guo C, et al. J Med Chem. 2012 May 24;55(10):4728-39. doi: 10.1021/jm300204j. Epub 2012 May 14. J Med Chem. 2012. PMID: 22554206
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
Glesatinib Exhibits Antitumor Activity in Lung Cancer Models and Patients Harboring MET Exon 14 Mutations and Overcomes Mutation-mediated Resistance to Type I MET Inhibitors in Nonclinical Models.
Engstrom LD, Aranda R, Lee M, Tovar EA, Essenburg CJ, Madaj Z, Chiang H, Briere D, Hallin J, Lopez-Casas PP, Baños N, Menendez C, Hidalgo M, Tassell V, Chao R, Chudova DI, Lanman RB, Olson P, Bazhenova L, Patel SP, Graveel C, Nishino M, Shapiro GI, Peled N, Awad MM, Jänne PA, Christensen JG. Engstrom LD, et al. Among authors: christensen jg. Clin Cancer Res. 2017 Nov 1;23(21):6661-6672. doi: 10.1158/1078-0432.CCR-17-1192. Epub 2017 Aug 1. Clin Cancer Res. 2017. PMID: 28765324 Clinical Trial.
The class I/IV HDAC inhibitor mocetinostat increases tumor antigen presentation, decreases immune suppressive cell types and augments checkpoint inhibitor therapy.
Briere D, Sudhakar N, Woods DM, Hallin J, Engstrom LD, Aranda R, Chiang H, Sodré AL, Olson P, Weber JS, Christensen JG. Briere D, et al. Among authors: christensen jg. Cancer Immunol Immunother. 2018 Mar;67(3):381-392. doi: 10.1007/s00262-017-2091-y. Epub 2017 Nov 9. Cancer Immunol Immunother. 2018. PMID: 29124315 Free PMC article.
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.
Fell JB, Fischer JP, Baer BR, Ballard J, Blake JF, Bouhana K, Brandhuber BJ, Briere DM, Burgess LE, Burkard MR, Chiang H, Chicarelli MJ, Davidson K, Gaudino JJ, Hallin J, Hanson L, Hee K, Hicken EJ, Hinklin RJ, Marx MA, Mejia MJ, Olson P, Savechenkov P, Sudhakar N, Tang TP, Vigers GP, Zecca H, Christensen JG. Fell JB, et al. Among authors: christensen jg. ACS Med Chem Lett. 2018 Nov 7;9(12):1230-1234. doi: 10.1021/acsmedchemlett.8b00382. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613331 Free PMC article.
161 results