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A precision therapy against cancers driven by KIT/PDGFRA mutations.
Evans EK, Gardino AK, Kim JL, Hodous BL, Shutes A, Davis A, Zhu XJ, Schmidt-Kittler O, Wilson D, Wilson K, DiPietro L, Zhang Y, Brooijmans N, LaBranche TP, Wozniak A, Gebreyohannes YK, Schöffski P, Heinrich MC, DeAngelo DJ, Miller S, Wolf B, Kohl N, Guzi T, Lydon N, Boral A, Lengauer C. Evans EK, et al. Among authors: brooijmans n. Sci Transl Med. 2017 Nov 1;9(414):eaao1690. doi: 10.1126/scitranslmed.aao1690. Sci Transl Med. 2017. PMID: 29093181 Clinical Trial.
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.
Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N, Shutes A, Winter C, Lengauer C, Kohl NE, Guzi T. Hagel M, et al. Among authors: brooijmans n. Cancer Discov. 2015 Apr;5(4):424-37. doi: 10.1158/2159-8290.CD-14-1029. Epub 2015 Mar 16. Cancer Discov. 2015. PMID: 25776529
Targeting kinases with precision.
Gardino AK, Evans EK, Kim JL, Brooijmans N, Hodous BL, Wolf B, Lengauer C. Gardino AK, et al. Among authors: brooijmans n. Mol Cell Oncol. 2018 Apr 11;5(3):e1435183. doi: 10.1080/23723556.2018.1435183. eCollection 2018. Mol Cell Oncol. 2018. PMID: 30250891 Free PMC article.
Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma.
Hatlen MA, Schmidt-Kittler O, Sherwin CA, Rozsahegyi E, Rubin N, Sheets MP, Kim JL, Miduturu C, Bifulco N, Brooijmans N, Shi H, Guzi T, Boral A, Lengauer C, Dorsch M, Kim RD, Kang YK, Wolf BB, Hoeflich KP. Hatlen MA, et al. Among authors: brooijmans n. Cancer Discov. 2019 Dec;9(12):1686-1695. doi: 10.1158/2159-8290.CD-19-0367. Epub 2019 Oct 1. Cancer Discov. 2019. PMID: 31575540
Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer.
Eno MS, Brubaker JD, Campbell JE, De Savi C, Guzi TJ, Williams BD, Wilson D, Wilson K, Brooijmans N, Kim J, Özen A, Perola E, Hsieh J, Brown V, Fetalvero K, Garner A, Zhang Z, Stevison F, Woessner R, Singh J, Timsit Y, Kinkema C, Medendorp C, Lee C, Albayya F, Zalutskaya A, Schalm S, Dineen TA. Eno MS, et al. Among authors: brooijmans n. J Med Chem. 2022 Jul 28;65(14):9662-9677. doi: 10.1021/acs.jmedchem.2c00704. Epub 2022 Jul 15. J Med Chem. 2022. PMID: 35838760 Free PMC article.
An ALK2 inhibitor, BLU-782, prevents heterotopic ossification in a mouse model of fibrodysplasia ossificans progressiva.
Davis AJ, Brooijmans N, Brubaker JD, Stevison F, LaBranche TP, Albayya F, Fleming P, Hodous BL, Kim JL, Kim S, Lobbardi R, Palmer M, Sheets MP, Vassiliadis J, Wang R, Williams BD, Wilson D, Xu L, Zhu XJ, Bouchard K, Hunter JW, Graul C, Greenblatt E, Hussein A, Lyon M, Russo J, Stewart R, Dorsch M, Guzi TJ, Kadambi V, Lengauer C, Garner AP. Davis AJ, et al. Among authors: brooijmans n. Sci Transl Med. 2024 May 29;16(749):eabp8334. doi: 10.1126/scitranslmed.abp8334. Epub 2024 May 29. Sci Transl Med. 2024. PMID: 38809966
Structure-based optimization of PKCtheta inhibitors.
Mosyak L, Xu Z, Joseph-McCarthy D, Brooijmans N, Somers W, Chaudhary D. Mosyak L, et al. Among authors: brooijmans n. Biochem Soc Trans. 2007 Nov;35(Pt 5):1027-31. doi: 10.1042/BST0351027. Biochem Soc Trans. 2007. PMID: 17956269 Review.
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
Verheijen JC, Richard DJ, Curran K, Kaplan J, Lefever M, Nowak P, Malwitz DJ, Brooijmans N, Toral-Barza L, Zhang WG, Lucas J, Hollander I, Ayral-Kaloustian S, Mansour TS, Yu K, Zask A. Verheijen JC, et al. Among authors: brooijmans n. J Med Chem. 2009 Dec 24;52(24):8010-24. doi: 10.1021/jm9013828. J Med Chem. 2009. PMID: 19894727
43 results