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Page 1
DrugMap: A quantitative pan-cancer analysis of cysteine ligandability.
Takahashi M, Chong HB, Zhang S, Yang TY, Lazarov MJ, Harry S, Maynard M, Hilbert B, White RD, Murrey HE, Tsou CC, Vordermark K, Assaad J, Gohar M, Dürr BR, Richter M, Patel H, Kryukov G, Brooijmans N, Alghali ASO, Rubio K, Villanueva A, Zhang J, Ge M, Makram F, Griesshaber H, Harrison D, Koglin AS, Ojeda S, Karakyriakou B, Healy A, Popoola G, Rachmin I, Khandelwal N, Neil JR, Tien PC, Chen N, Hosp T, van den Ouweland S, Hara T, Bussema L, Dong R, Shi L, Rasmussen MQ, Domingues AC, Lawless A, Fang J, Yoda S, Nguyen LP, Reeves SM, Wakefield FN, Acker A, Clark SE, Dubash T, Kastanos J, Oh E, Fisher DE, Maheswaran S, Haber DA, Boland GM, Sade-Feldman M, Jenkins RW, Hata AN, Bardeesy NM, Suvà ML, Martin BR, Liau BB, Ott CJ, Rivera MN, Lawrence MS, Bar-Peled L. Takahashi M, et al. Among authors: brooijmans n. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22. Cell. 2024. PMID: 38653237
DrugMap: A quantitative pan-cancer analysis of cysteine ligandability.
Takahashi M, Chong HB, Zhang S, Lazarov MJ, Harry S, Maynard M, White R, Murrey HE, Hilbert B, Neil JR, Gohar M, Ge M, Zhang J, Durr BR, Kryukov G, Tsou CC, Brooijmans N, Alghali ASO, Rubio K, Vilanueva A, Harrison D, Koglin AS, Ojeda S, Karakyriakou B, Healy A, Assaad J, Makram F, Rachman I, Khandelwal N, Tien PC, Popoola G, Chen N, Vordermark K, Richter M, Patel H, Yang TY, Griesshaber H, Hosp T, van den Ouweland S, Hara T, Bussema L, Dong R, Shi L, Rasmussen MQ, Domingues AC, Lawless A, Fang J, Yoda S, Nguyen LP, Reeves SM, Wakefield FN, Acker A, Clark SE, Dubash T, Fisher DE, Maheswaran S, Haber DA, Boland G, Sade-Feldman M, Jenkins R, Hata A, Bardeesy N, Suva ML, Martin B, Liau B, Ott C, Rivera MN, Lawrence MS, Bar-Peled L. Takahashi M, et al. Among authors: brooijmans n. bioRxiv [Preprint]. 2023 Oct 23:2023.10.20.563287. doi: 10.1101/2023.10.20.563287. bioRxiv. 2023. PMID: 37961514 Free PMC article. Updated. Preprint.
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
STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts.
Buckbinder L, St Jean DJ Jr, Tieu T, Ladd B, Hilbert B, Wang W, Alltucker JT, Manimala S, Kryukov GV, Brooijmans N, Dowdell G, Jonsson P, Huff M, Guzman-Perez A, Jackson EL, Goncalves MD, Stuart DD. Buckbinder L, et al. Among authors: brooijmans n. Cancer Discov. 2023 Nov 1;13(11):2432-2447. doi: 10.1158/2159-8290.CD-23-0396. Cancer Discov. 2023. PMID: 37623743 Free PMC article.
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.
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
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.
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
43 results