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Page 1
Preclinical Characterization of a Next-Generation Brain Permeable, Paradox Breaker BRAF Inhibitor.
Wichmann J, Rynn C, Friess T, Petrig-Schaffland J, Kornacker M, Handl C, Emmenegger J, Eckmann J, Herting F, Frances N, Hunziker D, Krummenacher D, Rüttinger D, Ribeiro A, Bacac M, Brigo A, Hewings DS, Dummer R, Levesque MP, Schnetzler G, Martoglio B, Bischoff JR, Pettazzoni P. Wichmann J, et al. Among authors: bischoff jr. Clin Cancer Res. 2022 Feb 15;28(4):770-780. doi: 10.1158/1078-0432.CCR-21-2761. Clin Cancer Res. 2022. PMID: 34782366
Activity and Resistance of a Brain-Permeable Paradox Breaker BRAF Inhibitor in Melanoma Brain Metastasis.
Bonfill-Teixidor E, Iurlaro R, Handl C, Wichmann J, Arias A, Cuartas I, Emmenegger J, Romagnani A, Mangano L, Lorber T, Berrera M, Godfried Sie C, Köchl F, Eckmann J, Feddersen R, Kornacker M, Schnetzler G, Cicuendez M, Cordero E, Topczewski TE, Ferres-Pijoan A, González J, Martínez-Ricarte F, Muñoz-Couselo E, Tabernero J, Bischoff JR, Pettazzoni P, Seoane J. Bonfill-Teixidor E, et al. Among authors: bischoff jr. Cancer Res. 2022 Jul 18;82(14):2552-2564. doi: 10.1158/0008-5472.CAN-21-4152. Cancer Res. 2022. PMID: 35584009
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Obst-Sander U, Ricci A, Kuhn B, Friess T, Koldewey P, Kuglstatter A, Hewings D, Goergler A, Steiner S, Rueher D, Imhoff MP, Raschetti N, Marty HP, Dietzig A, Rynn C, Ehler A, Burger D, Kornacker M, Schaffland JP, Herting F, Pao W, Bischoff JR, Martoglio B, Alice Nagel Y, Jaeschke G. Obst-Sander U, et al. Among authors: bischoff jr. J Med Chem. 2022 Oct 13;65(19):13052-13073. doi: 10.1021/acs.jmedchem.2c00893. Epub 2022 Sep 30. J Med Chem. 2022. PMID: 36178776
DUSP4 protects BRAF- and NRAS-mutant melanoma from oncogene overdose through modulation of MITF.
Gutierrez-Prat N, Zuberer HL, Mangano L, Karimaddini Z, Wolf L, Tyanova S, Wellinger LC, Marbach D, Griesser V, Pettazzoni P, Bischoff JR, Rohle D, Palladino C, Vivanco I. Gutierrez-Prat N, et al. Among authors: bischoff jr. Life Sci Alliance. 2022 May 17;5(9):e202101235. doi: 10.26508/lsa.202101235. Print 2022 Sep. Life Sci Alliance. 2022. PMID: 35580987 Free PMC article.
Cellular Resistance Mechanisms to Targeted Protein Degradation Converge Toward Impairment of the Engaged Ubiquitin Transfer Pathway.
Ottis P, Palladino C, Thienger P, Britschgi A, Heichinger C, Berrera M, Julien-Laferriere A, Roudnicky F, Kam-Thong T, Bischoff JR, Martoglio B, Pettazzoni P. Ottis P, et al. Among authors: bischoff jr. ACS Chem Biol. 2019 Oct 18;14(10):2215-2223. doi: 10.1021/acschembio.9b00525. Epub 2019 Oct 8. ACS Chem Biol. 2019. PMID: 31553577
Discovery of JNJ-63576253, a Next-Generation Androgen Receptor Antagonist Active Against Wild-Type and Clinically Relevant Ligand Binding Domain Mutations in Metastatic Castration-Resistant Prostate Cancer.
Branch JR, Bush TL, Pande V, Connolly PJ, Zhang Z, Hickson I, Ondrus J, Jaensch S, Bischoff JR, Habineza G, Van Hecke G, Meerpoel L, Packman K, Parrett CJ, Chong YT, Gottardis MM, Bignan G. Branch JR, et al. Among authors: bischoff jr. Mol Cancer Ther. 2021 May;20(5):763-774. doi: 10.1158/1535-7163.MCT-20-0510. Epub 2021 Mar 1. Mol Cancer Ther. 2021. PMID: 33649102
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors.
Richters A, Doyle SK, Freeman DB, Lee C, Leifer BS, Jagannathan S, Kabinger F, Koren JV, Struntz NB, Urgiles J, Stagg RA, Curtin BH, Chatterjee D, Mathea S, Mikochik PJ, Hopkins TD, Gao H, Branch JR, Xin H, Westover L, Bignan GC, Rupnow BA, Karlin KL, Olson CM, Westbrook TF, Vacca J, Wilfong CM, Trotter BW, Saffran DC, Bischofberger N, Knapp S, Russo JW, Hickson I, Bischoff JR, Gottardis MM, Balk SP, Lin CY, Pop MS, Koehler AN. Richters A, et al. Among authors: bischoff jr. Cell Chem Biol. 2021 Feb 18;28(2):134-147.e14. doi: 10.1016/j.chembiol.2020.10.001. Epub 2020 Oct 20. Cell Chem Biol. 2021. PMID: 33086052 Free article.
Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition.
Blanco-Aparicio C, Collazo AM, Oyarzabal J, Leal JF, Albarán MI, Lima FR, Pequeño B, Ajenjo N, Becerra M, Alfonso P, Reymundo MI, Palacios I, Mateos G, Quiñones H, Corrionero A, Carnero A, Pevarello P, Lopez AR, Fominaya J, Pastor J, Bischoff JR. Blanco-Aparicio C, et al. Among authors: bischoff jr. Cancer Lett. 2011 Jan 28;300(2):145-53. doi: 10.1016/j.canlet.2010.09.016. Epub 2010 Nov 3. Cancer Lett. 2011. PMID: 21051136
Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
Martínez-González S, Rodríguez-Arístegui S, Gómez de la Oliva CA, Hernández AI, González Cantalapiedra E, Varela C, García AB, Rabal O, Oyarzabal J, Bischoff JR, Klett J, Albarrán MI, Cebriá A, Ajenjo N, García-Serelde B, Gómez-Casero E, Cuadrado-Urbano M, Cebrián D, Blanco-Aparicio C, Pastor J. Martínez-González S, et al. Among authors: bischoff jr. Eur J Med Chem. 2019 Apr 15;168:87-109. doi: 10.1016/j.ejmech.2019.02.022. Epub 2019 Feb 19. Eur J Med Chem. 2019. PMID: 30802730
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
Zhang Z, Connolly PJ, Lim HK, Pande V, Meerpoel L, Teleha C, Branch JR, Ondrus J, Hickson I, Bush T, Luistro L, Packman K, Bischoff JR, Ibrahim S, Parrett C, Chong Y, Gottardis MM, Bignan G. Zhang Z, et al. Among authors: bischoff jr. J Med Chem. 2021 Jan 28;64(2):909-924. doi: 10.1021/acs.jmedchem.0c01563. Epub 2021 Jan 20. J Med Chem. 2021. PMID: 33470111
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