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BRD4 Inhibition Is Synthetic Lethal with PARP Inhibitors through the Induction of Homologous Recombination Deficiency.
Sun C, Yin J, Fang Y, Chen J, Jeong KJ, Chen X, Vellano CP, Ju Z, Zhao W, Zhang D, Lu Y, Meric-Bernstam F, Yap TA, Hattersley M, O'Connor MJ, Chen H, Fawell S, Lin SY, Peng G, Mills GB. Sun C, et al. Among authors: chen j, chen x, chen h. Cancer Cell. 2018 Mar 12;33(3):401-416.e8. doi: 10.1016/j.ccell.2018.01.019. Cancer Cell. 2018. PMID: 29533782 Free PMC article.
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).
Bradbury RH, Callis R, Carr GR, Chen H, Clark E, Feron L, Glossop S, Graham MA, Hattersley M, Jones C, Lamont SG, Ouvry G, Patel A, Patel J, Rabow AA, Roberts CA, Stokes S, Stratton N, Walker GE, Ward L, Whalley D, Whittaker D, Wrigley G, Waring MJ. Bradbury RH, et al. Among authors: chen h. J Med Chem. 2016 Sep 8;59(17):7801-17. doi: 10.1021/acs.jmedchem.6b00070. Epub 2016 Aug 24. J Med Chem. 2016. PMID: 27528113
AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies.
Rhyasen GW, Hattersley MM, Yao Y, Dulak A, Wang W, Petteruti P, Dale IL, Boiko S, Cheung T, Zhang J, Wen S, Castriotta L, Lawson D, Collins M, Bao L, Ahdesmaki MJ, Walker G, O'Connor G, Yeh TC, Rabow AA, Dry JR, Reimer C, Lyne P, Mills GB, Fawell SE, Waring MJ, Zinda M, Clark E, Chen H. Rhyasen GW, et al. Among authors: chen h. Mol Cancer Ther. 2016 Nov;15(11):2563-2574. doi: 10.1158/1535-7163.MCT-16-0141. Epub 2016 Aug 29. Mol Cancer Ther. 2016. PMID: 27573426
BRD4 facilitates replication stress-induced DNA damage response.
Zhang J, Dulak AM, Hattersley MM, Willis BS, Nikkilä J, Wang A, Lau A, Reimer C, Zinda M, Fawell SE, Mills GB, Chen H. Zhang J, et al. Among authors: chen h. Oncogene. 2018 Jul;37(28):3763-3777. doi: 10.1038/s41388-018-0194-3. Epub 2018 Apr 11. Oncogene. 2018. PMID: 29636547 Free PMC article.
BRD4 amplification facilitates an oncogenic gene expression program in high-grade serous ovarian cancer and confers sensitivity to BET inhibitors.
Rhyasen GW, Yao Y, Zhang J, Dulak A, Castriotta L, Jacques K, Zhao W, Gharahdaghi F, Hattersley MM, Lyne PD, Clark E, Zinda M, Fawell SE, Mills GB, Chen H. Rhyasen GW, et al. Among authors: chen h. PLoS One. 2018 Jul 23;13(7):e0200826. doi: 10.1371/journal.pone.0200826. eCollection 2018. PLoS One. 2018. PMID: 30036377 Free PMC article.
BET Bromodomain Inhibition Cooperates with PD-1 Blockade to Facilitate Antitumor Response in Kras-Mutant Non-Small Cell Lung Cancer.
Adeegbe DO, Liu S, Hattersley MM, Bowden M, Zhou CW, Li S, Vlahos R, Grondine M, Dolgalev I, Ivanova EV, Quinn MM, Gao P, Hammerman PS, Bradner JE, Diehl JA, Rustgi AK, Bass AJ, Tsirigos A, Freeman GJ, Chen H, Wong KK. Adeegbe DO, et al. Among authors: chen h. Cancer Immunol Res. 2018 Oct;6(10):1234-1245. doi: 10.1158/2326-6066.CIR-18-0077. Epub 2018 Aug 7. Cancer Immunol Res. 2018. PMID: 30087114 Free PMC article.
Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer.
Wang Z, Grosskurth SE, Cheung T, Petteruti P, Zhang J, Wang X, Wang W, Gharahdaghi F, Wu J, Su N, Howard RT, Mayo M, Widzowski D, Scott DA, Johannes JW, Lamb ML, Lawson D, Dry JR, Lyne PD, Tate EW, Zinda M, Mikule K, Fawell SE, Reimer C, Chen H. Wang Z, et al. Among authors: chen h. Cancer Res. 2018 Dec 1;78(23):6691-6702. doi: 10.1158/0008-5472.CAN-18-1362. Epub 2018 Oct 8. Cancer Res. 2018. PMID: 30297535 Free article.
Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.
McCoull W, Cheung T, Anderson E, Barton P, Burgess J, Byth K, Cao Q, Castaldi MP, Chen H, Chiarparin E, Carbajo RJ, Code E, Cowan S, Davey PR, Ferguson AD, Fillery S, Fuller NO, Gao N, Hargreaves D, Howard MR, Hu J, Kawatkar A, Kemmitt PD, Leo E, Molina DM, O'Connell N, Petteruti P, Rasmusson T, Raubo P, Rawlins PB, Ricchiuto P, Robb GR, Schenone M, Waring MJ, Zinda M, Fawell S, Wilson DM. McCoull W, et al. Among authors: chen h. ACS Chem Biol. 2018 Nov 16;13(11):3131-3141. doi: 10.1021/acschembio.8b00698. Epub 2018 Oct 17. ACS Chem Biol. 2018. PMID: 30335946
The landscape of therapeutic vulnerabilities in EGFR inhibitor osimertinib drug tolerant persister cells.
Criscione SW, Martin MJ, Oien DB, Gorthi A, Miragaia RJ, Zhang J, Chen H, Karl DL, Mendler K, Markovets A, Gagrica S, Delpuech O, Dry JR, Grondine M, Hattersley MM, Urosevic J, Floc'h N, Drew L, Yao Y, Smith PD. Criscione SW, et al. Among authors: chen h. NPJ Precis Oncol. 2022 Dec 27;6(1):95. doi: 10.1038/s41698-022-00337-w. NPJ Precis Oncol. 2022. PMID: 36575215 Free PMC article.
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