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Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Su Q, Banks E, Bebernitz G, Bell K, Borenstein CF, Chen H, Chuaqui CE, Deng N, Ferguson AD, Kawatkar S, Grimster NP, Ruston L, Lyne PD, Read JA, Peng X, Pei X, Fawell S, Tang Z, Throner S, Vasbinder MM, Wang H, Winter-Holt J, Woessner R, Wu A, Yang W, Zinda M, Kettle JG. Su Q, et al. Among authors: fawell s. J Med Chem. 2020 May 14;63(9):4517-4527. doi: 10.1021/acs.jmedchem.9b01392. Epub 2020 Apr 28. J Med Chem. 2020. PMID: 32297743
The MET Inhibitor AZD6094 (Savolitinib, HMPL-504) Induces Regression in Papillary Renal Cell Carcinoma Patient-Derived Xenograft Models.
Schuller AG, Barry ER, Jones RD, Henry RE, Frigault MM, Beran G, Linsenmayer D, Hattersley M, Smith A, Wilson J, Cairo S, Déas O, Nicolle D, Adam A, Zinda M, Reimer C, Fawell SE, Clark EA, D'Cruz CM. Schuller AG, et al. Among authors: fawell se. Clin Cancer Res. 2015 Jun 15;21(12):2811-9. doi: 10.1158/1078-0432.CCR-14-2685. Epub 2015 Mar 16. Clin Cancer Res. 2015. PMID: 25779944
Effective combination therapies in preclinical endocrine resistant breast cancer models harboring ER mutations.
Ladd B, Mazzola AM, Bihani T, Lai Z, Bradford J, Collins M, Barry E, Goeppert AU, Weir HM, Hearne K, Renshaw JG, Mohseni M, Hurt E, Jalla S, Bao H, Hollingsworth R, Reimer C, Zinda M, Fawell S, D'Cruz CM. Ladd B, et al. Among authors: fawell s. Oncotarget. 2016 Aug 23;7(34):54120-54136. doi: 10.18632/oncotarget.10852. Oncotarget. 2016. PMID: 27472462 Free PMC article.
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: fawell se. 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: fawell se. 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. PLoS One. 2018 Jul 23;13(7):e0200826. doi: 10.1371/journal.pone.0200826. eCollection 2018. PLoS One. 2018. PMID: 30036377 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. 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: fawell s. 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
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.
Tron AE, Belmonte MA, Adam A, Aquila BM, Boise LH, Chiarparin E, Cidado J, Embrey KJ, Gangl E, Gibbons FD, Gregory GP, Hargreaves D, Hendricks JA, Johannes JW, Johnstone RW, Kazmirski SL, Kettle JG, Lamb ML, Matulis SM, Nooka AK, Packer MJ, Peng B, Rawlins PB, Robbins DW, Schuller AG, Su N, Yang W, Ye Q, Zheng X, Secrist JP, Clark EA, Wilson DM, Fawell SE, Hird AW. Tron AE, et al. Nat Commun. 2018 Dec 17;9(1):5341. doi: 10.1038/s41467-018-07551-w. Nat Commun. 2018. PMID: 30559424 Free PMC article.
82 results