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Page 1
Small-molecule inhibition of kinesin KIF18A reveals a mitotic vulnerability enriched in chromosomally unstable cancers.
Payton M, Belmontes B, Hanestad K, Moriguchi J, Chen K, McCarter JD, Chung G, Ninniri MS, Sun J, Manoukian R, Chambers S, Ho SM, Kurzeja RJM, Edson KZ, Dahal UP, Wu T, Wannberg S, Beltran PJ, Canon J, Boghossian AS, Rees MG, Ronan MM, Roth JA, Minocherhomji S, Bourbeau MP, Allen JR, Coxon A, Tamayo NA, Hughes PE. Payton M, et al. Among authors: bourbeau mp. Nat Cancer. 2024 Jan;5(1):66-84. doi: 10.1038/s43018-023-00699-5. Epub 2023 Dec 27. Nat Cancer. 2024. PMID: 38151625 Free PMC article.
AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients with MTAP-Deleted Cancers.
Belmontes B, Slemmons KK, Su C, Liu S, Policheni AN, Moriguchi J, Tan H, Xie F, Aiello DA, Yang Y, Lazaro R, Aeffner F, Rees MG, Ronan MM, Roth JA, Vestergaard M, Cowland S, Andersson J, Sarvary I, Chen Q, Sharma P, Lopez P, Tamayo N, Pettus LH, Ghimire-Rijal S, Mukund S, Allen JR, DeVoss J, Coxon A, Rodon J, Ghiringhelli F, Penel N, Prenen H, Glad S, Chuang CH, Keyvanjah K, Townsley DM, Butler JR, Bourbeau MP, Caenepeel S, Hughes PE. Belmontes B, et al. Among authors: bourbeau mp. Cancer Discov. 2025 Jan 13;15(1):139-161. doi: 10.1158/2159-8290.CD-24-0887. Cancer Discov. 2025. PMID: 39282709 Free PMC article.
Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe.
Tamayo NA, Bourbeau MP, Allen JR, Ashton KS, Chen JJ, Kaller MR, Nguyen TT, Nishimura N, Pettus LH, Walton M, Belmontes B, Moriguchi J, Chen K, McCarter JD, Hanestad K, Chung G, Ninniri MSS, Sun J, Poppe L, Spahr C, Hui J, Jia L, Wu T, Dahal UP, Edson KZ, Payton M. Tamayo NA, et al. Among authors: bourbeau mp. J Med Chem. 2022 Mar 24;65(6):4972-4990. doi: 10.1021/acs.jmedchem.1c02030. Epub 2022 Mar 14. J Med Chem. 2022. PMID: 35286090
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.
Frohn M, Liu L, Siegmund AC, Qian W, Amegadzie A, Chen N, Tan H, Hickman D, Wood S, Wen PH, Bartberger MD, Whittington DA, Allen JR, Bourbeau MP. Frohn M, et al. Among authors: bourbeau mp. Bioorg Med Chem Lett. 2020 Jul 15;30(14):127240. doi: 10.1016/j.bmcl.2020.127240. Epub 2020 May 4. Bioorg Med Chem Lett. 2020. PMID: 32527542
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
Pettus LH, Bourbeau MP, Bradley J, Bartberger MD, Chen K, Hickman D, Johnson M, Liu Q, Manning JR, Nanez A, Siegmund AC, Wen PH, Whittington DA, Allen JR, Wood S. Pettus LH, et al. Among authors: bourbeau mp. J Med Chem. 2020 Mar 12;63(5):2263-2281. doi: 10.1021/acs.jmedchem.9b01034. Epub 2019 Oct 18. J Med Chem. 2020. PMID: 31589043
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.
Pennington LD, Bartberger MD, Croghan MD, Andrews KL, Ashton KS, Bourbeau MP, Chen J, Chmait S, Cupples R, Fotsch C, Helmering J, Hong FT, Hungate RW, Jordan SR, Kong K, Liu L, Michelsen K, Moyer C, Nishimura N, Norman MH, Reichelt A, Siegmund AC, Sivits G, Tadesse S, Tegley CM, Van G, Yang KC, Yao G, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Pennington LD, et al. Among authors: bourbeau mp. J Med Chem. 2015 Dec 24;58(24):9663-79. doi: 10.1021/acs.jmedchem.5b01367. Epub 2015 Dec 1. J Med Chem. 2015. PMID: 26551034 Free article.
Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).
Hu E, Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR. Hu E, et al. Among authors: bourbeau mp. J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4. J Med Chem. 2014. PMID: 25062128
Nonracemic synthesis of GK-GKRP disruptor AMG-3969.
Bourbeau MP, Ashton KS, Yan J, St Jean DJ Jr. Bourbeau MP, et al. J Org Chem. 2014 Apr 18;79(8):3684-7. doi: 10.1021/jo500336e. Epub 2014 Apr 10. J Org Chem. 2014. PMID: 24678849
Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase.
Bourbeau MP, Siegmund A, Allen JG, Shu H, Fotsch C, Bartberger MD, Kim KW, Komorowski R, Graham M, Busby J, Wang M, Meyer J, Xu Y, Salyers K, Fielden M, Véniant MM, Gu W. Bourbeau MP, et al. J Med Chem. 2013 Dec 27;56(24):10132-41. doi: 10.1021/jm401601s. Epub 2013 Dec 11. J Med Chem. 2013. PMID: 24294923
20 results