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Page 1
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: pettus lh. Cancer Discov. 2024 Sep 16. doi: 10.1158/2159-8290.CD-24-0887. Online ahead of print. Cancer Discov. 2024. PMID: 39282709
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: pettus lh. 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
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Norman MH, Andrews KL, Bo YY, Booker SK, Caenepeel S, Cee VJ, D'Angelo ND, Freeman DJ, Herberich BJ, Hong FT, Jackson CL, Jiang J, Lanman BA, Liu L, McCarter JD, Mullady EL, Nishimura N, Pettus LH, Reed AB, Miguel TS, Smith AL, Stec MM, Tadesse S, Tasker A, Aidasani D, Zhu X, Subramanian R, Tamayo NA, Wang L, Whittington DA, Wu B, Wu T, Wurz RP, Yang K, Zalameda L, Zhang N, Hughes PE. Norman MH, et al. Among authors: pettus lh. J Med Chem. 2012 Sep 13;55(17):7796-816. doi: 10.1021/jm300846z. Epub 2012 Aug 30. J Med Chem. 2012. PMID: 22897589
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.
Smith AL, D'Angelo ND, Bo YY, Booker SK, Cee VJ, Herberich B, Hong FT, Jackson CL, Lanman BA, Liu L, Nishimura N, Pettus LH, Reed AB, Tadesse S, Tamayo NA, Wurz RP, Yang K, Andrews KL, Whittington DA, McCarter JD, Miguel TS, Zalameda L, Jiang J, Subramanian R, Mullady EL, Caenepeel S, Freeman DJ, Wang L, Zhang N, Wu T, Hughes PE, Norman MH. Smith AL, et al. Among authors: pettus lh. J Med Chem. 2012 Jun 14;55(11):5188-219. doi: 10.1021/jm300184s. Epub 2012 May 23. J Med Chem. 2012. PMID: 22548365
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.
Wurz RP, Liu L, Yang K, Nishimura N, Bo Y, Pettus LH, Caenepeel S, Freeman DJ, McCarter JD, Mullady EL, Miguel TS, Wang L, Zhang N, Andrews KL, Whittington DA, Jiang J, Subramanian R, Hughes PE, Norman MH. Wurz RP, et al. Among authors: pettus lh. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5714-20. doi: 10.1016/j.bmcl.2012.06.078. Epub 2012 Jul 3. Bioorg Med Chem Lett. 2012. PMID: 22832322
Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.
Lanman BA, Reed AB, Cee VJ, Hong FT, Pettus LH, Wurz RP, Andrews KL, Jiang J, McCarter JD, Mullady EL, San Miguel T, Subramanian R, Wang L, Whittington DA, Wu T, Zalameda L, Zhang N, Tasker AS, Hughes PE, Norman MH. Lanman BA, et al. Among authors: pettus lh. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5630-5634. doi: 10.1016/j.bmcl.2014.10.085. Epub 2014 Nov 1. Bioorg Med Chem Lett. 2014. PMID: 25466188
Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
Pettus LH, Andrews KL, Booker SK, Chen J, Cee VJ, Chavez F Jr, Chen Y, Eastwood H, Guerrero N, Herberich B, Hickman D, Lanman BA, Laszlo J 3rd, Lee MR, Lipford JR, Mattson B, Mohr C, Nguyen Y, Norman MH, Powers D, Reed AB, Rex K, Sastri C, Tamayo N, Wang P, Winston JT, Wu B, Wu T, Wurz RP, Xu Y, Zhou Y, Tasker AS, Wang HL. Pettus LH, et al. J Med Chem. 2016 Jul 14;59(13):6407-30. doi: 10.1021/acs.jmedchem.6b00610. Epub 2016 Jun 22. J Med Chem. 2016. PMID: 27285051
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. 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 Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.
Cee VJ, Chavez F Jr, Herberich B, Lanman BA, Pettus LH, Reed AB, Wu B, Wurz RP, Andrews KL, Chen J, Hickman D, Laszlo J 3rd, Lee MR, Guerrero N, Mattson BK, Nguyen Y, Mohr C, Rex K, Sastri CE, Wang P, Wu Q, Wu T, Xu Y, Zhou Y, Winston JT, Lipford JR, Tasker AS, Wang HL. Cee VJ, et al. Among authors: pettus lh. ACS Med Chem Lett. 2016 Feb 12;7(4):408-12. doi: 10.1021/acsmedchemlett.5b00403. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096050 Free PMC article.
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Doherty EM, Fotsch C, Bannon AW, Bo Y, Chen N, Dominguez C, Falsey J, Gavva NR, Katon J, Nixey T, Ognyanov VI, Pettus L, Rzasa RM, Stec M, Surapaneni S, Tamir R, Zhu J, Treanor JJ, Norman MH. Doherty EM, et al. J Med Chem. 2007 Jul 26;50(15):3515-27. doi: 10.1021/jm070190p. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585750
26 results