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Page 1
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.
René O, Fauber BP, Boenig Gde L, Burton B, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, Kiefer JR, Liimatta M, Lockey P, Norman M, Ouyang W, Wallweber HA, Wong H. René O, et al. Among authors: wallweber ha. ACS Med Chem Lett. 2014 Dec 4;6(3):276-81. doi: 10.1021/ml500420y. eCollection 2015 Mar 12. ACS Med Chem Lett. 2014. PMID: 25815138 Free PMC article.
Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.
Hu H, Wang X, Chan GK, Chang JH, Do S, Drummond J, Ebens A, Lee W, Ly J, Lyssikatos JP, Murray J, Moffat JG, Chao Q, Tsui V, Wallweber H, Kolesnikov A. Hu H, et al. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5258-64. doi: 10.1016/j.bmcl.2015.09.052. Epub 2015 Sep 30. Bioorg Med Chem Lett. 2015. PMID: 26459208
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.
Beveridge RE, Wallweber HA, Ashkenazi A, Beresini M, Clark KR, Gibbons P, Ghiro E, Kaufman S, Larivée A, Leblanc M, Leclerc JP, Lemire A, Ly C, Rudolph J, Schwarz JB, Srivastava S, Wang W, Zhao L, Braun MG. Beveridge RE, et al. Among authors: wallweber ha. ACS Med Chem Lett. 2020 Oct 16;11(12):2389-2396. doi: 10.1021/acsmedchemlett.0c00344. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335661 Free PMC article.
Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model.
Braun MG, Ashkenazi A, Beveridge RE, Castanedo G, Wallweber HA, Beresini MH, Clark KR, De Bruyn T, Fu L, Gibbons P, Jiang F, Kaufman S, Kan D, Kiefer JR, Leclerc JP, Lemire A, Ly C, Segal E, Sims J, Wang W, Wei W, Zhao L, Schwarz JB, Rudolph J. Braun MG, et al. Among authors: wallweber ha. J Med Chem. 2024 Jun 13;67(11):8708-8729. doi: 10.1021/acs.jmedchem.3c02425. Epub 2024 May 15. J Med Chem. 2024. PMID: 38748820
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Wang X, Blackaby W, Allen V, Chan GKY, Chang JH, Chiang PC, Diène C, Drummond J, Do S, Fan E, Harstad EB, Hodges A, Hu H, Jia W, Kofie W, Kolesnikov A, Lyssikatos JP, Ly J, Matteucci M, Moffat JG, Munugalavadla V, Murray J, Nash D, Noland CL, Del Rosario G, Ross L, Rouse C, Sharpe A, Slaga D, Sun M, Tsui V, Wallweber H, Yu SF, Ebens AJ. Wang X, et al. J Med Chem. 2019 Feb 28;62(4):2140-2153. doi: 10.1021/acs.jmedchem.8b01857. Epub 2019 Feb 20. J Med Chem. 2019. PMID: 30715878
A BCMA/CD16A bispecific innate cell engager for the treatment of multiple myeloma.
Kakiuchi-Kiyota S, Ross T, Wallweber HA, Kiefer JR, Schutten MM, Adedeji AO, Cai H, Hendricks R, Cohen S, Myneni S, Liu L, Fullerton A, Corr N, Yu L, de Almeida Nagata D, Zhong S, Leong SR, Li J, Nakamura R, Sumiyoshi T, Li J, Ovacik AM, Zheng B, Dillon M, Spiess C, Wingert S, Rajkovic E, Ellwanger K, Reusch U, Polson AG. Kakiuchi-Kiyota S, et al. Among authors: wallweber ha. Leukemia. 2022 Apr;36(4):1006-1014. doi: 10.1038/s41375-021-01478-w. Epub 2022 Jan 10. Leukemia. 2022. PMID: 35001074
Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands.
Ferri E, Le Thomas A, Wallweber HA, Day ES, Walters BT, Kaufman SE, Braun MG, Clark KR, Beresini MH, Mortara K, Chen YA, Canter B, Phung W, Liu PS, Lammens A, Ashkenazi A, Rudolph J, Wang W. Ferri E, et al. Among authors: wallweber ha. Nat Commun. 2020 Dec 14;11(1):6387. doi: 10.1038/s41467-020-19974-5. Nat Commun. 2020. PMID: 33318494 Free PMC article.
Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors.
Hu DX, Patel S, Chen H, Wang S, Staben ST, Dimitrova YN, Wallweber HA, Lee JY, Chan GKY, Sneeringer CJ, Prangley MS, Moffat JG, Wu KC, Schutt LK, Salphati L, Pang J, McNamara E, Huang H, Chen Y, Wang Y, Zhao W, Lim J, Murthy A, Siu M. Hu DX, et al. Among authors: wallweber ha. J Med Chem. 2022 Sep 8;65(17):11500-11512. doi: 10.1021/acs.jmedchem.1c01180. Epub 2021 Nov 15. J Med Chem. 2022. PMID: 34779204
13 results