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Page 1
Optimization of a Novel DEL Hit That Binds in the Cbl-b SH2 Domain and Blocks Substrate Binding.
Liang J, Lambrecht MJ, Arenzana TL, Aubert-Nicol S, Bao L, Broccatelli F, Cai J, Eidenschenk C, Everett C, Garner T, Gruber F, Haghshenas P, Huestis MP, Hsu PL, Kou P, Jakalian A, Larouche-Gauthier R, Leclerc JP, Leung DH, Martin A, Murray J, Prangley M, Rutz S, Kakiuchi-Kiyota S, Satz AL, Skelton NJ, Steffek M, Stoffler D, Sudhamsu J, Tan S, Wang J, Wang S, Wang Q, Wendorff TJ, Wichert M, Yadav A, Yu C, Wang X. Liang J, et al. Among authors: jakalian a. ACS Med Chem Lett. 2024 May 29;15(6):864-872. doi: 10.1021/acsmedchemlett.4c00068. eCollection 2024 Jun 13. ACS Med Chem Lett. 2024. PMID: 38894924
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP. Bronner SM, et al. Among authors: jakalian a. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2294-2301. doi: 10.1016/j.bmcl.2019.06.021. Epub 2019 Jun 26. Bioorg Med Chem Lett. 2019. PMID: 31307887
Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.
Fader LD, Bailey M, Beaulieu E, Bilodeau F, Bonneau P, Bousquet Y, Carson RJ, Chabot C, Coulombe R, Duan J, Fenwick C, Garneau M, Halmos T, Jakalian A, James C, Kawai SH, Landry S, LaPlante SR, Mason SW, Morin S, Rioux N, Simoneau B, Surprenant S, Thavonekham B, Thibeault C, Trinh T, Tsantrizos Y, Tsoung J, Yoakim C, Wernic D. Fader LD, et al. Among authors: jakalian a. ACS Med Chem Lett. 2016 Jun 9;7(8):797-801. doi: 10.1021/acsmedchemlett.6b00194. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563405 Free PMC article.
Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.
Fader LD, Malenfant E, Parisien M, Carson R, Bilodeau F, Landry S, Pesant M, Brochu C, Morin S, Chabot C, Halmos T, Bousquet Y, Bailey MD, Kawai SH, Coulombe R, LaPlante S, Jakalian A, Bhardwaj PK, Wernic D, Schroeder P, Amad M, Edwards P, Garneau M, Duan J, Cordingley M, Bethell R, Mason SW, Bös M, Bonneau P, Poupart MA, Faucher AM, Simoneau B, Fenwick C, Yoakim C, Tsantrizos Y. Fader LD, et al. Among authors: jakalian a. ACS Med Chem Lett. 2014 Jan 22;5(4):422-7. doi: 10.1021/ml500002n. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900852 Free PMC article.
Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.
Fader LD, Carson R, Morin S, Bilodeau F, Chabot C, Halmos T, Bailey MD, Kawai SH, Coulombe R, Laplante S, Mekhssian K, Jakalian A, Garneau M, Duan J, Mason SW, Simoneau B, Fenwick C, Tsantrizos Y, Yoakim C. Fader LD, et al. Among authors: jakalian a. ACS Med Chem Lett. 2014 Apr 16;5(6):711-6. doi: 10.1021/ml500110j. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944749 Free PMC article.
Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: discovery of deleobuvir (BI 207127).
LaPlante SR, Bös M, Brochu C, Chabot C, Coulombe R, Gillard JR, Jakalian A, Poirier M, Rancourt J, Stammers T, Thavonekham B, Beaulieu PL, Kukolj G, Tsantrizos YS. LaPlante SR, et al. Among authors: jakalian a. J Med Chem. 2014 Mar 13;57(5):1845-54. doi: 10.1021/jm4011862. Epub 2013 Nov 11. J Med Chem. 2014. PMID: 24159919
Anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors with sub-micromolar potency in the cell-based replicon assay.
Stammers TA, Coulombe R, Duplessis M, Fazal G, Gagnon A, Garneau M, Goulet S, Jakalian A, LaPlante S, Rancourt J, Thavonekham B, Wernic D, Kukolj G, Beaulieu PL. Stammers TA, et al. Among authors: jakalian a. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6879-85. doi: 10.1016/j.bmcl.2013.09.102. Epub 2013 Oct 8. Bioorg Med Chem Lett. 2013. PMID: 24176401
27 results