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128 results

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Page 1
Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors.
Gonzalez-Lopez de Turiso F, Shin Y, Brown M, Cardozo M, Chen Y, Fong D, Hao X, He X, Henne K, Hu YL, Johnson MG, Kohn T, Lohman J, McBride HJ, McGee LR, Medina JC, Metz D, Miner K, Mohn D, Pattaropong V, Seganish J, Simard JL, Wannberg S, Whittington DA, Yu G, Cushing TD. Gonzalez-Lopez de Turiso F, et al. Among authors: henne k. J Med Chem. 2012 Sep 13;55(17):7667-85. doi: 10.1021/jm300679u. Epub 2012 Aug 29. J Med Chem. 2012. PMID: 22876881
Synthesis and SAR study of potent and selective PI3Kδ inhibitors.
Bui M, Hao X, Shin Y, Cardozo M, He X, Henne K, Suchomel J, McCarter J, McGee LR, San Miguel T, Medina JC, Mohn D, Tran T, Wannberg S, Wong J, Wong S, Zalameda L, Metz D, Cushing TD. Bui M, et al. Among authors: henne k. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1104-9. doi: 10.1016/j.bmcl.2015.01.001. Epub 2015 Jan 17. Bioorg Med Chem Lett. 2015. PMID: 25666823
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Shin Y, Suchomel J, Cardozo M, Duquette J, He X, Henne K, Hu YL, Kelly RC, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wong S, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Shin Y, et al. Among authors: henne k. J Med Chem. 2016 Jan 14;59(1):431-47. doi: 10.1021/acs.jmedchem.5b01651. Epub 2015 Dec 21. J Med Chem. 2016. PMID: 26652588
Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).
Gonzalez-Lopez de Turiso F, Hao X, Shin Y, Bui M, Campuzano ID, Cardozo M, Dunn MC, Duquette J, Fisher B, Foti RS, Henne K, He X, Hu YL, Kelly RC, Johnson MG, Lucas BS, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Gonzalez-Lopez de Turiso F, et al. Among authors: henne k. J Med Chem. 2016 Aug 11;59(15):7252-67. doi: 10.1021/acs.jmedchem.6b00827. Epub 2016 Jul 25. J Med Chem. 2016. PMID: 27411843
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F, He X, Henne KR, Hu YL, Hungate R, Johnson MG, Kelly RC, Lucas B, McCarter JD, McGee LR, Medina JC, San Miguel T, Mohn D, Pattaropong V, Pettus LH, Reichelt A, Rzasa RM, Seganish J, Tasker AS, Wahl RC, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang D, Metz DP. Cushing TD, et al. Among authors: henne kr. J Med Chem. 2015 Jan 8;58(1):480-511. doi: 10.1021/jm501624r. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25469863
Imidazo-pyrazine derivatives as potent CXCR3 antagonists.
Du X, Gustin DJ, Chen X, Duquette J, McGee LR, Wang Z, Ebsworth K, Henne K, Lemon B, Ma J, Miao S, Sabalan E, Sullivan TJ, Tonn G, Collins TL, Medina JC. Du X, et al. Among authors: henne k. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5200-4. doi: 10.1016/j.bmcl.2009.07.021. Epub 2009 Jul 9. Bioorg Med Chem Lett. 2009. PMID: 19631529
Discovery of potent and specific CXCR3 antagonists.
Chen X, Mihalic J, Deignan J, Gustin DJ, Duquette J, Du X, Chan J, Fu Z, Johnson M, Li AR, Henne K, Sullivan T, Lemon B, Ma J, Miao S, Tonn G, Collins T, Medina JC. Chen X, et al. Among authors: henne k. Bioorg Med Chem Lett. 2012 Jan 1;22(1):357-62. doi: 10.1016/j.bmcl.2011.10.120. Epub 2011 Nov 9. Bioorg Med Chem Lett. 2012. PMID: 22130135
Bioactivation of a novel 2-methylindole-containing dual chemoattractant receptor-homologous molecule expressed on T-helper type-2 cells/D-prostanoid receptor antagonist leads to mechanism-based CYP3A inactivation: glutathione adduct characterization and prediction of in vivo drug-drug interaction.
Wong SG, Fan PW, Subramanian R, Tonn GR, Henne KR, Johnson MG, Tadano Lohr M, Wong BK. Wong SG, et al. Among authors: henne kr. Drug Metab Dispos. 2010 May;38(5):841-50. doi: 10.1124/dmd.109.031344. Epub 2010 Jan 25. Drug Metab Dispos. 2010. PMID: 20100816
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
Henne KR, Tran TB, VandenBrink BM, Rock DA, Aidasani DK, Subramanian R, Mason AK, Stresser DM, Teffera Y, Wong SG, Johnson MG, Chen X, Tonn GR, Wong BK. Henne KR, et al. Drug Metab Dispos. 2012 Jul;40(7):1429-40. doi: 10.1124/dmd.112.045708. Epub 2012 Apr 19. Drug Metab Dispos. 2012. PMID: 22517972
Anti-PCSK9 antibody pharmacokinetics and low-density lipoprotein-cholesterol pharmacodynamics in nonhuman primates are antigen affinity-dependent and exhibit limited sensitivity to neonatal Fc receptor-binding enhancement.
Henne KR, Ason B, Howard M, Wang W, Sun J, Higbee J, Tang J, Matsuda KC, Xu R, Zhou L, Chan JC, King C, Piper DE, Ketchem RR, Michaels ML, Jackson SM, Retter MW. Henne KR, et al. J Pharmacol Exp Ther. 2015 Apr;353(1):119-31. doi: 10.1124/jpet.114.221242. Epub 2015 Feb 4. J Pharmacol Exp Ther. 2015. PMID: 25653417
128 results