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12 results

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Page 1
Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.
Hu E, Ma J, Biorn C, Lester-Zeiner D, Cho R, Rumfelt S, Kunz RK, Nixey T, Michelsen K, Miller S, Shi J, Wong J, Hill Della Puppa G, Able J, Talreja S, Hwang DR, Hitchcock SA, Porter A, Immke D, Allen JR, Treanor J, Chen H. Hu E, et al. Among authors: lester zeiner d. J Med Chem. 2012 May 24;55(10):4776-87. doi: 10.1021/jm3002372. Epub 2012 May 11. J Med Chem. 2012. PMID: 22548439
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).
Hu E, Kunz RK, Chen N, Rumfelt S, Siegmund A, Andrews K, Chmait S, Zhao S, Davis C, Chen H, Lester-Zeiner D, Ma J, Biorn C, Shi J, Porter A, Treanor J, Allen JR. Hu E, et al. Among authors: lester zeiner d. J Med Chem. 2013 Nov 14;56(21):8781-92. doi: 10.1021/jm401234w. Epub 2013 Oct 25. J Med Chem. 2013. PMID: 24102193
Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).
Hu E, Andrews K, Chmait S, Zhao X, Davis C, Miller S, Hill Della Puppa G, Dovlatyan M, Chen H, Lester-Zeiner D, Able J, Biorn C, Ma J, Shi J, Treanor J, Allen JR. Hu E, et al. Among authors: lester zeiner d. ACS Med Chem Lett. 2014 Mar 28;5(6):700-5. doi: 10.1021/ml5000993. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944747 Free PMC 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: lester zeiner d. J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4. J Med Chem. 2014. PMID: 25062128
AMG 580: a novel small molecule phosphodiesterase 10A (PDE10A) positron emission tomography tracer.
Chen H, Lester-Zeiner D, Shi J, Miller S, Glaus C, Hu E, Chen N, Able J, Biorn C, Wong J, Ma J, Michelsen K, Hill Della Puppa G, Kazules T, Dou HH, Talreja S, Zhao X, Chen A, Rumfelt S, Kunz RK, Ye H, Thiel OR, Williamson T, Davis C, Porter A, Immke D, Allen JR, Treanor J. Chen H, et al. Among authors: lester zeiner d. J Pharmacol Exp Ther. 2015 Feb;352(2):327-37. doi: 10.1124/jpet.114.220517. Epub 2014 Dec 11. J Pharmacol Exp Ther. 2015. PMID: 25502803
Discovery of Phosphodiesterase 10A (PDE10A) PET Tracer AMG 580 to Support Clinical Studies.
Hu E, Chen N, Kunz RK, Hwang DR, Michelsen K, Davis C, Ma J, Shi J, Lester-Zeiner D, Hungate R, Treanor J, Chen H, Allen JR. Hu E, et al. Among authors: lester zeiner d. ACS Med Chem Lett. 2016 May 19;7(7):719-23. doi: 10.1021/acsmedchemlett.6b00185. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437084 Free PMC article.
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
Gustin DJ, Ma Z, Min X, Li Y, Hedberg C, Guimaraes C, Porter AC, Lindstrom M, Lester-Zeiner D, Xu G, Carlson TJ, Xiao S, Meleza C, Connors R, Wang Z, Kayser F. Gustin DJ, et al. Among authors: lester zeiner d. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2492-6. doi: 10.1016/j.bmcl.2011.02.052. Epub 2011 Feb 17. Bioorg Med Chem Lett. 2011. PMID: 21392988
Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.
D'Amico DC, Aya T, Human J, Fotsch C, Chen JJ, Biswas K, Riahi B, Norman MH, Willoughby CA, Hungate R, Reider PJ, Biddlecome G, Lester-Zeiner D, Staden CV, Johnson E, Kamassah A, Arik L, Wang J, Viswanadhan VN, Groneberg RD, Zhan J, Suzuki H, Toro A, Mareska DA, Clarke DE, Harvey DM, Burgess LE, Laird ER, Askew B, Ng G. D'Amico DC, et al. J Med Chem. 2007 Feb 22;50(4):607-10. doi: 10.1021/jm061224g. Epub 2007 Jan 23. J Med Chem. 2007. PMID: 17243660
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Biswas K, Li A, Chen JJ, D'Amico DC, Fotsch C, Han N, Human J, Liu Q, Norman MH, Riahi B, Yuan C, Suzuki H, Mareska DA, Zhan J, Clarke DE, Toro A, Groneberg RD, Burgess LE, Lester-Zeiner D, Biddlecome G, Manning BH, Arik L, Dong H, Huang M, Kamassah A, Loeloff R, Sun H, Hsieh FY, Kumar G, Ng GY, Hungate RW, Askew BC, Johnson E. Biswas K, et al. Among authors: lester zeiner d. J Med Chem. 2007 May 3;50(9):2200-12. doi: 10.1021/jm070055c. Epub 2007 Apr 5. J Med Chem. 2007. PMID: 17408249
Aryl sulfones as novel bradykinin B1 receptor antagonists for treatment of chronic pain.
Biswas K, Aya T, Qian W, Peterkin TA, Chen JJ, Human J, Hungate RW, Kumar G, Arik L, Lester-Zeiner D, Biddlecome G, Manning BH, Sun H, Dong H, Huang M, Loeloff R, Johnson EJ, Askew BC. Biswas K, et al. Among authors: lester zeiner d. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4764-9. doi: 10.1016/j.bmcl.2008.07.108. Epub 2008 Jul 31. Bioorg Med Chem Lett. 2008. PMID: 18706809
12 results