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Page 1
Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors.
Lu Y, Zhang L, Nolan CE, Becker SL, Atchison K, Robshaw AE, Pustilnik LR, Osgood SM, Miller EH, Stepan AF, Subramanyam C, Efremov I, Hallgren AJ, Riddell D. Lu Y, et al. Among authors: becker sl. J Pharmacol Exp Ther. 2011 Dec;339(3):922-34. doi: 10.1124/jpet.111.186791. Epub 2011 Sep 19. J Pharmacol Exp Ther. 2011. PMID: 21930801
Cerebrospinal fluid amyloid-β (Aβ) as an effect biomarker for brain Aβ lowering verified by quantitative preclinical analyses.
Lu Y, Riddell D, Hajos-Korcsok E, Bales K, Wood KM, Nolan CE, Robshaw AE, Zhang L, Leung L, Becker SL, Tseng E, Barricklow J, Miller EH, Osgood S, O'Neill BT, Brodney MA, Johnson DS, Pettersson M. Lu Y, et al. Among authors: becker sl. J Pharmacol Exp Ther. 2012 Aug;342(2):366-75. doi: 10.1124/jpet.112.192625. Epub 2012 May 4. J Pharmacol Exp Ther. 2012. PMID: 22562771 Free PMC article.
Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors.
Stepan AF, Karki K, McDonald WS, Dorff PH, Dutra JK, Dirico KJ, Won A, Subramanyam C, Efremov IV, O'Donnell CJ, Nolan CE, Becker SL, Pustilnik LR, Sneed B, Sun H, Lu Y, Robshaw AE, Riddell D, O'Sullivan TJ, Sibley E, Capetta S, Atchison K, Hallgren AJ, Miller E, Wood A, Obach RS. Stepan AF, et al. Among authors: becker sl. J Med Chem. 2011 Nov 24;54(22):7772-83. doi: 10.1021/jm200893p. Epub 2011 Oct 26. J Med Chem. 2011. PMID: 21995460
Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor.
Stepan AF, Subramanyam C, Efremov IV, Dutra JK, O'Sullivan TJ, DiRico KJ, McDonald WS, Won A, Dorff PH, Nolan CE, Becker SL, Pustilnik LR, Riddell DR, Kauffman GW, Kormos BL, Zhang L, Lu Y, Capetta SH, Green ME, Karki K, Sibley E, Atchison KP, Hallgren AJ, Oborski CE, Robshaw AE, Sneed B, O'Donnell CJ. Stepan AF, et al. Among authors: becker sl. J Med Chem. 2012 Apr 12;55(7):3414-24. doi: 10.1021/jm300094u. Epub 2012 Mar 29. J Med Chem. 2012. PMID: 22420884
Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014.
Lanz TA, Wood KM, Richter KE, Nolan CE, Becker SL, Pozdnyakov N, Martin BA, Du P, Oborski CE, Wood DE, Brown TM, Finley JE, Sokolowski SA, Hicks CD, Coffman KJ, Geoghegan KF, Brodney MA, Liston D, Tate B. Lanz TA, et al. Among authors: becker sl. J Pharmacol Exp Ther. 2010 Jul;334(1):269-77. doi: 10.1124/jpet.110.167379. Epub 2010 Apr 2. J Pharmacol Exp Ther. 2010. PMID: 20363853
Diamide amino-imidazoles: a novel series of γ-secretase inhibitors for the treatment of Alzheimer's disease.
Brodney MA, Auperin DD, Becker SL, Bronk BS, Brown TM, Coffman KJ, Finley JE, Hicks CD, Karmilowicz MJ, Lanz TA, Liston D, Liu X, Martin BA, Nelson RB, Nolan CE, Oborski CE, Parker CP, Richter KE, Pozdnyakov N, Sahagan BG, Schachter JB, Sokolowski SA, Tate B, Van Deusen JW, Wood DE, Wood KM. Brodney MA, et al. Among authors: becker sl. Bioorg Med Chem Lett. 2011 May 1;21(9):2631-6. doi: 10.1016/j.bmcl.2010.12.117. Epub 2010 Dec 30. Bioorg Med Chem Lett. 2011. PMID: 21269825
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014.
Brodney MA, Auperin DD, Becker SL, Bronk BS, Brown TM, Coffman KJ, Finley JE, Hicks CD, Karmilowicz MJ, Lanz TA, Liston D, Liu X, Martin BA, Nelson RB, Nolan CE, Oborski CE, Parker CP, Richter KE, Pozdnyakov N, Sahagan BG, Schachter JB, Sokolowski SA, Tate B, Wood DE, Wood KM, Van Deusen JW, Zhang L. Brodney MA, et al. Among authors: becker sl. Bioorg Med Chem Lett. 2011 May 1;21(9):2637-40. doi: 10.1016/j.bmcl.2010.12.118. Epub 2010 Dec 30. Bioorg Med Chem Lett. 2011. PMID: 21269827
Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding.
Liu X, Smith BJ, Chen C, Callegari E, Becker SL, Chen X, Cianfrogna J, Doran AC, Doran SD, Gibbs JP, Hosea N, Liu J, Nelson FR, Szewc MA, Van Deusen J. Liu X, et al. Among authors: becker sl. J Pharmacol Exp Ther. 2005 Jun;313(3):1254-62. doi: 10.1124/jpet.104.079319. Epub 2005 Mar 2. J Pharmacol Exp Ther. 2005. PMID: 15743928
253 results