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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: nolan ce. 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: nolan ce. 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.
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: nolan ce. 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
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: nolan ce. 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: nolan ce. J Med Chem. 2012 Apr 12;55(7):3414-24. doi: 10.1021/jm300094u. Epub 2012 Mar 29. J Med Chem. 2012. PMID: 22420884
Spirocyclic sulfamides as β-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors.
Brodney MA, Barreiro G, Ogilvie K, Hajos-Korcsok E, Murray J, Vajdos F, Ambroise C, Christoffersen C, Fisher K, Lanyon L, Liu J, Nolan CE, Withka JM, Borzilleri KA, Efremov I, Oborski CE, Varghese A, O'Neill BT. Brodney MA, et al. Among authors: nolan ce. J Med Chem. 2012 Nov 8;55(21):9224-39. doi: 10.1021/jm3009426. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 22984865
Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of β-secretase inhibitors.
Zuhl AM, Nolan CE, Brodney MA, Niessen S, Atchison K, Houle C, Karanian DA, Ambroise C, Brulet JW, Beck EM, Doran SD, O'Neill BT, Am Ende CW, Chang C, Geoghegan KF, West GM, Judkins JC, Hou X, Riddell DR, Johnson DS. Zuhl AM, et al. Among authors: nolan ce. Nat Commun. 2016 Oct 11;7:13042. doi: 10.1038/ncomms13042. Nat Commun. 2016. PMID: 27727204 Free PMC article.
Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain.
Zhang L, Chen L, Dutra JK, Beck EM, Nag S, Takano A, Amini N, Arakawa R, Brodney MA, Buzon LM, Doran SD, Lanyon LF, McCarthy TJ, Bales KR, Nolan CE, O'Neill BT, Schildknegt K, Halldin C, Villalobos A. Zhang L, et al. Among authors: nolan ce. J Med Chem. 2018 Apr 26;61(8):3296-3308. doi: 10.1021/acs.jmedchem.7b01769. Epub 2018 Feb 2. J Med Chem. 2018. PMID: 29356535
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
O'Neill BT, Beck EM, Butler CR, Nolan CE, Gonzales C, Zhang L, Doran SD, Lapham K, Buzon LM, Dutra JK, Barreiro G, Hou X, Martinez-Alsina LA, Rogers BN, Villalobos A, Murray JC, Ogilvie K, LaChapelle EA, Chang C, Lanyon LF, Steppan CM, Robshaw A, Hales K, Boucher GG, Pandher K, Houle C, Ambroise CW, Karanian D, Riddell D, Bales KR, Brodney MA. O'Neill BT, et al. Among authors: nolan ce. J Med Chem. 2018 May 24;61(10):4476-4504. doi: 10.1021/acs.jmedchem.8b00246. Epub 2018 Apr 17. J Med Chem. 2018. PMID: 29613789
41 results