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Page 1
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: bales kr. 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: bales kr. 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
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. 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.
Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione γ-secretase modulators.
Pettersson M, Johnson DS, Subramanyam C, Bales KR, am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, Navaratnam T, Sakya SM, Stiff CM, Tran TP, Xie L, Zhang L, Pustilnik LR, Vetelino BC, Wood KM, Pozdnyakov N, Verhoest PR, O'Donnell CJ. Pettersson M, et al. Among authors: bales kr. J Med Chem. 2014 Feb 13;57(3):1046-62. doi: 10.1021/jm401782h. Epub 2014 Jan 28. J Med Chem. 2014. PMID: 24428186
Class I HDAC inhibition is a novel pathway for regulating astrocytic apoE secretion.
Dresselhaus E, Duerr JM, Vincent F, Sylvain EK, Beyna M, Lanyon LF, LaChapelle E, Pettersson M, Bales KR, Ramaswamy G. Dresselhaus E, et al. Among authors: bales kr. PLoS One. 2018 Mar 26;13(3):e0194661. doi: 10.1371/journal.pone.0194661. eCollection 2018. PLoS One. 2018. PMID: 29579087 Free PMC article.
Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators.
Pettersson M, Johnson DS, Subramanyam C, Bales KR, am Ende CW, Fish BA, Green ME, Kauffman GW, Lira R, Mullins PB, Navaratnam T, Sakya SM, Stiff CM, Tran TP, Vetelino BC, Xie L, Zhang L, Pustilnik LR, Wood KM, O'Donnell CJ. Pettersson M, et al. Among authors: bales kr. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2906-11. doi: 10.1016/j.bmcl.2012.02.059. Epub 2012 Mar 1. Bioorg Med Chem Lett. 2012. PMID: 22429469
Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.
Pettersson M, Johnson DS, Humphrey JM, Butler TW, Am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, O'Donnell CJ, Stepan AF, Stiff CM, Subramanyam C, Tran TP, Vetelino BC, Yang E, Xie L, Bales KR, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR. Pettersson M, et al. Among authors: bales kr. ACS Med Chem Lett. 2015 Apr 3;6(5):596-601. doi: 10.1021/acsmedchemlett.5b00070. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005540 Free PMC article.
Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.
Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Evrard E, Efremov I, Kauffman GW, Stepan AF, Stiff CM, Xie L, Bales KR, Hajos-Korcsok E, Murrey HE, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR. Pettersson M, et al. Among authors: bales kr. Bioorg Med Chem Lett. 2015 Feb 15;25(4):908-13. doi: 10.1016/j.bmcl.2014.12.059. Epub 2014 Dec 25. Bioorg Med Chem Lett. 2015. PMID: 25582600
Development of clickable active site-directed photoaffinity probes for γ-secretase.
Crump CJ, am Ende CW, Ballard TE, Pozdnyakov N, Pettersson M, Chau DM, Bales KR, Li YM, Johnson DS. Crump CJ, et al. Among authors: bales kr. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2997-3000. doi: 10.1016/j.bmcl.2012.02.027. Epub 2012 Feb 20. Bioorg Med Chem Lett. 2012. PMID: 22418280 Free PMC article.
124 results