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Quantitative Analysis of 18F-PF-06684511, a Novel PET Radioligand for Selective β-Secretase 1 Imaging, in Nonhuman Primate Brain.
Takano A, Chen L, Nag S, Brodney MA, Arakawa R, Chang C, Amini N, Doran SD, Dutra JK, McCarthy TJ, Nolan CE, O'Neill BT, Villalobos A, Zhang L, Halldin C. Takano A, et al. Among authors: chang c. J Nucl Med. 2019 Jul;60(7):992-997. doi: 10.2967/jnumed.118.217372. Epub 2018 Dec 7. J Nucl Med. 2019. PMID: 30530832 Free article.
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: chang c. Nat Commun. 2016 Oct 11;7:13042. doi: 10.1038/ncomms13042. Nat Commun. 2016. PMID: 27727204 Free PMC article.
Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors.
Wager TT, Galatsis P, Chandrasekaran RY, Butler TW, Li J, Zhang L, Mente S, Subramanyam C, Liu S, Doran AC, Chang C, Fisher K, Grimwood S, Hedde JR, Marconi M, Schildknegt K. Wager TT, et al. Among authors: chang c. ACS Chem Neurosci. 2017 Sep 20;8(9):1995-2004. doi: 10.1021/acschemneuro.7b00155. Epub 2017 Jun 30. ACS Chem Neurosci. 2017. PMID: 28609096
Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.
Stepan AF, Tran TP, Helal CJ, Brown MS, Chang C, O'Connor RE, De Vivo M, Doran SD, Fisher EL, Jenkinson S, Karanian D, Kormos BL, Sharma R, Walker GS, Wright AS, Yang EX, Brodney MA, Wager TT, Verhoest PR, Obach RS. Stepan AF, et al. Among authors: chang c. ACS Med Chem Lett. 2018 Jan 4;9(2):68-72. doi: 10.1021/acsmedchemlett.7b00343. eCollection 2018 Feb 8. ACS Med Chem Lett. 2018. PMID: 29456790 Free PMC article.
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: chang c. 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
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Pandit J, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, McGinnis D, O'Connor RE, O'Donnell CJ, Ogden A, Piotrowski M, Schmidt CJ, Seymour PA, Ueno H, Vansell N, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: chang c. J Med Chem. 2018 Feb 8;61(3):1001-1018. doi: 10.1021/acs.jmedchem.7b01466. Epub 2018 Jan 16. J Med Chem. 2018. PMID: 29293004
Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior.
Wager TT, Chandrasekaran RY, Bradley J, Rubitski D, Berke H, Mente S, Butler T, Doran A, Chang C, Fisher K, Knafels J, Liu S, Ohren J, Marconi M, DeMarco G, Sneed B, Walton K, Horton D, Rosado A, Mead A. Wager TT, et al. Among authors: chang c. ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65. doi: 10.1021/cn500201x. Epub 2014 Oct 28. ACS Chem Neurosci. 2014. PMID: 25299732 Clinical Trial.
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: chang c. J Med Chem. 2017 Jul 13;60(13):5673-5698. doi: 10.1021/acs.jmedchem.7b00397. Epub 2017 Jun 16. J Med Chem. 2017. PMID: 28574706
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