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Page 1
Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Butler TW, Dorff PH, Efremov IV, Evrard E, Green ME, Helal CJ, Kauffman GW, Mullins PB, Navaratnam T, O'Donnell CJ, O'Sullivan TJ, Patel NC, Stepan AF, Stiff CM, Subramanyam C, Trapa P, Tran TP, Vetelino BC, Yang E, Xie L, Pustilnik LR, Steyn SJ, Wood KM, Bales KR, Hajos-Korcsok E, Verhoest PR. Pettersson M, et al. Among authors: green me. J Med Chem. 2024 Jun 27;67(12):10248-10262. doi: 10.1021/acs.jmedchem.4c00580. Epub 2024 Jun 7. J Med Chem. 2024. PMID: 38848667
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: green me. J Med Chem. 2012 Apr 12;55(7):3414-24. doi: 10.1021/jm300094u. Epub 2012 Mar 29. J Med Chem. 2012. PMID: 22420884
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: green me. 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, 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: green me. J Med Chem. 2014 Feb 13;57(3):1046-62. doi: 10.1021/jm401782h. Epub 2014 Jan 28. J Med Chem. 2014. PMID: 24428186
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: green me. 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.
Design and optimization of selective azaindole amide M1 positive allosteric modulators.
Davoren JE, O'Neil SV, Anderson DP, Brodney MA, Chenard L, Dlugolenski K, Edgerton JR, Green M, Garnsey M, Grimwood S, Harris AR, Kauffman GW, LaChapelle E, Lazzaro JT, Lee CW, Lotarski SM, Nason DM, Obach RS, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Yan J, Zhang L. Davoren JE, et al. Bioorg Med Chem Lett. 2016 Jan 15;26(2):650-655. doi: 10.1016/j.bmcl.2015.11.053. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26631313
Ligand-protein interactions of selective casein kinase 1δ inhibitors.
Mente S, Arnold E, Butler T, Chakrapani S, Chandrasekaran R, Cherry K, DiRico K, Doran A, Fisher K, Galatsis P, Green M, Hayward M, Humphrey J, Knafels J, Li J, Liu S, Marconi M, McDonald S, Ohren J, Paradis V, Sneed B, Walton K, Wager T. Mente S, et al. J Med Chem. 2013 Sep 12;56(17):6819-28. doi: 10.1021/jm4006324. Epub 2013 Aug 28. J Med Chem. 2013. PMID: 23919824
Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE.
Seneviratne U, Huang Z, Am Ende CW, Butler TW, Cleary L, Dresselhaus E, Evrard E, Fisher EL, Green ME, Helal CJ, Humphrey JM, Lanyon LF, Marconi M, Mukherjee P, Sciabola S, Steppan CM, Sylvain EK, Tuttle JB, Verhoest PR, Wager TT, Xie L, Ramaswamy G, Johnson DS, Pettersson M. Seneviratne U, et al. Among authors: green me. Cell Chem Biol. 2021 Feb 18;28(2):148-157.e7. doi: 10.1016/j.chembiol.2020.09.002. Epub 2020 Sep 29. Cell Chem Biol. 2021. PMID: 32997975 Free article.
Natural Product Splicing Inhibitors: A New Class of Antibody-Drug Conjugate (ADC) Payloads.
Puthenveetil S, Loganzo F, He H, Dirico K, Green M, Teske J, Musto S, Clark T, Rago B, Koehn F, Veneziale R, Falahaptisheh H, Han X, Barletta F, Lucas J, Subramanyam C, O'Donnell CJ, Tumey LN, Sapra P, Gerber HP, Ma D, Graziani EI. Puthenveetil S, et al. Bioconjug Chem. 2016 Aug 17;27(8):1880-8. doi: 10.1021/acs.bioconjchem.6b00291. Epub 2016 Jul 28. Bioconjug Chem. 2016. PMID: 27412791
148 results