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Page 1
Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.
Liang SH, Chen JM, Normandin MD, Chang JS, Chang GC, Taylor CK, Trapa P, Plummer MS, Para KS, Conn EL, Lopresti-Morrow L, Lanyon LF, Cook JM, Richter KE, Nolan CE, Schachter JB, Janat F, Che Y, Shanmugasundaram V, Lefker BA, Enerson BE, Livni E, Wang L, Guehl NJ, Patnaik D, Wagner FF, Perlis R, Holson EB, Haggarty SJ, El Fakhri G, Kurumbail RG, Vasdev N. Liang SH, et al. Among authors: chen jm. Angew Chem Int Ed Engl. 2016 Aug 8;55(33):9601-5. doi: 10.1002/anie.201603797. Epub 2016 Jun 29. Angew Chem Int Ed Engl. 2016. PMID: 27355874 Free PMC article.
Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery.
Bernard-Gauthier V, Mossine AV, Knight A, Patnaik D, Zhao WN, Cheng C, Krishnan HS, Xuan LL, Chindavong PS, Reis SA, Chen JM, Shao X, Stauff J, Arteaga J, Sherman P, Salem N, Bonsall D, Amaral B, Varlow C, Wells L, Martarello L, Patel S, Liang SH, Kurumbail RG, Haggarty SJ, Scott PJH, Vasdev N. Bernard-Gauthier V, et al. Among authors: chen jm. J Med Chem. 2019 Nov 14;62(21):9600-9617. doi: 10.1021/acs.jmedchem.9b01030. Epub 2019 Oct 21. J Med Chem. 2019. PMID: 31535859 Free PMC article.
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.
Ahn K, Boehm M, Brown MF, Calloway J, Che Y, Chen J, Fennell KF, Geoghegan KF, Gilbert AM, Gutierrez JA, Kalgutkar AS, Lanba A, Limberakis C, Magee TV, O'Doherty I, Oliver R, Pabst B, Pandit J, Parris K, Pfefferkorn JA, Rolph TP, Patel R, Schuff B, Shanmugasundaram V, Starr JT, Varghese AH, Vera NB, Vernochet C, Yan J. Ahn K, et al. ACS Chem Biol. 2016 Sep 16;11(9):2529-40. doi: 10.1021/acschembio.6b00266. Epub 2016 Jul 19. ACS Chem Biol. 2016. PMID: 27391855
Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents.
McAllister LA, Montgomery JI, Abramite JA, Reilly U, Brown MF, Chen JM, Barham RA, Che Y, Chung SW, Menard CA, Mitton-Fry M, Mullins LM, Noe MC, O'Donnell JP, Oliver RM 3rd, Penzien JB, Plummer M, Price LM, Shanmugasundaram V, Tomaras AP, Uccello DP. McAllister LA, et al. Among authors: chen jm. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6832-8. doi: 10.1016/j.bmcl.2012.09.058. Epub 2012 Sep 24. Bioorg Med Chem Lett. 2012. PMID: 23046961
Potent inhibitors of LpxC for the treatment of Gram-negative infections.
Brown MF, Reilly U, Abramite JA, Arcari JT, Oliver R, Barham RA, Che Y, Chen JM, Collantes EM, Chung SW, Desbonnet C, Doty J, Doroski M, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, Marra A, McElroy E, Melnick M, Menard CA, Montgomery JI, Mullins L, Noe MC, O'Donnell J, Penzien J, Plummer MS, Price LM, Shanmugasundaram V, Thoma C, Uccello DP, Warmus JS, Wishka DG. Brown MF, et al. Among authors: chen jm. J Med Chem. 2012 Jan 26;55(2):914-23. doi: 10.1021/jm2014748. Epub 2012 Jan 11. J Med Chem. 2012. PMID: 22175825
Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections.
Montgomery JI, Brown MF, Reilly U, Price LM, Abramite JA, Arcari J, Barham R, Che Y, Chen JM, Chung SW, Collantes EM, Desbonnet C, Doroski M, Doty J, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, McAllister L, McElroy E, Menard CA, Mitton-Fry M, Mullins L, Noe MC, O'Donnell J, Oliver R, Penzien J, Plummer M, Shanmugasundaram V, Thoma C, Tomaras AP, Uccello DP, Vaz A, Wishka DG. Montgomery JI, et al. Among authors: chen jm. J Med Chem. 2012 Feb 23;55(4):1662-70. doi: 10.1021/jm2014875. Epub 2012 Feb 8. J Med Chem. 2012. PMID: 22257165
Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists.
Liu S, Dakin LA, Xing L, Withka JM, Sahasrabudhe PV, Li W, Banker ME, Balbo P, Shanker S, Chrunyk BA, Guo Z, Chen JM, Young JA, Bai G, Starr JT, Wright SW, Bussenius J, Tan S, Gopalsamy A, Lefker BA, Vincent F, Jones LH, Xu H, Hoth LR, Geoghegan KF, Qiu X, Bunnage ME, Thorarensen A. Liu S, et al. Among authors: chen jm. Sci Rep. 2016 Aug 16;6:30859. doi: 10.1038/srep30859. Sci Rep. 2016. PMID: 27527709 Free PMC article.
Chemical and computational methods for the characterization of covalent reactive groups for the prospective design of irreversible inhibitors.
Flanagan ME, Abramite JA, Anderson DP, Aulabaugh A, Dahal UP, Gilbert AM, Li C, Montgomery J, Oppenheimer SR, Ryder T, Schuff BP, Uccello DP, Walker GS, Wu Y, Brown MF, Chen JM, Hayward MM, Noe MC, Obach RS, Philippe L, Shanmugasundaram V, Shapiro MJ, Starr J, Stroh J, Che Y. Flanagan ME, et al. Among authors: chen jm. J Med Chem. 2014 Dec 11;57(23):10072-9. doi: 10.1021/jm501412a. Epub 2014 Nov 26. J Med Chem. 2014. PMID: 25375838
The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.
Lippa B, Kauffman GS, Arcari J, Kwan T, Chen J, Hungerford W, Bhattacharya S, Zhao X, Williams C, Xiao J, Pustilnik L, Su C, Moyer JD, Ma L, Campbell M, Steyn S. Lippa B, et al. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3081-6. doi: 10.1016/j.bmcl.2007.03.046. Epub 2007 Mar 19. Bioorg Med Chem Lett. 2007. PMID: 17398092
1,951 results