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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: lefker ba. 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.
Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility.
Kalgutkar AS, Frederick KS, Hatch HL, Ambler CM, Perry DA, Garigipati RS, Chang GC, Lefker BA, Clark RW, Morehouse LA, Francone O, Hu X. Kalgutkar AS, et al. Among authors: lefker ba. Xenobiotica. 2014 Jul;44(7):591-605. doi: 10.3109/00498254.2013.874611. Epub 2013 Dec 31. Xenobiotica. 2014. PMID: 24380613
Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
Li JJ, Iula DM, Nguyen MN, Hu LY, Dettling D, Johnson TR, Du DY, Shanmugasundaram V, Van Camp JA, Wang Z, Harter WG, Yue WS, Boys ML, Wade KJ, Drummond EM, Samas BM, Lefker BA, Hoge GS, Lovdahl MJ, Asbill J, Carroll M, Meade MA, Ciotti SM, Krieger-Burke T. Li JJ, et al. Among authors: lefker ba. J Med Chem. 2008 Nov 13;51(21):7010-4. doi: 10.1021/jm8009316. Epub 2008 Oct 16. J Med Chem. 2008. PMID: 18921992
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: lefker ba. Sci Rep. 2016 Aug 16;6:30859. doi: 10.1038/srep30859. Sci Rep. 2016. PMID: 27527709 Free PMC article.
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Chesworth R, Wessel MD, Heyden L, Mangano FM, Zawistoski M, Gegnas L, Galluzzo D, Lefker B, Cameron KO, Tickner J, Lu B, Castleberry TA, Petersen DN, Brault A, Perry P, Ng O, Owen TA, Pan L, Ke HZ, Brown TA, Thompson DD, DaSilva-Jardine P. Chesworth R, et al. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. doi: 10.1016/j.bmcl.2005.08.010. Epub 2005 Oct 10. Bioorg Med Chem Lett. 2005. PMID: 16219463
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.
Chesworth R, Zawistoski MP, Lefker BA, Cameron KO, Day RF, Mangano FM, Rosati RL, Colella S, Petersen DN, Brault A, Lu B, Pan LC, Perry P, Ng O, Castleberry TA, Owen TA, Brown TA, Thompson DD, DaSilva-Jardine P. Chesworth R, et al. Among authors: lefker ba. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2729-33. doi: 10.1016/j.bmcl.2004.03.077. Bioorg Med Chem Lett. 2004. PMID: 15125923
Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay.
Hall J, Brault A, Vincent F, Weng S, Wang H, Dumlao D, Aulabaugh A, Aivazian D, Castro D, Chen M, Culp J, Dower K, Gardner J, Hawrylik S, Golenbock D, Hepworth D, Horn M, Jones L, Jones P, Latz E, Li J, Lin LL, Lin W, Lin D, Lovering F, Niljanskul N, Nistler R, Pierce B, Plotnikova O, Schmitt D, Shanker S, Smith J, Snyder W, Subashi T, Trujillo J, Tyminski E, Wang G, Wong J, Lefker B, Dakin L, Leach K. Hall J, et al. PLoS One. 2017 Sep 21;12(9):e0184843. doi: 10.1371/journal.pone.0184843. eCollection 2017. PLoS One. 2017. PMID: 28934246 Free PMC article.
From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.
Futatsugi K, Mascitti V, Guimarães CR, Morishita N, Cai C, DeNinno MP, Gao H, Hamilton MD, Hank R, Harris AR, Kung DW, Lavergne SY, Lefker BA, Lopaze MG, McClure KF, Munchhof MJ, Preville C, Robinson RP, Wright SW, Bonin PD, Cornelius P, Chen Y, Kalgutkar AS. Futatsugi K, et al. Among authors: lefker ba. Bioorg Med Chem Lett. 2013 Jan 1;23(1):194-7. doi: 10.1016/j.bmcl.2012.10.119. Epub 2012 Nov 5. Bioorg Med Chem Lett. 2013. PMID: 23177788
38 results