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Page 1
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).
Curtin ML, Heyman HR, Clark RF, Sorensen BK, Doherty GA, Hansen TM, Frey RR, Sarris KA, Aguirre AL, Shrestha A, Tu N, Woller K, Pliushchev MA, Sweis RF, Cheng M, Wilsbacher JL, Kovar PJ, Guo J, Cheng D, Longenecker KL, Raich D, Korepanova AV, Soni NB, Algire MA, Richardson PL, Marin VL, Badagnani I, Vasudevan A, Buchanan FG, Maag D, Chiang GG, Tse C, Michaelides MR. Curtin ML, et al. Among authors: woller k. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3317-3325. doi: 10.1016/j.bmcl.2017.06.018. Epub 2017 Jun 14. Bioorg Med Chem Lett. 2017. PMID: 28610984
Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors.
Friedman M, Frank KE, Aguirre A, Argiriadi MA, Davis H, Edmunds JJ, George DM, George JS, Goedken E, Fiamengo B, Hyland D, Li B, Murtaza A, Morytko M, Somal G, Stewart K, Tarcsa E, Van Epps S, Voss J, Wang L, Woller K, Wishart N. Friedman M, et al. Among authors: woller k. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4399-404. doi: 10.1016/j.bmcl.2015.09.020. Epub 2015 Sep 8. Bioorg Med Chem Lett. 2015. PMID: 26372653
Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 (IDH1): Direct Covalent Modification of His315.
Jakob CG, Upadhyay AK, Donner PL, Nicholl E, Addo SN, Qiu W, Ling C, Gopalakrishnan SM, Torrent M, Cepa SP, Shanley J, Shoemaker AR, Sun CC, Vasudevan A, Woller KR, Shotwell JB, Shaw B, Bian Z, Hutti JE. Jakob CG, et al. Among authors: woller kr. J Med Chem. 2018 Aug 9;61(15):6647-6657. doi: 10.1021/acs.jmedchem.8b00305. Epub 2018 Jul 30. J Med Chem. 2018. PMID: 30004704
Discovery of thieno[2,3-c]pyridines as potent COT inhibitors.
George D, Friedman M, Allen H, Argiriadi M, Barberis C, Bischoff A, Clabbers A, Cusack K, Dixon R, Fix-Stenzel S, Gordon T, Janssen B, Jia Y, Moskey M, Quinn C, Salmeron JA, Wishart N, Woller K, Yu Z. George D, et al. Among authors: woller k. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4952-5. doi: 10.1016/j.bmcl.2008.08.037. Epub 2008 Aug 14. Bioorg Med Chem Lett. 2008. PMID: 18755587
Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.
Kreft A, Harrison B, Aschmies S, Atchison K, Casebier D, Cole DC, Diamantidis G, Ellingboe J, Hauze D, Hu Y, Huryn D, Jin M, Kubrak D, Lu P, Lundquist J, Mann C, Martone R, Moore W, Oganesian A, Porte A, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Woller K, Xu Z, Zhou H, Steven Jacobsen J. Kreft A, et al. Among authors: woller k. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4232-6. doi: 10.1016/j.bmcl.2008.05.064. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18556202
Targeting IRAK3 for Degradation to Enhance IL-12 Pro-inflammatory Cytokine Production.
Rowley A, Brown BS, Stofega M, Hoh H, Mathew R, Marin V, Ding RX, McClure RA, Bittencourt FM, Chen J, Gururaja T, Kinoshita T, Wang X, Rivkin A, Woller KR. Rowley A, et al. Among authors: woller kr. ACS Chem Biol. 2022 Jun 17;17(6):1315-1320. doi: 10.1021/acschembio.2c00037. Epub 2022 May 17. ACS Chem Biol. 2022. PMID: 35580266
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS. Mayer SC, et al. Among authors: woller k. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
(S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor.
Cole DC, Stock JR, Kreft AF, Antane M, Aschmies SH, Atchison KP, Casebier DS, Comery TA, Diamantidis G, Ellingboe JW, Harrison BL, Hu Y, Jin M, Kubrak DM, Lu P, Mann CW, Martone RL, Moore WJ, Oganesian A, Riddell DR, Sonnenberg-Reines J, Sun SC, Wagner E, Wang Z, Woller KR, Xu Z, Zhou H, Jacobsen JS. Cole DC, et al. Bioorg Med Chem Lett. 2009 Feb 1;19(3):926-9. doi: 10.1016/j.bmcl.2008.11.116. Epub 2008 Dec 6. Bioorg Med Chem Lett. 2009. PMID: 19097890
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.
Betschmann P, Bettencourt B, Donnelly-Roberts D, Friedman M, George J, Hirst G, Josephsohn N, Konopacki D, Li B, Maull J, Morytko MJ, Moore NS, Namovic M, Rafferty P, Salmeron-Garcia JA, Tarcsa E, Wang L, Woller K. Betschmann P, et al. Among authors: woller k. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3848-51. doi: 10.1016/j.bmcl.2008.06.055. Epub 2008 Jun 20. Bioorg Med Chem Lett. 2008. PMID: 18595695
26 results