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31 results

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Page 1
The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.
Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Seiffert DA, Zaczek R, Albright CF, Toyn JH. Burton CR, et al. Among authors: bergstrom cp. J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23. J Biol Chem. 2008. PMID: 18574238 Free article.
N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.
Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Deshpande MS, Felsenstein KM, Guss VL, Hansel SB, Johnson G, Keavy DJ, Lau WY, Mock J, Prasad CV, Polson CT, Sloan CP, Smith DW, Wallace OB, Wang HH, Williams A, Zheng M. Parker MF, et al. Among authors: bergstrom cp. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4432-6. doi: 10.1016/j.bmcl.2007.06.022. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17606371
Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Bergstrom CP, Sloan CP, Wang HH, Parker MF, Smith DW, Zheng M, Hansel SB, Polson CT, Barber LE, Bursuker I, Guss VL, Corsa JA, Barten DM, Felsenstein KM, Roberts SB. Bergstrom CP, et al. Bioorg Med Chem Lett. 2008 Jan 1;18(1):175-8. doi: 10.1016/j.bmcl.2007.10.105. Epub 2007 Nov 1. Bioorg Med Chem Lett. 2008. PMID: 18023581
Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Bergstrom CP, Sloan CP, Lau WY, Smith DW, Zheng M, Hansel SB, Polson CT, Corsa JA, Barten DM, Felsenstein KM, Roberts SB. Bergstrom CP, et al. Bioorg Med Chem Lett. 2008 Jan 15;18(2):464-8. doi: 10.1016/j.bmcl.2007.11.102. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18178084
Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.
Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE. Gillman KW, et al. Among authors: bergstrom cp. ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10. ACS Med Chem Lett. 2010. PMID: 24900185 Free PMC article.
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.
Prasad CV, Zheng M, Vig S, Bergstrom C, Smith DW, Gao Q, Yeola S, Polson CT, Corsa JA, Guss VL, Loo A, Wang J, Sleczka BG, Dangler C, Robertson BJ, Hendrick JP, Roberts SB, Barten DM. Prasad CV, et al. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4006-11. doi: 10.1016/j.bmcl.2007.04.082. Epub 2007 Apr 30. Bioorg Med Chem Lett. 2007. PMID: 17502137
2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors.
Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Dee MF, Gai Y, Guss VL, Higgins MA, Keavy DJ, Loo A, Mate RA, Marcin LR, McElhone KE, Polson CT, Roberts SB, Macor JE. Parker MF, et al. Among authors: bergstrom cp. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6828-31. doi: 10.1016/j.bmcl.2012.09.057. Epub 2012 Sep 24. Bioorg Med Chem Lett. 2012. PMID: 23046960
Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Gentles RG, Ding M, Bender JA, Bergstrom CP, Grant-Young K, Hewawasam P, Hudyma T, Martin S, Nickel A, Regueiro-Ren A, Tu Y, Yang Z, Yeung KS, Zheng X, Chao S, Sun JH, Beno BR, Camac DM, Chang CH, Gao M, Morin PE, Sheriff S, Tredup J, Wan J, Witmer MR, Xie D, Hanumegowda U, Knipe J, Mosure K, Santone KS, Parker DD, Zhuo X, Lemm J, Liu M, Pelosi L, Rigat K, Voss S, Wang Y, Wang YK, Colonno RJ, Gao M, Roberts SB, Gao Q, Ng A, Meanwell NA, Kadow JF. Gentles RG, et al. Among authors: bergstrom cp. J Med Chem. 2014 Mar 13;57(5):1855-79. doi: 10.1021/jm4016894. Epub 2014 Jan 7. J Med Chem. 2014. PMID: 24397558
Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus.
Zheng X, Hudyma TW, Martin SW, Bergstrom C, Ding M, He F, Romine J, Poss MA, Kadow JF, Chang CH, Wan J, Witmer MR, Morin P, Camac DM, Sheriff S, Beno BR, Rigat KL, Wang YK, Fridell R, Lemm J, Qiu D, Liu M, Voss S, Pelosi L, Roberts SB, Gao M, Knipe J, Gentles RG. Zheng X, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):2925-9. doi: 10.1016/j.bmcl.2011.03.067. Epub 2011 Mar 23. Bioorg Med Chem Lett. 2011. PMID: 21486696
The synthesis and evaluation of a novel class of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid hepatitis C virus polymerase NS5B inhibitors.
Martin SW, Glunz P, Beno BR, Bergstrom C, Romine JL, Priestley ES, Newman M, Gao M, Roberts S, Rigat K, Fridell R, Qiu D, Knobloh G, Wang YK. Martin SW, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):2869-72. doi: 10.1016/j.bmcl.2011.03.086. Epub 2011 Mar 30. Bioorg Med Chem Lett. 2011. PMID: 21507645
31 results