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Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.

Probst G, Aubele DL, Bowers S, Dressen D, Garofalo AW, Hom RK, Konradi AW, Marugg JL, Mattson MN, Neitzel ML, Semko CM, Sham HL, Smith J, Sun M, Truong AP, Ye XM, Xu YZ, Dappen MS, Jagodzinski JJ, Keim PS, Peterson B, Latimer LH, Quincy D, Wu J, Goldbach E, Ness DK, Quinn KP, Sauer JM, Wong K, Zhang H, Zmolek W, Brigham EF, Kholodenko D, Hu K, Kwong GT, Lee M, Liao A, Motter RN, Sacayon P, Santiago P, Willits C, Bard F, Bova MP, Hemphill SS, Nguyen L, Ruslim L, Tanaka K, Tanaka P, Wallace W, Yednock TA, Basi GS.

J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20.


Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease.

Neitzel ML, Aubele DL, Marugg JL, Jagodzinski JJ, Konradi AW, Pleiss MA, Szoke B, Zmolek W, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Bova MP, Hemphill S, Basi G.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3715-20. doi: 10.1016/j.bmcl.2011.04.079. Epub 2011 May 1.


Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.

Basi GS, Hemphill S, Brigham EF, Liao A, Aubele DL, Baker J, Barbour R, Bova M, Chen XH, Dappen MS, Eichenbaum T, Goldbach E, Hawkinson J, Lawler-Herbold R, Hu K, Hui T, Jagodzinski JJ, Keim PS, Kholodenko D, Latimer LH, Lee M, Marugg J, Mattson MN, McCauley S, Miller JL, Motter R, Mutter L, Neitzel ML, Ni H, Nguyen L, Quinn K, Ruslim L, Semko CM, Shapiro P, Smith J, Soriano F, Szoke B, Tanaka K, Tang P, Tucker JA, Ye XM, Yu M, Wu J, Xu YZ, Garofalo AW, Sauer JM, Konradi AW, Ness D, Shopp G, Pleiss MA, Freedman SB, Schenk D.

Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60.


Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II).

Ye XM, Konradi AW, Smith J, Aubele DL, Garofalo AW, Marugg J, Neitzel ML, Semko CM, Sham HL, Sun M, Truong AP, Wu J, Zhang H, Goldbach E, Sauer JM, Brigham EF, Bova M, Basi GS.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3502-6. doi: 10.1016/j.bmcl.2010.04.148. Epub 2010 May 6.


Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.

Ye XM, Konradi AW, Smith J, Xu YZ, Dressen D, Garofalo AW, Marugg J, Sham HL, Truong AP, Jagodzinski J, Pleiss M, Zhang H, Goldbach E, Sauer JM, Brigham E, Bova M, Basi GS.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2195-9. doi: 10.1016/j.bmcl.2010.02.039. Epub 2010 Feb 13.


A rapid and reliable alternative to ISO 21528-1:2004 for detection of Enterobacteriaceae.

Joosten H, Marugg J, Stephan R, Klijn A, Jackson T, Iversen C.

Int J Food Microbiol. 2008 Jul 31;125(3):344-6. doi: 10.1016/j.ijfoodmicro.2008.04.003. Epub 2008 May 1.


Identification of gamma-secretase inhibitor potency determinants on presenilin.

Zhao B, Yu M, Neitzel M, Marugg J, Jagodzinski J, Lee M, Hu K, Schenk D, Yednock T, Basi G.

J Biol Chem. 2008 Feb 1;283(5):2927-38. Epub 2007 Nov 21.


Identification of "Cronobacter" spp. (Enterobacter sakazakii).

Iversen C, Lehner A, Mullane N, Marugg J, Fanning S, Stephan R, Joosten H.

J Clin Microbiol. 2007 Nov;45(11):3814-6. Epub 2007 Sep 19.


Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.

Dressen D, Garofalo AW, Hawkinson J, Hom D, Jagodzinski J, Marugg JL, Neitzel ML, Pleiss MA, Szoke B, Tung JS, Wone DW, Wu J, Zhang H.

J Med Chem. 2007 Oct 18;50(21):5161-7. Epub 2007 Sep 19.


A simple and rapid cultural method for detection of Enterobacter sakazakii in environmental samples.

Guillaume-Gentil O, Sonnard V, Kandhai MC, Marugg JD, Joosten H.

J Food Prot. 2005 Jan;68(1):64-9.


Specialized roles of the two pathways for the synthesis of mannosylglycerate in osmoadaptation and thermoadaptation of Rhodothermus marinus.

Borges N, Marugg JD, Empadinhas N, da Costa MS, Santos H.

J Biol Chem. 2004 Mar 12;279(11):9892-8. Epub 2003 Dec 29.


Reverse transcription-PCR analysis of bottled and natural mineral waters for the presence of noroviruses.

Lamothe GT, Putallaz T, Joosten H, Marugg JD.

Appl Environ Microbiol. 2003 Nov;69(11):6541-9.


Osmotic adaptation of Thermus thermophilus RQ-1: lesson from a mutant deficient in synthesis of trehalose.

Silva Z, Alarico S, Nobre A, Horlacher R, Marugg J, Boos W, Mingote AI, da Costa MS.

J Bacteriol. 2003 Oct;185(20):5943-52.


Comparison of media for enumeration of Clostridium perfringens from foods.

de Jong AE, Eijhusen GP, Brouwer-Post EJ, Grand M, Johansson T, Kärkkäinen T, Marugg J, in't Veld PH, Warmerdam FH, Wörner G, Zicavo A, Rombouts FM, Beumer RR.

J Microbiol Methods. 2003 Sep;54(3):359-66.


Genetic heterogeneity in Bacillus sporothermodurans as demonstrated by ribotyping and repetitive extragenic palindromic-PCR fingerprinting.

Guillaume-Gentil O, Scheldeman P, Marugg J, Herman L, Joosten H, Heyndrickx M.

Appl Environ Microbiol. 2002 Sep;68(9):4216-24.


A siderophore peptide synthetase gene from plant-growth-promoting Pseudomonas putida WCS358.

Devescovi G, Aguilar C, Majolini MB, Marugg J, Weisbeek P, Venturi V.

Syst Appl Microbiol. 2001 Nov;24(3):321-30.


Pathway for the synthesis of mannosylglycerate in the hyperthermophilic archaeon Pyrococcus horikoshii. Biochemical and genetic characterization of key enzymes.

Empadinhas N, Marugg JD, Borges N, Santos H, da Costa MS.

J Biol Chem. 2001 Nov 23;276(47):43580-8. Epub 2001 Sep 18.


Molecular and functional analyses of the metC gene of Lactococcus lactis, encoding cystathionine beta-lyase.

Fernández M, van Doesburg W, Rutten GA, Marugg JD, Alting AC, van Kranenburg R, Kuipers OP.

Appl Environ Microbiol. 2000 Jan;66(1):42-8.


Biosynthesis of mannosylglycerate in the thermophilic bacterium Rhodothermus marinus. Biochemical and genetic characterization of a mannosylglycerate synthase.

Martins LO, Empadinhas N, Marugg JD, Miguel C, Ferreira C, da Costa MS, Santos H.

J Biol Chem. 1999 Dec 10;274(50):35407-14.

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