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Items: 19

1.

Pharmacokinetic/Pharmacodynamic Correlation Analysis of Amantadine for Levodopa-Induced Dyskinesia.

Brigham EF, Johnston TH, Brown C, Holt JDS, Fox SH, Hill MP, Howson PA, Brotchie JM, Nguyen JT.

J Pharmacol Exp Ther. 2018 Nov;367(2):373-381. doi: 10.1124/jpet.118.247650. Epub 2018 Aug 7.

PMID:
30087157
2.

Chronic γ-secretase inhibition reduces amyloid plaque-associated instability of pre- and postsynaptic structures.

Liebscher S, Page RM, Käfer K, Winkler E, Quinn K, Goldbach E, Brigham EF, Quincy D, Basi GS, Schenk DB, Steiner H, Bonhoeffer T, Haass C, Meyer-Luehmann M, Hübener M.

Mol Psychiatry. 2014 Aug;19(8):937-46. doi: 10.1038/mp.2013.122. Epub 2013 Sep 24.

3.

Leucine-rich repeat kinase 2 (LRRK2)-deficient rats exhibit renal tubule injury and perturbations in metabolic and immunological homeostasis.

Ness D, Ren Z, Gardai S, Sharpnack D, Johnson VJ, Brennan RJ, Brigham EF, Olaharski AJ.

PLoS One. 2013 Jun 14;8(6):e66164. doi: 10.1371/journal.pone.0066164. Print 2013.

4.

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.

PMID:
23713656
5.

Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.

Garofalo AW, Adler M, Aubele DL, Brigham EF, Chian D, Franzini M, Goldbach E, Kwong GT, Motter R, Probst GD, Quinn KP, Ruslim L, Sham HL, Tam D, Tanaka P, Truong AP, Ye XM, Ren Z.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):1974-7. doi: 10.1016/j.bmcl.2013.02.041. Epub 2013 Feb 15.

PMID:
23453068
6.

Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.

Aubele DL, Truong AP, Dressen DB, Probst GD, Bowers S, Mattson MN, Semko CM, Sun M, Garofalo AW, Konradi AW, Sham HL, Zmolek W, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Bova MP, Hemphill SS, Basi G.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5791-4. doi: 10.1016/j.bmcl.2011.08.008. Epub 2011 Aug 9.

PMID:
21885276
7.

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.

PMID:
21571529
8.

Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.

Bowers S, Truong AP, Neitz RJ, Neitzel M, Probst GD, Hom RK, Peterson B, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Brigham EF, Quinn KP, Sauer JM, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1838-43. doi: 10.1016/j.bmcl.2011.01.046. Epub 2011 Jan 20.

PMID:
21316234
9.

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.

10.

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.

Truong AP, Tóth G, Probst GD, Sealy JM, Bowers S, Wone DW, Dressen D, Hom RK, Konradi AW, Sham HL, Wu J, Peterson BT, Ruslim L, Bova MP, Kholodenko D, Motter RN, Bard F, Santiago P, Ni H, Chian D, Soriano F, Cole T, Brigham EF, Wong K, Zmolek W, Goldbach E, Samant B, Chen L, Zhang H, Nakamura DF, Quinn KP, Yednock TA, Sauer JM.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6231-6. doi: 10.1016/j.bmcl.2010.08.102. Epub 2010 Aug 24.

PMID:
20833041
11.

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.

PMID:
20529683
12.

Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

Mattson MN, Neitzel ML, Quincy DA, Semko CM, Garofalo AW, Keim PS, Konradi AW, Pleiss MA, Sham HL, Brigham EF, Goldbach EG, Zhang H, Sauer JM, Basi GS.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2148-50. doi: 10.1016/j.bmcl.2010.02.050. Epub 2010 Feb 14.

PMID:
20206516
13.

Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.

Truong AP, Aubele DL, Probst GD, Neitzel ML, Semko CM, Bowers S, Dressen D, Hom RK, Konradi AW, Sham HL, Garofalo AW, Keim PS, Wu J, Dappen MS, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Hemphill SS, Bova MP, Bard F, Yednock TA, Basi G.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):4920-3. doi: 10.1016/j.bmcl.2009.07.092. Epub 2009 Jul 23. Erratum in: Bioorg Med Chem Lett. 2010 Dec 15;20(24):7553. Bard, Frédérique [added]; Yednock, Ted A [added].

PMID:
19660943
14.

Polo-like kinase 2 (PLK2) phosphorylates alpha-synuclein at serine 129 in central nervous system.

Inglis KJ, Chereau D, Brigham EF, Chiou SS, Schöbel S, Frigon NL, Yu M, Caccavello RJ, Nelson S, Motter R, Wright S, Chian D, Santiago P, Soriano F, Ramos C, Powell K, Goldstein JM, Babcock M, Yednock T, Bard F, Basi GS, Sham H, Chilcote TJ, McConlogue L, Griswold-Prenner I, Anderson JP.

J Biol Chem. 2009 Jan 30;284(5):2598-602. doi: 10.1074/jbc.C800206200. Epub 2008 Nov 12.

15.

Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP Transgenic Mice.

McConlogue L, Buttini M, Anderson JP, Brigham EF, Chen KS, Freedman SB, Games D, Johnson-Wood K, Lee M, Zeller M, Liu W, Motter R, Sinha S.

J Biol Chem. 2007 Sep 7;282(36):26326-34. Epub 2007 Jul 6.

16.

Inflammatory repertoire of Alzheimer's disease and nondemented elderly microglia in vitro.

Lue LF, Rydel R, Brigham EF, Yang LB, Hampel H, Murphy GM Jr, Brachova L, Yan SD, Walker DG, Shen Y, Rogers J.

Glia. 2001 Jul;35(1):72-9.

PMID:
11424194
17.
18.

Aggregated amyloid-beta protein induces cortical neuronal apoptosis and concomitant "apoptotic" pattern of gene induction.

Estus S, Tucker HM, van Rooyen C, Wright S, Brigham EF, Wogulis M, Rydel RE.

J Neurosci. 1997 Oct 15;17(20):7736-45.

19.

Secondary structure of amyloid beta peptide correlates with neurotoxic activity in vitro.

Simmons LK, May PC, Tomaselli KJ, Rydel RE, Fuson KS, Brigham EF, Wright S, Lieberburg I, Becker GW, Brems DN, et al.

Mol Pharmacol. 1994 Mar;45(3):373-9.

PMID:
8145724

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