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Items: 1 to 50 of 104

1.

Translocator protein in late stage Alzheimer's disease and Dementia with Lewy bodies brains.

Xu J, Sun J, Perrin RJ, Mach RH, Bales KR, Morris JC, Benzinger TLS, Holtzman DM.

Ann Clin Transl Neurol. 2019 Aug;6(8):1423-1434. doi: 10.1002/acn3.50837. Epub 2019 Jul 9.

2.

Targeting apolipoprotein E for treating Alzheimer's disease.

Bales KR, Paul SM.

Neurosci Lett. 2019 Jul 20;709:134366. doi: 10.1016/j.neulet.2019.134366. [Epub ahead of print]

PMID:
31336138
3.

Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.

O'Neill BT, Beck EM, Butler CR, Nolan CE, Gonzales C, Zhang L, Doran SD, Lapham K, Buzon LM, Dutra JK, Barreiro G, Hou X, Martinez-Alsina LA, Rogers BN, Villalobos A, Murray JC, Ogilvie K, LaChapelle EA, Chang C, Lanyon LF, Steppan CM, Robshaw A, Hales K, Boucher GG, Pandher K, Houle C, Ambroise CW, Karanian D, Riddell D, Bales KR, Brodney MA.

J Med Chem. 2018 May 24;61(10):4476-4504. doi: 10.1021/acs.jmedchem.8b00246. Epub 2018 Apr 17.

PMID:
29613789
4.

Class I HDAC inhibition is a novel pathway for regulating astrocytic apoE secretion.

Dresselhaus E, Duerr JM, Vincent F, Sylvain EK, Beyna M, Lanyon LF, LaChapelle E, Pettersson M, Bales KR, Ramaswamy G.

PLoS One. 2018 Mar 26;13(3):e0194661. doi: 10.1371/journal.pone.0194661. eCollection 2018.

5.

Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain.

Zhang L, Chen L, Dutra JK, Beck EM, Nag S, Takano A, Amini N, Arakawa R, Brodney MA, Buzon LM, Doran SD, Lanyon LF, McCarthy TJ, Bales KR, Nolan CE, O'Neill BT, Schildknegt K, Halldin C, Villalobos A.

J Med Chem. 2018 Apr 26;61(8):3296-3308. doi: 10.1021/acs.jmedchem.7b01769. Epub 2018 Feb 2.

PMID:
29356535
6.

Incorporating basic and applied approaches to evaluate the effects of invasive Asian Carp on native fishes: A necessary first step for integrated pest management.

Phelps QE, Tripp SJ, Bales KR, James D, Hrabik RA, Herzog DP.

PLoS One. 2017 Sep 5;12(9):e0184081. doi: 10.1371/journal.pone.0184081. eCollection 2017.

7.

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Pettersson M, Johnson DS, Rankic DA, Kauffman GW, Am Ende CW, Butler TW, Boscoe B, Evrard E, Helal CJ, Humphrey JM, Stepan AF, Stiff CM, Yang E, Xie L, Bales KR, Hajos-Korcsok E, Jenkinson S, Pettersen B, Pustilnik LR, Ramirez DS, Steyn SJ, Wood KM, Verhoest PR.

Medchemcomm. 2016 Nov 2;8(4):730-743. doi: 10.1039/c6md00406g. eCollection 2017 Apr 1.

8.

Passive immunotherapy targeting amyloid-β reduces cerebral amyloid angiopathy and improves vascular reactivity.

Bales KR, O'Neill SM, Pozdnyakov N, Pan F, Caouette D, Pi Y, Wood KM, Volfson D, Cirrito JR, Han BH, Johnson AW, Zipfel GJ, Samad TA.

Brain. 2016 Feb;139(Pt 2):563-77. doi: 10.1093/brain/awv313. Epub 2015 Oct 22.

PMID:
26493635
9.

Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.

Pettersson M, Johnson DS, Humphrey JM, Butler TW, Am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, O'Donnell CJ, Stepan AF, Stiff CM, Subramanyam C, Tran TP, Vetelino BC, Yang E, Xie L, Bales KR, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

ACS Med Chem Lett. 2015 Apr 3;6(5):596-601. doi: 10.1021/acsmedchemlett.5b00070. eCollection 2015 May 14.

10.

Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.

Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Evrard E, Efremov I, Kauffman GW, Stepan AF, Stiff CM, Xie L, Bales KR, Hajos-Korcsok E, Murrey HE, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):908-13. doi: 10.1016/j.bmcl.2014.12.059. Epub 2014 Dec 25.

PMID:
25582600
11.

Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione γ-secretase modulators.

Pettersson M, Johnson DS, Subramanyam C, Bales KR, am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, Navaratnam T, Sakya SM, Stiff CM, Tran TP, Xie L, Zhang L, Pustilnik LR, Vetelino BC, Wood KM, Pozdnyakov N, Verhoest PR, O'Donnell CJ.

J Med Chem. 2014 Feb 13;57(3):1046-62. doi: 10.1021/jm401782h. Epub 2014 Jan 28.

PMID:
24428186
12.

γ-Secretase modulator (GSM) photoaffinity probes reveal distinct allosteric binding sites on presenilin.

Pozdnyakov N, Murrey HE, Crump CJ, Pettersson M, Ballard TE, Am Ende CW, Ahn K, Li YM, Bales KR, Johnson DS.

J Biol Chem. 2013 Apr 5;288(14):9710-20. doi: 10.1074/jbc.M112.398602. Epub 2013 Feb 8.

13.

BMS-708,163 targets presenilin and lacks notch-sparing activity.

Crump CJ, Castro SV, Wang F, Pozdnyakov N, Ballard TE, Sisodia SS, Bales KR, Johnson DS, Li YM.

Biochemistry. 2012 Sep 18;51(37):7209-11. doi: 10.1021/bi301137h. Epub 2012 Sep 4.

14.

Chronic administration of an aglycosylated murine antibody of ponezumab does not worsen microhemorrhages in aged Tg2576 mice.

Freeman GB, Brown TP, Wallace K, Bales KR.

Curr Alzheimer Res. 2012 Nov;9(9):1059-68.

PMID:
22631613
15.

The value and limitations of transgenic mouse models used in drug discovery for Alzheimer's disease: an update.

Bales KR.

Expert Opin Drug Discov. 2012 Apr;7(4):281-97. doi: 10.1517/17460441.2012.666234. Epub 2012 Feb 23. Review.

PMID:
22458501
16.

Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators.

Pettersson M, Johnson DS, Subramanyam C, Bales KR, am Ende CW, Fish BA, Green ME, Kauffman GW, Lira R, Mullins PB, Navaratnam T, Sakya SM, Stiff CM, Tran TP, Vetelino BC, Xie L, Zhang L, Pustilnik LR, Wood KM, O'Donnell CJ.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2906-11. doi: 10.1016/j.bmcl.2012.02.059. Epub 2012 Mar 1.

PMID:
22429469
17.

Development of clickable active site-directed photoaffinity probes for γ-secretase.

Crump CJ, am Ende CW, Ballard TE, Pozdnyakov N, Pettersson M, Chau DM, Bales KR, Li YM, Johnson DS.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2997-3000. doi: 10.1016/j.bmcl.2012.02.027. Epub 2012 Feb 20.

18.

Piperidine acetic acid based γ-secretase modulators directly bind to Presenilin-1.

Crump CJ, Fish BA, Castro SV, Chau DM, Gertsik N, Ahn K, Stiff C, Pozdnyakov N, Bales KR, Johnson DS, Li YM.

ACS Chem Neurosci. 2011 Dec 21;2(12):705-710.

19.

High throughput object-based image analysis of β-amyloid plaques in human and transgenic mouse brain.

Samaroo HD, Opsahl AC, Schreiber J, O'Neill SM, Marconi M, Qian J, Carvajal-Gonzalez S, Tate B, Milici AJ, Bales KR, Stephenson DT.

J Neurosci Methods. 2012 Feb 15;204(1):179-188. doi: 10.1016/j.jneumeth.2011.10.003. Epub 2011 Oct 12.

PMID:
22019329
20.

Human apoE isoforms differentially regulate brain amyloid-β peptide clearance.

Castellano JM, Kim J, Stewart FR, Jiang H, DeMattos RB, Patterson BW, Fagan AM, Morris JC, Mawuenyega KG, Cruchaga C, Goate AM, Bales KR, Paul SM, Bateman RJ, Holtzman DM.

Sci Transl Med. 2011 Jun 29;3(89):89ra57. doi: 10.1126/scitranslmed.3002156.

21.

Multiplexed immunoassay panel identifies novel CSF biomarkers for Alzheimer's disease diagnosis and prognosis.

Craig-Schapiro R, Kuhn M, Xiong C, Pickering EH, Liu J, Misko TP, Perrin RJ, Bales KR, Soares H, Fagan AM, Holtzman DM.

PLoS One. 2011 Apr 19;6(4):e18850. doi: 10.1371/journal.pone.0018850.

22.

Genome-wide association study identifies multiple novel loci associated with disease progression in subjects with mild cognitive impairment.

Hu X, Pickering EH, Hall SK, Naik S, Liu YC, Soares H, Katz E, Paciga SA, Liu W, Aisen PS, Bales KR, Samad TA, John SL.

Transl Psychiatry. 2011 Nov 15;1:e54. doi: 10.1038/tp.2011.50.

23.

Cortical M1 receptor concentration increases without a concomitant change in function in Alzheimer's disease.

Overk CR, Felder CC, Tu Y, Schober DA, Bales KR, Wuu J, Mufson EJ.

J Chem Neuroanat. 2010 Sep;40(1):63-70. doi: 10.1016/j.jchemneu.2010.03.005. Epub 2010 Mar 27.

24.

Brain lipid metabolism, apolipoprotein E and the pathophysiology of Alzheimer's disease.

Bales KR.

Neuropharmacology. 2010 Sep-Oct;59(4-5):295-302. doi: 10.1016/j.neuropharm.2010.01.005. Epub 2010 Jan 15. Review.

PMID:
20079752
25.

Reduced levels of human apoE4 protein in an animal model of cognitive impairment.

Sullivan PM, Han B, Liu F, Mace BE, Ervin JF, Wu S, Koger D, Paul S, Bales KR.

Neurobiol Aging. 2011 May;32(5):791-801. doi: 10.1016/j.neurobiolaging.2009.05.011. Epub 2009 Jul 4.

PMID:
19577821
26.

Human APOE isoform-dependent effects on brain beta-amyloid levels in PDAPP transgenic mice.

Bales KR, Liu F, Wu S, Lin S, Koger D, DeLong C, Hansen JC, Sullivan PM, Paul SM.

J Neurosci. 2009 May 27;29(21):6771-9. doi: 10.1523/JNEUROSCI.0887-09.2009.

27.

Macrophage-mediated degradation of beta-amyloid via an apolipoprotein E isoform-dependent mechanism.

Zhao L, Lin S, Bales KR, Gelfanova V, Koger D, Delong C, Hale J, Liu F, Hunter JM, Paul SM.

J Neurosci. 2009 Mar 18;29(11):3603-12. doi: 10.1523/JNEUROSCI.5302-08.2009.

28.

Sortilin-related receptor with A-type repeats (SORLA) affects the amyloid precursor protein-dependent stimulation of ERK signaling and adult neurogenesis.

Rohe M, Carlo AS, Breyhan H, Sporbert A, Militz D, Schmidt V, Wozny C, Harmeier A, Erdmann B, Bales KR, Wolf S, Kempermann G, Paul SM, Schmitz D, Bayer TA, Willnow TE, Andersen OM.

J Biol Chem. 2008 May 23;283(21):14826-34. doi: 10.1074/jbc.M710574200. Epub 2008 Mar 24.

29.

Overexpression of ABCA1 reduces amyloid deposition in the PDAPP mouse model of Alzheimer disease.

Wahrle SE, Jiang H, Parsadanian M, Kim J, Li A, Knoten A, Jain S, Hirsch-Reinshagen V, Wellington CL, Bales KR, Paul SM, Holtzman DM.

J Clin Invest. 2008 Feb;118(2):671-82. doi: 10.1172/JCI33622.

30.

Paroxetine administration decreases AD-like pathology and reverses memory impairments in a transgenic model of Alzheimer disease.

Bales KR.

Exp Neurol. 2007 Sep;207(1):1-3. Epub 2007 Jun 23. Review. No abstract available.

PMID:
17662278
31.

Liver X receptor-mediated gene regulation and cholesterol homeostasis in brain: relevance to Alzheimer's disease therapeutics.

Cao G, Bales KR, DeMattos RB, Paul SM.

Curr Alzheimer Res. 2007 Apr;4(2):179-84. Review.

PMID:
17430244
32.

Enrichment improves cognition in AD mice by amyloid-related and unrelated mechanisms.

Costa DA, Cracchiolo JR, Bachstetter AD, Hughes TF, Bales KR, Paul SM, Mervis RF, Arendash GW, Potter H.

Neurobiol Aging. 2007 Jun;28(6):831-44. Epub 2006 May 26.

PMID:
16730391
33.

Cholinergic dysfunction in a mouse model of Alzheimer disease is reversed by an anti-A beta antibody.

Bales KR, Tzavara ET, Wu S, Wade MR, Bymaster FP, Paul SM, Nomikos GG.

J Clin Invest. 2006 Mar;116(3):825-32. Epub 2006 Feb 23.

34.

Synaptic activity regulates interstitial fluid amyloid-beta levels in vivo.

Cirrito JR, Yamada KA, Finn MB, Sloviter RS, Bales KR, May PC, Schoepp DD, Paul SM, Mennerick S, Holtzman DM.

Neuron. 2005 Dec 22;48(6):913-22.

35.

Impact of variable domain glycosylation on antibody clearance: an LC/MS characterization.

Huang L, Biolsi S, Bales KR, Kuchibhotla U.

Anal Biochem. 2006 Feb 15;349(2):197-207. Epub 2005 Nov 28.

PMID:
16360109
36.

P-glycoprotein deficiency at the blood-brain barrier increases amyloid-beta deposition in an Alzheimer disease mouse model.

Cirrito JR, Deane R, Fagan AM, Spinner ML, Parsadanian M, Finn MB, Jiang H, Prior JL, Sagare A, Bales KR, Paul SM, Zlokovic BV, Piwnica-Worms D, Holtzman DM.

J Clin Invest. 2005 Nov;115(11):3285-90. Epub 2005 Oct 20.

37.

Deletion of Abca1 increases Abeta deposition in the PDAPP transgenic mouse model of Alzheimer disease.

Wahrle SE, Jiang H, Parsadanian M, Hartman RE, Bales KR, Paul SM, Holtzman DM.

J Biol Chem. 2005 Dec 30;280(52):43236-42. Epub 2005 Oct 5.

38.

Neuronal sorting protein-related receptor sorLA/LR11 regulates processing of the amyloid precursor protein.

Andersen OM, Reiche J, Schmidt V, Gotthardt M, Spoelgen R, Behlke J, von Arnim CA, Breiderhoff T, Jansen P, Wu X, Bales KR, Cappai R, Masters CL, Gliemann J, Mufson EJ, Hyman BT, Paul SM, Nykjaer A, Willnow TE.

Proc Natl Acad Sci U S A. 2005 Sep 20;102(38):13461-6. Epub 2005 Sep 7.

39.

Minocycline blocks bilirubin neurotoxicity and prevents hyperbilirubinemia-induced cerebellar hypoplasia in the Gunn rat.

Lin S, Wei X, Bales KR, Paul AB, Ma Z, Yan G, Paul SM, Du Y.

Eur J Neurosci. 2005 Jul;22(1):21-7.

PMID:
16029192
40.
41.

NF-(kappa)B mediates amyloid beta peptide-stimulated activity of the human apolipoprotein E gene promoter in human astroglial cells.

Du Y, Chen X, Wei X, Bales KR, Berg DT, Paul SM, Farlow MR, Maloney B, Ge YW, Lahiri DK.

Brain Res Mol Brain Res. 2005 May 20;136(1-2):177-88.

PMID:
15893602
42.

The low density lipoprotein receptor regulates the level of central nervous system human and murine apolipoprotein E but does not modify amyloid plaque pathology in PDAPP mice.

Fryer JD, Demattos RB, McCormick LM, O'Dell MA, Spinner ML, Bales KR, Paul SM, Sullivan PM, Parsadanian M, Bu G, Holtzman DM.

J Biol Chem. 2005 Jul 8;280(27):25754-9. Epub 2005 May 11.

43.

Human apolipoprotein E4 alters the amyloid-beta 40:42 ratio and promotes the formation of cerebral amyloid angiopathy in an amyloid precursor protein transgenic model.

Fryer JD, Simmons K, Parsadanian M, Bales KR, Paul SM, Sullivan PM, Holtzman DM.

J Neurosci. 2005 Mar 16;25(11):2803-10.

44.

Anti-Abeta antibody treatment promotes the rapid recovery of amyloid-associated neuritic dystrophy in PDAPP transgenic mice.

Brendza RP, Bacskai BJ, Cirrito JR, Simmons KA, Skoch JM, Klunk WE, Mathis CA, Bales KR, Paul SM, Hyman BT, Holtzman DM.

J Clin Invest. 2005 Feb;115(2):428-33.

45.

Exacerbation of cerebral amyloid angiopathy-associated microhemorrhage in amyloid precursor protein transgenic mice by immunotherapy is dependent on antibody recognition of deposited forms of amyloid beta.

Racke MM, Boone LI, Hepburn DL, Parsadainian M, Bryan MT, Ness DK, Piroozi KS, Jordan WH, Brown DD, Hoffman WP, Holtzman DM, Bales KR, Gitter BD, May PC, Paul SM, DeMattos RB.

J Neurosci. 2005 Jan 19;25(3):629-36.

47.

ApoAI deficiency results in marked reductions in plasma cholesterol but no alterations in amyloid-beta pathology in a mouse model of Alzheimer's disease-like cerebral amyloidosis.

Fagan AM, Christopher E, Taylor JW, Parsadanian M, Spinner M, Watson M, Fryer JD, Wahrle S, Bales KR, Paul SM, Holtzman DM.

Am J Pathol. 2004 Oct;165(4):1413-22.

48.

Cognitive impairment in PDAPP mice depends on ApoE and ACT-catalyzed amyloid formation.

Nilsson LN, Arendash GW, Leighty RE, Costa DA, Low MA, Garcia MF, Cracciolo JR, Rojiani A, Wu X, Bales KR, Paul SM, Potter H.

Neurobiol Aging. 2004 Oct;25(9):1153-67.

PMID:
15312961
49.

Use of multimetric statistical analysis to characterize and discriminate between the performance of four Alzheimer's transgenic mouse lines differing in Abeta deposition.

Leighty RE, Nilsson LN, Potter H, Costa DA, Low MA, Bales KR, Paul SM, Arendash GW.

Behav Brain Res. 2004 Aug 12;153(1):107-21.

PMID:
15219712
50.

Neurodegenerative disease research in the 21st century.

Bales KR.

Drug Discov Today. 2004 Jul 1;9(13):553-6. No abstract available.

PMID:
15203090

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