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Items: 1 to 50 of 91

1.

Amyloid-β plaques enhance Alzheimer's brain tau-seeded pathologies by facilitating neuritic plaque tau aggregation.

He Z, Guo JL, McBride JD, Narasimhan S, Kim H, Changolkar L, Zhang B, Gathagan RJ, Yue C, Dengler C, Stieber A, Nitla M, Coulter DA, Abel T, Brunden KR, Trojanowski JQ, Lee VM.

Nat Med. 2018 Jan;24(1):29-38. doi: 10.1038/nm.4443. Epub 2017 Dec 4.

PMID:
29200205
2.

Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.

Lassalas P, Oukoloff K, Makani V, James M, Tran V, Yao Y, Huang L, Vijayendran K, Monti L, Trojanowski JQ, Lee VM, Kozlowski MC, Smith AB 3rd, Brunden KR, Ballatore C.

ACS Med Chem Lett. 2017 Jul 5;8(8):864-868. doi: 10.1021/acsmedchemlett.7b00212. eCollection 2017 Aug 10.

PMID:
28835803
3.

Multitargeted Imidazoles: Potential Therapeutic Leads for Alzheimer's and Other Neurodegenerative Diseases.

Cornec AS, Monti L, Kovalevich J, Makani V, James MJ, Vijayendran KG, Oukoloff K, Yao Y, Lee VM, Trojanowski JQ, Smith AB 3rd, Brunden KR, Ballatore C.

J Med Chem. 2017 Jun 22;60(12):5120-5145. doi: 10.1021/acs.jmedchem.7b00475. Epub 2017 Jun 8.

4.

Non-Naturally Occurring Small Molecule Microtubule-Stabilizing Agents: A Potential Tactic for CNS-Directed Therapies.

Ballatore C, Brunden KR, Trojanowski JQ, Lee VM, Smith AB 3rd.

ACS Chem Neurosci. 2017 Jan 18;8(1):5-7. doi: 10.1021/acschemneuro.6b00384. Epub 2016 Nov 29. Review.

5.

Altered microtubule dynamics in neurodegenerative disease: Therapeutic potential of microtubule-stabilizing drugs.

Brunden KR, Lee VM, Smith AB 3rd, Trojanowski JQ, Ballatore C.

Neurobiol Dis. 2017 Sep;105:328-335. doi: 10.1016/j.nbd.2016.12.021. Epub 2016 Dec 22. Review.

PMID:
28012891
6.

Therapeutic strategies for the treatment of tauopathies: Hopes and challenges.

Khanna MR, Kovalevich J, Lee VM, Trojanowski JQ, Brunden KR.

Alzheimers Dement. 2016 Oct;12(10):1051-1065. doi: 10.1016/j.jalz.2016.06.006. Review.

7.

Evaluation of the brain-penetrant microtubule-stabilizing agent, dictyostatin, in the PS19 tau transgenic mouse model of tauopathy.

Makani V, Zhang B, Han H, Yao Y, Lassalas P, Lou K, Paterson I, Lee VM, Trojanowski JQ, Ballatore C, Smith AB 3rd, Brunden KR.

Acta Neuropathol Commun. 2016 Sep 29;4(1):106.

8.

The Dynamics and Turnover of Tau Aggregates in Cultured Cells: INSIGHTS INTO THERAPIES FOR TAUOPATHIES.

Guo JL, Buist A, Soares A, Callaerts K, Calafate S, Stevenaert F, Daniels JP, Zoll BE, Crowe A, Brunden KR, Moechars D, Lee VM.

J Biol Chem. 2016 Jun 17;291(25):13175-93. doi: 10.1074/jbc.M115.712083. Epub 2016 Apr 18.

9.

Characterization of Brain-Penetrant Pyrimidine-Containing Molecules with Differential Microtubule-Stabilizing Activities Developed as Potential Therapeutic Agents for Alzheimer's Disease and Related Tauopathies.

Kovalevich J, Cornec AS, Yao Y, James M, Crowe A, Lee VM, Trojanowski JQ, Smith AB 3rd, Ballatore C, Brunden KR.

J Pharmacol Exp Ther. 2016 May;357(2):432-50. doi: 10.1124/jpet.115.231175. Epub 2016 Mar 15.

10.

Structure Property Relationships of Carboxylic Acid Isosteres.

Lassalas P, Gay B, Lasfargeas C, James MJ, Tran V, Vijayendran KG, Brunden KR, Kozlowski MC, Thomas CJ, Smith AB 3rd, Huryn DM, Ballatore C.

J Med Chem. 2016 Apr 14;59(7):3183-203. doi: 10.1021/acs.jmedchem.5b01963. Epub 2016 Mar 30.

11.

Inflammatory Eicosanoids Increase Amyloid Precursor Protein Expression via Activation of Multiple Neuronal Receptors.

Herbst-Robinson KJ, Liu L, James M, Yao Y, Xie SX, Brunden KR.

Sci Rep. 2015 Dec 17;5:18286. doi: 10.1038/srep18286.

12.

Passive immunization with phospho-tau antibodies reduces tau pathology and functional deficits in two distinct mouse tauopathy models.

Sankaranarayanan S, Barten DM, Vana L, Devidze N, Yang L, Cadelina G, Hoque N, DeCarr L, Keenan S, Lin A, Cao Y, Snyder B, Zhang B, Nitla M, Hirschfeld G, Barrezueta N, Polson C, Wes P, Rangan VS, Cacace A, Albright CF, Meredith J Jr, Trojanowski JQ, Lee VM, Brunden KR, Ahlijanian M.

PLoS One. 2015 May 1;10(5):e0125614. doi: 10.1371/journal.pone.0125614. eCollection 2015.

13.

Pharmacokinetic, pharmacodynamic and metabolic characterization of a brain retentive microtubule (MT)-stabilizing triazolopyrimidine.

Cornec AS, James MJ, Kovalevich J, Trojanowski JQ, Lee VM, Smith AB 3rd, Ballatore C, Brunden KR.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4980-2. doi: 10.1016/j.bmcl.2015.03.002. Epub 2015 Mar 14.

14.

Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.

Wang X, Liu L, Huang L, Herbst-Robinson K, Cornec AS, James MJ, Sugiyama S, Bassetto M, Brancale A, Trojanowski JQ, Lee VM, Smith AB 3rd, Brunden KR, Ballatore C.

ACS Med Chem Lett. 2014 Jul 24;5(9):1015-20. doi: 10.1021/ml5002085. eCollection 2014 Sep 11.

15.

Intracerebral injection of preformed synthetic tau fibrils initiates widespread tauopathy and neuronal loss in the brains of tau transgenic mice.

Peeraer E, Bottelbergs A, Van Kolen K, Stancu IC, Vasconcelos B, Mahieu M, Duytschaever H, Ver Donck L, Torremans A, Sluydts E, Van Acker N, Kemp JA, Mercken M, Brunden KR, Trojanowski JQ, Dewachter I, Lee VM, Moechars D.

Neurobiol Dis. 2015 Jan;73:83-95. doi: 10.1016/j.nbd.2014.08.032. Epub 2014 Sep 16.

16.

Evaluation of the cyclopentane-1,2-dione as a potential bio-isostere of the carboxylic acid functional group.

Ballatore C, Gay B, Huang L, Robinson KH, James MJ, Trojanowski JQ, Lee VM, Brunden KR, Smith AB 3rd.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4171-5. doi: 10.1016/j.bmcl.2014.07.047. Epub 2014 Jul 23.

17.

Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.

Lou K, Yao Y, Hoye AT, James MJ, Cornec AS, Hyde E, Gay B, Lee VM, Trojanowski JQ, Smith AB 3rd, Brunden KR, Ballatore C.

J Med Chem. 2014 Jul 24;57(14):6116-27. doi: 10.1021/jm5005623. Epub 2014 Jul 3.

18.

MT-Stabilizer, Dictyostatin, Exhibits Prolonged Brain Retention and Activity: Potential Therapeutic Implications.

Brunden KR, Gardner NM, James MJ, Yao Y, Trojanowski JQ, Lee VM, Paterson I, Ballatore C, Smith AB 3rd.

ACS Med Chem Lett. 2013 Jul 23;4(9):886-9. doi: 10.1021/ml400233e. eCollection 2013 Sep 12.

19.

Microtubule-stabilizing agents as potential therapeutics for neurodegenerative disease.

Brunden KR, Trojanowski JQ, Smith AB 3rd, Lee VM, Ballatore C.

Bioorg Med Chem. 2014 Sep 15;22(18):5040-9. doi: 10.1016/j.bmc.2013.12.046. Epub 2013 Dec 30. Review.

20.

Aminothienopyridazines as imaging probes of tau pathology: a patent evaluation of WO2013090497.

Ballatore C, Smith AB 3rd, Lee VM, Trojanowski JQ, Brunden KR.

Expert Opin Ther Pat. 2014 Mar;24(3):355-60. doi: 10.1517/13543776.2014.871526. Epub 2014 Jan 3.

21.

Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3β inhibitors.

La Pietra V, La Regina G, Coluccia A, Famiglini V, Pelliccia S, Plotkin B, Eldar-Finkelman H, Brancale A, Ballatore C, Crowe A, Brunden KR, Marinelli L, Novellino E, Silvestri R.

J Med Chem. 2013 Dec 27;56(24):10066-78. doi: 10.1021/jm401466v. Epub 2013 Dec 11.

PMID:
24295046
22.

Response to comments on "ApoE-directed therapeutics rapidly clear β-amyloid and reverse deficits in AD mouse models".

Landreth GE, Cramer PE, Lakner MM, Cirrito JR, Wesson DW, Brunden KR, Wilson DA.

Science. 2013 May 24;340(6135):924-g. doi: 10.1126/science.1234114.

23.

Lewy body-like α-synuclein aggregates resist degradation and impair macroautophagy.

Tanik SA, Schultheiss CE, Volpicelli-Daley LA, Brunden KR, Lee VM.

J Biol Chem. 2013 May 24;288(21):15194-210. doi: 10.1074/jbc.M113.457408. Epub 2013 Mar 26.

24.

Aminothienopyridazines and methylene blue affect Tau fibrillization via cysteine oxidation.

Crowe A, James MJ, Lee VM, Smith AB 3rd, Trojanowski JQ, Ballatore C, Brunden KR.

J Biol Chem. 2013 Apr 19;288(16):11024-37. doi: 10.1074/jbc.M112.436006. Epub 2013 Feb 26.

25.

Brain-penetrant tetrahydronaphthalene thromboxane A2-prostanoid (TP) receptor antagonists as prototype therapeutics for Alzheimer's disease.

Soper JH, Sugiyama S, Herbst-Robinson K, James MJ, Wang X, Trojanowski JQ, Smith AB 3rd, Lee VM, Ballatore C, Brunden KR.

ACS Chem Neurosci. 2012 Nov 21;3(11):928-40. doi: 10.1021/cn3000795. Epub 2012 Jul 27.

26.

A model for improving the treatment and care of Alzheimer's disease patients through interdisciplinary research.

Trojanowski JQ, Arnold SE, Karlawish JH, Naylor M, Brunden KR, Lee VM.

Alzheimers Dement. 2012 Nov;8(6):564-73. doi: 10.1016/j.jalz.2011.08.005.

27.

Microtubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathies.

Ballatore C, Brunden KR, Huryn DM, Trojanowski JQ, Lee VM, Smith AB 3rd.

J Med Chem. 2012 Nov 8;55(21):8979-96. doi: 10.1021/jm301079z. Epub 2012 Sep 28. Review.

28.

Advancing Alzheimer's disease diagnosis, treatment, and care: recommendations from the Ware Invitational Summit.

Naylor MD, Karlawish JH, Arnold SE, Khachaturian AS, Khachaturian ZS, Lee VM, Baumgart M, Banerjee S, Beck C, Blennow K, Brookmeyer R, Brunden KR, Buckwalter KC, Comer M, Covinsky K, Feinberg LF, Frisoni G, Green C, Guimaraes RM, Gwyther LP, Hefti FF, Hutton M, Kawas C, Kent DM, Kuller L, Langa KM, Mahley RW, Maslow K, Masters CL, Meier DE, Neumann PJ, Paul SM, Petersen RC, Sager MA, Sano M, Schenk D, Soares H, Sperling RA, Stahl SM, van Deerlin V, Stern Y, Weir D, Wolk DA, Trojanowski JQ.

Alzheimers Dement. 2012 Sep;8(5):445-52. doi: 10.1016/j.jalz.2012.08.001.

29.

Brain-penetrant microtubule-stabilizing compounds as potential therapeutic agents for tauopathies.

Brunden KR, Ballatore C, Lee VM, Smith AB 3rd, Trojanowski JQ.

Biochem Soc Trans. 2012 Aug;40(4):661-6. doi: 10.1042/BST20120010. Review.

30.

Aminothienopyridazine inhibitors of tau aggregation: evaluation of structure-activity relationship leads to selection of candidates with desirable in vivo properties.

Ballatore C, Crowe A, Piscitelli F, James M, Lou K, Rossidivito G, Yao Y, Trojanowski JQ, Lee VM, Brunden KR, Smith AB 3rd.

Bioorg Med Chem. 2012 Jul 15;20(14):4451-61. doi: 10.1016/j.bmc.2012.05.027. Epub 2012 May 23.

31.

The microtubule-stabilizing agent, epothilone D, reduces axonal dysfunction, neurotoxicity, cognitive deficits, and Alzheimer-like pathology in an interventional study with aged tau transgenic mice.

Zhang B, Carroll J, Trojanowski JQ, Yao Y, Iba M, Potuzak JS, Hogan AM, Xie SX, Ballatore C, Smith AB 3rd, Lee VM, Brunden KR.

J Neurosci. 2012 Mar 14;32(11):3601-11. doi: 10.1523/JNEUROSCI.4922-11.2012.

32.

ApoE-directed therapeutics rapidly clear β-amyloid and reverse deficits in AD mouse models.

Cramer PE, Cirrito JR, Wesson DW, Lee CY, Karlo JC, Zinn AE, Casali BT, Restivo JL, Goebel WD, James MJ, Brunden KR, Wilson DA, Landreth GE.

Science. 2012 Mar 23;335(6075):1503-6. doi: 10.1126/science.1217697. Epub 2012 Feb 9.

33.

Developing therapeutic approaches to tau, selected kinases, and related neuronal protein targets.

Lee VM, Brunden KR, Hutton M, Trojanowski JQ.

Cold Spring Harb Perspect Med. 2011 Sep;1(1):a006437. doi: 10.1101/cshperspect.a006437. Review.

34.

Chronic stress exacerbates tau pathology, neurodegeneration, and cognitive performance through a corticotropin-releasing factor receptor-dependent mechanism in a transgenic mouse model of tauopathy.

Carroll JC, Iba M, Bangasser DA, Valentino RJ, James MJ, Brunden KR, Lee VM, Trojanowski JQ.

J Neurosci. 2011 Oct 5;31(40):14436-49. doi: 10.1523/JNEUROSCI.3836-11.2011.

35.

Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists.

Ballatore C, Soper JH, Piscitelli F, James M, Huang L, Atasoylu O, Huryn DM, Trojanowski JQ, Lee VM, Brunden KR, Smith AB.

J Med Chem. 2011 Oct 13;54(19):6969-83. doi: 10.1021/jm200980u. Epub 2011 Sep 9.

36.

High Throughput Screening for Small Molecule Inhibitors of Heparin-induced Tau Fibril Formation.

Johnson RL, Huang W, Huang R, Crowe A, Ballatore C, Trojanowski JQ, Brunden KR, Lee VMY.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 May 18 [updated 2010 Sep 2].

37.

Modulation of protein-protein interactions as a therapeutic strategy for the treatment of neurodegenerative tauopathies.

Ballatore C, Brunden KR, Trojanowski JQ, Lee VM, Smith AB 3rd, Huryn DM.

Curr Top Med Chem. 2011;11(3):317-30. Review.

38.

The characterization of microtubule-stabilizing drugs as possible therapeutic agents for Alzheimer's disease and related tauopathies.

Brunden KR, Yao Y, Potuzak JS, Ferrer NI, Ballatore C, James MJ, Hogan AM, Trojanowski JQ, Smith AB 3rd, Lee VM.

Pharmacol Res. 2011 Apr;63(4):341-51. doi: 10.1016/j.phrs.2010.12.002. Epub 2010 Dec 14.

39.

Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy.

Brunden KR, Zhang B, Carroll J, Yao Y, Potuzak JS, Hogan AM, Iba M, James MJ, Xie SX, Ballatore C, Smith AB 3rd, Lee VM, Trojanowski JQ.

J Neurosci. 2010 Oct 13;30(41):13861-6. doi: 10.1523/JNEUROSCI.3059-10.2010.

40.

Investigation of 4-piperidinols as novel H3 antagonists.

Anderson JT, Campbell M, Wang J, Brunden KR, Harrington JJ, Stricker-Krongrad A, Song J, Doucette C, Murphy S, Bennani YL.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6246-9. doi: 10.1016/j.bmcl.2010.08.099. Epub 2010 Aug 24.

PMID:
20833043
41.

3-Indolyl sultams as selective CRTh2 antagonists.

Tumey LN, Robarge MJ, Gleason E, Song J, Murphy SM, Ekema G, Doucette C, Hanniford D, Palmer M, Pawlowski G, Danzig J, Loftus M, Hunady K, Sherf B, Mays RW, Stricker-Krongrad A, Brunden KR, Bennani YL, Harrington JJ.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3287-90. doi: 10.1016/j.bmcl.2010.04.046. Epub 2010 Apr 14.

PMID:
20457519
42.

Discovery of brain-penetrant, orally bioavailable aminothienopyridazine inhibitors of tau aggregation.

Ballatore C, Brunden KR, Piscitelli F, James MJ, Crowe A, Yao Y, Hyde E, Trojanowski JQ, Lee VM, Smith AB 3rd.

J Med Chem. 2010 May 13;53(9):3739-47. doi: 10.1021/jm100138f.

43.

Characterization of tau fibrillization in vitro.

Xu S, Brunden KR, Trojanowski JQ, Lee VM.

Alzheimers Dement. 2010 Mar;6(2):110-7. doi: 10.1016/j.jalz.2009.06.002.

44.

Exogenous alpha-synuclein fibrils seed the formation of Lewy body-like intracellular inclusions in cultured cells.

Luk KC, Song C, O'Brien P, Stieber A, Branch JR, Brunden KR, Trojanowski JQ, Lee VM.

Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20051-6. doi: 10.1073/pnas.0908005106. Epub 2009 Nov 5.

45.

Advances in tau-focused drug discovery for Alzheimer's disease and related tauopathies.

Brunden KR, Trojanowski JQ, Lee VM.

Nat Rev Drug Discov. 2009 Oct;8(10):783-93. doi: 10.1038/nrd2959. Review.

46.

Tau-directed drug discovery for Alzheimer's disease and related tauopathies: a focus on tau assembly inhibitors.

Brunden KR, Ballatore C, Crowe A, Smith AB 3rd, Lee VM, Trojanowski JQ.

Exp Neurol. 2010 Jun;223(2):304-10. doi: 10.1016/j.expneurol.2009.08.031. Epub 2009 Sep 8. Review.

47.

Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening.

Crowe A, Huang W, Ballatore C, Johnson RL, Hogan AM, Huang R, Wichterman J, McCoy J, Huryn D, Auld DS, Smith AB 3rd, Inglese J, Trojanowski JQ, Austin CP, Brunden KR, Lee VM.

Biochemistry. 2009 Aug 18;48(32):7732-45. doi: 10.1021/bi9006435.

48.

GPRC6A null mice exhibit osteopenia, feminization and metabolic syndrome.

Pi M, Chen L, Huang MZ, Zhu W, Ringhofer B, Luo J, Christenson L, Li B, Zhang J, Jackson PD, Faber P, Brunden KR, Harrington JJ, Quarles LD.

PLoS One. 2008;3(12):e3858. doi: 10.1371/journal.pone.0003858. Epub 2008 Dec 3.

49.

Effects of TNFalpha-converting enzyme inhibition on amyloid beta production and APP processing in vitro and in vivo.

Kim ML, Zhang B, Mills IP, Milla ME, Brunden KR, Lee VM.

J Neurosci. 2008 Nov 12;28(46):12052-61. doi: 10.1523/JNEUROSCI.2913-08.2008.

50.

Evidence that non-fibrillar tau causes pathology linked to neurodegeneration and behavioral impairments.

Brunden KR, Trojanowski JQ, Lee VM.

J Alzheimers Dis. 2008 Aug;14(4):393-9. Review.

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