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Items: 47

1.

Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.

Mandal M, Mitra K, Grotz D, Lin X, Palamanda J, Kumari P, Buevich A, Caldwell JP, Chen X, Cox K, Favreau L, Hyde L, Kennedy ME, Kuvelkar R, Liu X, Mazzola RD, Parker E, Rindgen D, Sherer E, Wang H, Zhu Z, Stamford AW, Cumming JN.

J Med Chem. 2018 Nov 15. doi: 10.1021/acs.jmedchem.8b01326. [Epub ahead of print]

PMID:
30388368
2.

Extending a Systems Model of the APP Pathway: Separation of β- and γ-Secretase Sequential Cleavage Steps of APP.

van Maanen EMT, van Steeg TJ, Ahsman MJ, Michener MS, Savage MJ, Kennedy ME, Kleijn HJ, Stone J, Danhof M.

J Pharmacol Exp Ther. 2018 Jun;365(3):507-518. doi: 10.1124/jpet.117.244699. Epub 2018 Mar 21.

PMID:
29563326
3.

Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-AβPPswe Mice Without Inducing Microhemorrhage.

Villarreal S, Zhao F, Hyde LA, Holder D, Forest T, Sondey M, Chen X, Sur C, Parker EM, Kennedy ME.

J Alzheimers Dis. 2017;59(4):1393-1413. doi: 10.3233/JAD-170056.

4.

Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.

Scott JD, DeMong DE, Greshock TJ, Basu K, Dai X, Harris J, Hruza A, Li SW, Lin SI, Liu H, Macala MK, Hu Z, Mei H, Zhang H, Walsh P, Poirier M, Shi ZC, Xiao L, Agnihotri G, Baptista MA, Columbus J, Fell MJ, Hyde LA, Kuvelkar R, Lin Y, Mirescu C, Morrow JA, Yin Z, Zhang X, Zhou X, Chang RK, Embrey MW, Sanders JM, Tiscia HE, Drolet RE, Kern JT, Sur SM, Renger JJ, Bilodeau MT, Kennedy ME, Parker EM, Stamford AW, Nargund R, McCauley JA, Miller MW.

J Med Chem. 2017 Apr 13;60(7):2983-2992. doi: 10.1021/acs.jmedchem.7b00045. Epub 2017 Mar 16.

PMID:
28245354
5.

Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease.

Scott JD, Li SW, Brunskill AP, Chen X, Cox K, Cumming JN, Forman M, Gilbert EJ, Hodgson RA, Hyde LA, Jiang Q, Iserloh U, Kazakevich I, Kuvelkar R, Mei H, Meredith J, Misiaszek J, Orth P, Rossiter LM, Slater M, Stone J, Strickland CO, Voigt JH, Wang G, Wang H, Wu Y, Greenlee WJ, Parker EM, Kennedy ME, Stamford AW.

J Med Chem. 2016 Dec 8;59(23):10435-10450. Epub 2016 Nov 18.

PMID:
27933948
6.

The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients.

Kennedy ME, Stamford AW, Chen X, Cox K, Cumming JN, Dockendorf MF, Egan M, Ereshefsky L, Hodgson RA, Hyde LA, Jhee S, Kleijn HJ, Kuvelkar R, Li W, Mattson BA, Mei H, Palcza J, Scott JD, Tanen M, Troyer MD, Tseng JL, Stone JA, Parker EM, Forman MS.

Sci Transl Med. 2016 Nov 2;8(363):363ra150.

PMID:
27807285
7.

Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.

Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW.

J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22.

PMID:
26937601
8.

Systems Pharmacology Analysis of the Amyloid Cascade after β-Secretase Inhibition Enables the Identification of an Aβ42 Oligomer Pool.

van Maanen EM, van Steeg TJ, Michener MS, Savage MJ, Kennedy ME, Kleijn HJ, Stone JA, Danhof M.

J Pharmacol Exp Ther. 2016 Apr;357(1):205-16. doi: 10.1124/jpet.115.230565. Epub 2016 Jan 29.

PMID:
26826190
9.

MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition.

Fell MJ, Mirescu C, Basu K, Cheewatrakoolpong B, DeMong DE, Ellis JM, Hyde LA, Lin Y, Markgraf CG, Mei H, Miller M, Poulet FM, Scott JD, Smith MD, Yin Z, Zhou X, Parker EM, Kennedy ME, Morrow JA.

J Pharmacol Exp Ther. 2015 Dec;355(3):397-409. doi: 10.1124/jpet.115.227587. Epub 2015 Sep 25.

PMID:
26407721
10.

CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition.

Dobrowolska JA, Michener MS, Wu G, Patterson BW, Chott R, Ovod V, Pyatkivskyy Y, Wildsmith KR, Kasten T, Mathers P, Dancho M, Lennox C, Smith BE, Gilberto D, McLoughlin D, Holder DJ, Stamford AW, Yarasheski KE, Kennedy ME, Savage MJ, Bateman RJ.

J Neurosci. 2014 Jun 11;34(24):8336-46. doi: 10.1523/JNEUROSCI.0540-14.2014.

11.

Function, therapeutic potential and cell biology of BACE proteases: current status and future prospects.

Vassar R, Kuhn PH, Haass C, Kennedy ME, Rajendran L, Wong PC, Lichtenthaler SF.

J Neurochem. 2014 Jul;130(1):4-28. doi: 10.1111/jnc.12715. Epub 2014 Apr 19. Review.

12.

Methylation of promoters of microRNAs and their host genes in myelodysplastic syndromes.

Erdogan B, Bosompem A, Peng D, Han L, Smith E, Kennedy ME, Alford CE, Wu H, Zhao Z, Mosse CA, El-Rifai W, Kim AS.

Leuk Lymphoma. 2013 Dec;54(12):2720-7. doi: 10.3109/10428194.2013.790542. Epub 2013 May 15.

13.

Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction.

Stamford AW, Scott JD, Li SW, Babu S, Tadesse D, Hunter R, Wu Y, Misiaszek J, Cumming JN, Gilbert EJ, Huang C, McKittrick BA, Hong L, Guo T, Zhu Z, Strickland C, Orth P, Voigt JH, Kennedy ME, Chen X, Kuvelkar R, Hodgson R, Hyde LA, Cox K, Favreau L, Parker EM, Greenlee WJ.

ACS Med Chem Lett. 2012 Nov 8;3(11):897-902. Epub 2012 Jul 12.

14.

Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.

Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW.

J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1.

PMID:
22989333
15.

Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.

Cumming JN, Smith EM, Wang L, Misiaszek J, Durkin J, Pan J, Iserloh U, Wu Y, Zhu Z, Strickland C, Voigt J, Chen X, Kennedy ME, Kuvelkar R, Hyde LA, Cox K, Favreau L, Czarniecki MF, Greenlee WJ, McKittrick BA, Parker EM, Stamford AW.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2444-9. doi: 10.1016/j.bmcl.2012.02.013. Epub 2012 Feb 16.

PMID:
22390835
16.

Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors.

Wang YS, Strickland C, Voigt JH, Kennedy ME, Beyer BM, Senior MM, Smith EM, Nechuta TL, Madison VS, Czarniecki M, McKittrick BA, Stamford AW, Parker EM, Hunter JC, Greenlee WJ, Wyss DF.

J Med Chem. 2010 Feb 11;53(3):942-50. doi: 10.1021/jm901472u.

PMID:
20043700
17.

Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.

Zhu Z, Sun ZY, Ye Y, Voigt J, Strickland C, Smith EM, Cumming J, Wang L, Wong J, Wang YS, Wyss DF, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Parker E, McKittrick BA, Stamford A, Czarniecki M, Greenlee W, Hunter JC.

J Med Chem. 2010 Feb 11;53(3):951-65. doi: 10.1021/jm901408p.

PMID:
20043696
18.

Antitumour and antimalarial activity of artemisinin-acridine hybrids.

Jones M, Mercer AE, Stocks PA, La Pensée LJ, Cosstick R, Park BK, Kennedy ME, Piantanida I, Ward SA, Davies J, Bray PG, Rawe SL, Baird J, Charidza T, Janneh O, O'Neill PM.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2033-7. doi: 10.1016/j.bmcl.2009.02.028. Epub 2009 Feb 11.

PMID:
19249201
19.

Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.

Cumming JN, Le TX, Babu S, Carroll C, Chen X, Favreau L, Gaspari P, Guo T, Hobbs DW, Huang Y, Iserloh U, Kennedy ME, Kuvelkar R, Li G, Lowrie J, McHugh NA, Ozgur L, Pan J, Parker EM, Saionz K, Stamford AW, Strickland C, Tadesse D, Voigt J, Wang L, Wu Y, Zhang L, Zhang Q.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3236-41. doi: 10.1016/j.bmcl.2008.04.050. Epub 2008 Apr 25. Erratum in: Bioorg Med Chem Lett. 2008 Aug 1;18(15):4447.

PMID:
18468890
20.

Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.

Iserloh U, Wu Y, Cumming JN, Pan J, Wang LY, Stamford AW, Kennedy ME, Kuvelkar R, Chen X, Parker EM, Strickland C, Voigt J.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):414-7. Epub 2007 Nov 6.

PMID:
18023580
21.

Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.

Iserloh U, Pan J, Stamford AW, Kennedy ME, Zhang Q, Zhang L, Parker EM, McHugh NA, Favreau L, Strickland C, Voigt J.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):418-22. Epub 2007 Oct 18.

PMID:
17980584
22.

Design and development of BACE-1 inhibitors.

Cumming JN, Iserloh U, Kennedy ME.

Curr Opin Drug Discov Devel. 2004 Jul;7(4):536-56. Review.

PMID:
15338962
23.

Measuring human beta-secretase (BACE1) activity using homogeneous time-resolved fluorescence.

Kennedy ME, Wang W, Song L, Lee J, Zhang L, Wong G, Wang L, Parker E.

Anal Biochem. 2003 Aug 1;319(1):49-55.

PMID:
12842106
24.

Functional and biochemical evidence for G-protein-gated inwardly rectifying K+ (GIRK) channels composed of GIRK2 and GIRK3.

Jelacic TM, Kennedy ME, Wickman K, Clapham DE.

J Biol Chem. 2000 Nov 17;275(46):36211-6.

25.

GIRK4 confers appropriate processing and cell surface localization to G-protein-gated potassium channels.

Kennedy ME, Nemec J, Corey S, Wickman K, Clapham DE.

J Biol Chem. 1999 Jan 22;274(4):2571-82.

26.

Gbeta binding to GIRK4 subunit is critical for G protein-gated K+ channel activation.

Krapivinsky G, Kennedy ME, Nemec J, Medina I, Krapivinsky L, Clapham DE.

J Biol Chem. 1998 Jul 3;273(27):16946-52.

27.

Burst kinetics of co-expressed Kir6.2/SUR1 clones: comparison of recombinant with native ATP-sensitive K+ channel behavior.

Alekseev AE, Kennedy ME, Navarro B, Terzic A.

J Membr Biol. 1997 Sep 15;159(2):161-8.

PMID:
9307442
28.

Nonselective and G betagamma-insensitive weaver K+ channels.

Navarro B, Kennedy ME, Velimirovíc B, Bhat D, Peterson AS, Clapham DE.

Science. 1996 Jun 28;272(5270):1950-3.

PMID:
8658170
29.

Localization and interaction of epitope-tagged GIRK1 and CIR inward rectifier K+ channel subunits.

Kennedy ME, Nemec J, Clapham DE.

Neuropharmacology. 1996;35(7):831-9.

PMID:
8938714
30.

Sterilization and disinfection of instruments and materials in the surgery unit and laboratory areas.

Best M, Kennedy ME.

Semin Dermatol. 1995 Sep;14(3):243-6. Review. No abstract available.

PMID:
7488542
32.

Recommendations for hantavirus risk reduction.

Artsob H, Kennedy ME.

Can Commun Dis Rep. 1994 Aug 15;20(15):126-8. English, French. No abstract available.

PMID:
7920364
33.

The effects of ultrasound irradiation on a biodegradable 50-50% copolymer of polylactic and polyglycolic acids.

Agrawal CM, Kennedy ME, Micallef DM.

J Biomed Mater Res. 1994 Aug;28(8):851-9.

PMID:
7983083
36.

Effectiveness of handwashing agents in eliminating Staphylococcus aureus from gloved hands.

Best M, Kennedy ME.

J Appl Bacteriol. 1992 Jul;73(1):63-6.

PMID:
1512180
37.

Synthesis of a yohimbine-agarose matrix useful for large-scale and micropurification of multiple alpha 2-receptor subtypes.

Domino SE, Repaske MG, Bonner CA, Kennedy ME, Wilson AL, Brandon S, Limbird LE.

Methods Enzymol. 1992;215:181-200.

PMID:
1359387
38.

Human platelet/erythroleukemia cell prostaglandin G/H synthase: cDNA cloning, expression, and gene chromosomal assignment.

Funk CD, Funk LB, Kennedy ME, Pong AS, Fitzgerald GA.

FASEB J. 1991 Jun;5(9):2304-12.

PMID:
1907252
39.

Efficacies of selected disinfectants against Mycobacterium tuberculosis.

Best M, Sattar SA, Springthorpe VS, Kennedy ME.

J Clin Microbiol. 1990 Oct;28(10):2234-9.

40.

Efficacy of a variety of disinfectants against Listeria spp.

Best M, Kennedy ME, Coates F.

Appl Environ Microbiol. 1990 Feb;56(2):377-80.

41.

Comparative mycobactericidal efficacy of chemical disinfectants in suspension and carrier tests.

Best M, Sattar SA, Springthorpe VS, Kennedy ME.

Appl Environ Microbiol. 1988 Nov;54(11):2856-8.

42.

The major heat-shock protein (hsp70) gene family: related sequences in mouse, Drosophila, and yeast.

Moran LA, Chauvin M, Kennedy ME, Korri M, Lowe DG, Nicholson RC, Perry MD.

Can J Biochem Cell Biol. 1983 Jun;61(6):488-99.

PMID:
6349754
43.

The dexamethasone suppression test in depressed outpatients with and without melancholia.

Jaffe K, Barnshaw HD, Kennedy ME.

Am J Psychiatry. 1983 Apr;140(4):492-3. No abstract available.

PMID:
6837794
44.

Salmonella isolations from snakes and other reptiles.

Kennedy ME.

Can J Comp Med. 1973 Jul;37(3):325-6.

45.

Salmonella serotypes isolated from turtle environment.

Kennedy ME.

Can J Microbiol. 1969 Jan;15(1):130-2. No abstract available.

PMID:
5765171
46.

Microflora of crêpe rubber.

TURNER JN, KENNEDY ME.

Nature. 1954 Mar 13;173(4402):506. No abstract available.

PMID:
13144795
47.

Administration and methods of enumeration of the sickness surveys in Alberta.

KENNEDY ME.

Can J Public Health. 1953 May;44(5):177-9. No abstract available.

PMID:
13051747

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