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Items: 14

1.

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
2.

Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.

Stachel SJ, Zerbinatti C, Rudd MT, Cosden M, Suon S, Nanda KK, Wessner K, DiMuzio J, Maxwell J, Wu Z, Uslaner JM, Michener MS, Szczerba P, Brnardic E, Rada V, Kim Y, Meissner R, Wuelfing P, Yuan Y, Ballard J, Holahan M, Klein DJ, Lu J, Fradera X, Parthasarathy G, Uebele VN, Chen Z, Li Y, Li J, Cooke AJ, Bennett DJ, Bilodeau MT, Renger J.

J Med Chem. 2016 Apr 14;59(7):3489-98. doi: 10.1021/acs.jmedchem.6b00176. Epub 2016 Apr 1.

PMID:
27011007
3.

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
4.

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
5.

Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys.

Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Hayashi I, Hughes BL, Moxham CM, Bays NW, Smotrov N, Hill AD, Pan BS, Wu Z, Moy LY, Tanga F, Kenific C, Cruz JC, Walker D, Bouthillette M, Nikov GN, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Michener MS, Cook JJ, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3488-94. doi: 10.1016/j.bmcl.2015.07.003. Epub 2015 Jul 9.

PMID:
26212776
6.

Platelet transfusion reverses bleeding evoked by triple anti-platelet therapy including vorapaxar, a novel platelet thrombin receptor antagonist.

Cai TQ, Wickham LA, Sitko G, Michener MS, Raubertas R, Handt L, Chintala M, Seiffert D, Forrest M.

Eur J Pharmacol. 2015 Jul 5;758:107-14. doi: 10.1016/j.ejphar.2015.03.073. Epub 2015 Apr 7.

PMID:
25857224
7.

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.

8.

GAD65 autoantibodies in Kleine-Levin syndrome.

Rout UK, Michener MS, Dhossche DM.

J Neuropsychiatry Clin Neurosci. 2014 Apr 1;26(2):E49-51. doi: 10.1176/appi.neuropsych.13050110. No abstract available.

PMID:
24763794
9.

Characterization of plasma β-secretase (BACE1) activity and soluble amyloid precursor proteins as potential biomarkers for Alzheimer's disease.

Wu G, Sankaranarayanan S, Wong J, Tugusheva K, Michener MS, Shi X, Cook JJ, Simon AJ, Savage MJ.

J Neurosci Res. 2012 Dec;90(12):2247-58. doi: 10.1002/jnr.23122. Epub 2012 Sep 18.

PMID:
22987781
10.

Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound.

Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, Wang JX, Wu G, Yarasheski KE, Bateman RJ.

J Neurosci. 2010 May 12;30(19):6743-50. doi: 10.1523/JNEUROSCI.1381-10.2010.

11.

Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.

Zhu H, Young MB, Nantermet PG, Graham SL, Colussi D, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Shi XP, Tugusheva K, Holahan MA, Michener MS, Cook JJ, Simon A, Hazuda DJ, Vacca JP, Rajapakse HA.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1779-82. doi: 10.1016/j.bmcl.2010.01.005. Epub 2010 Jan 11.

PMID:
20122828
12.

Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.

Salvatore CA, Moore EL, Calamari A, Cook JJ, Michener MS, O'Malley S, Miller PJ, Sur C, Williams DL Jr, Zeng Z, Danziger A, Lynch JJ, Regan CP, Fay JF, Tang YS, Li CC, Pudvah NT, White RB, Bell IM, Gallicchio SN, Graham SL, Selnick HG, Vacca JP, Kane SA.

J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. doi: 10.1124/jpet.109.163816. Epub 2010 Jan 11.

PMID:
20065019
13.

Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid concentrations in rhesus monkeys.

Tang C, Kuo Y, Pudvah NT, Ellis JD, Michener MS, Egbertson M, Graham SL, Cook JJ, Hochman JH, Prueksaritanont T.

Biochem Pharmacol. 2009 Sep 15;78(6):642-7. doi: 10.1016/j.bcp.2009.05.026. Epub 2009 May 27.

PMID:
19481060
14.

Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing.

Nantermet PG, Rajapakse HA, Stanton MG, Stauffer SR, Barrow JC, Gregro AR, Moore KP, Steinbeiser MA, Swestock J, Selnick HG, Graham SL, McGaughey GB, Colussi D, Lai MT, Sankaranarayanan S, Simon AJ, Munshi S, Cook JJ, Holahan MA, Michener MS, Vacca JP.

ChemMedChem. 2009 Jan;4(1):37-40. doi: 10.1002/cmdc.200800308. No abstract available.

PMID:
19085994

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