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Items: 1 to 20 of 54

1.

Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.

Wu YJ, Guernon J, Rajamani R, Toyn JH, Ahlijanian MK, Albright CF, Muckelbauer J, Chang C, Camac D, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5729-5731. doi: 10.1016/j.bmcl.2016.10.055. Epub 2016 Oct 20.

PMID:
27816517
2.

Discovery of S3-Truncated, C-6 Heteroaryl Substituted Aminothiazine β-Site APP Cleaving Enzyme-1 (BACE1) Inhibitors.

Wu YJ, Guernon J, Shi J, Marcin L, Higgins M, Rajamani R, Muckelbauer J, Lewis H, Chang C, Camac D, Toyn JH, Ahlijanian MK, Albright CF, Macor JE, Thompson LA.

J Med Chem. 2016 Sep 22;59(18):8593-600. doi: 10.1021/acs.jmedchem.6b01012. Epub 2016 Sep 7.

PMID:
27559936
3.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.

Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF.

J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13.

4.

Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects.

Toyn JH, Boy KM, Raybon J, Meredith JE Jr, Robertson AS, Guss V, Hoque N, Sweeney F, Zhuo X, Clarke W, Snow K, Denton RR, Zuev D, Thompson LA, Morrison J, Grace J, Berisha F, Furlong M, Wang JS, Lentz KA, Padmanabha R, Cook L, Wei C, Drexler DM, Macor JE, Albright CF, Gasior M, Olson RE, Hong Q, Soares HD, AbuTarif M, Ahlijanian MK.

J Pharmacol Exp Ther. 2016 Jul;358(1):125-37. doi: 10.1124/jpet.116.232249. Epub 2016 Apr 20.

5.

The γ-Secretase Modulator, BMS-932481, Modulates Aβ Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers.

Soares HD, Gasior M, Toyn JH, Wang JS, Hong Q, Berisha F, Furlong MT, Raybon J, Lentz KA, Sweeney F, Zheng N, Akinsanya B, Berman RM, Thompson LA, Olson RE, Morrison J, Drexler DM, Macor JE, Albright CF, Ahlijanian MK, AbuTarif M.

J Pharmacol Exp Ther. 2016 Jul;358(1):138-50. doi: 10.1124/jpet.116.232256. Epub 2016 Apr 20.

6.

Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents.

Wu YJ, Guernon J, Yang F, Snyder L, Shi J, Mcclure A, Rajamani R, Park H, Ng A, Lewis H, Chang C, Camac D, Toyn JH, Ahlijanian MK, Albright CF, Macor JE, Thompson LA.

ACS Med Chem Lett. 2016 Jan 11;7(3):271-6. doi: 10.1021/acsmedchemlett.5b00432. eCollection 2016 Mar 10.

7.

Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE).

Boy KM, Guernon JM, Wu YJ, Zhang Y, Shi J, Zhai W, Zhu S, Gerritz SW, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Good AC, Grace JE, Lentz KA, Olson RE, Macor JE, Thompson LA 3rd.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5040-7. doi: 10.1016/j.bmcl.2015.10.031. Epub 2015 Oct 20.

PMID:
26497283
8.

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.

9.

Centrally Delivered BACE1 Inhibitor Activates Microglia, and Reverses Amyloid Pathology and Cognitive Deficit in Aged Tg2576 Mice.

Thakker DR, Sankaranarayanan S, Weatherspoon MR, Harrison J, Pierdomenico M, Heisel JM, Thompson LA, Haskell R, Grace JE, Taylor SJ, Albright CF, Shafer LL.

J Neurosci. 2015 Apr 29;35(17):6931-6. doi: 10.1523/JNEUROSCI.2262-14.2015.

10.

Distinctive transcriptome alterations of prefrontal pyramidal neurons in schizophrenia and schizoaffective disorder.

Arion D, Corradi JP, Tang S, Datta D, Boothe F, He A, Cacace AM, Zaczek R, Albright CF, Tseng G, Lewis DA.

Mol Psychiatry. 2015 Nov;20(11):1397-405. doi: 10.1038/mp.2014.171. Epub 2015 Jan 6.

11.

Tau overexpression impacts a neuroinflammation gene expression network perturbed in Alzheimer's disease.

Wes PD, Easton A, Corradi J, Barten DM, Devidze N, DeCarr LB, Truong A, He A, Barrezueta NX, Polson C, Bourin C, Flynn ME, Keenan S, Lidge R, Meredith J, Natale J, Sankaranarayanan S, Cadelina GW, Albright CF, Cacace AM.

PLoS One. 2014 Aug 25;9(8):e106050. doi: 10.1371/journal.pone.0106050. eCollection 2014. Erratum in: PLoS One. 2015;10(3):e0121509.

12.

Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.

Toyn JH, Thompson LA, Lentz KA, Meredith JE Jr, Burton CR, Sankaranararyanan S, Guss V, Hall T, Iben LG, Krause CM, Krause R, Lin XA, Pierdomenico M, Polson C, Robertson AS, Denton RR, Grace JE, Morrison J, Raybon J, Zhuo X, Snow K, Padmanabha R, Agler M, Esposito K, Harden D, Prack M, Varma S, Wong V, Zhu Y, Zvyaga T, Gerritz S, Marcin LR, Higgins MA, Shi J, Wei C, Cantone JL, Drexler DM, Macor JE, Olson RE, Ahlijanian MK, Albright CF.

Int J Alzheimers Dis. 2014;2014:431858. doi: 10.1155/2014/431858. Epub 2014 Jul 8.

13.

Characterization of novel CSF Tau and ptau biomarkers for Alzheimer's disease.

Meredith JE Jr, Sankaranarayanan S, Guss V, Lanzetti AJ, Berisha F, Neely RJ, Slemmon JR, Portelius E, Zetterberg H, Blennow K, Soares H, Ahlijanian M, Albright CF.

PLoS One. 2013 Oct 7;8(10):e76523. doi: 10.1371/journal.pone.0076523. eCollection 2013.

14.

Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.

Albright CF, Dockens RC, Meredith JE Jr, Olson RE, Slemmon R, Lentz KA, Wang JS, Denton RR, Pilcher G, Rhyne PW, Raybon JJ, Barten DM, Burton C, Toyn JH, Sankaranarayanan S, Polson C, Guss V, White R, Simutis F, Sanderson T, Gillman KW, Starrett JE Jr, Bronson J, Sverdlov O, Huang SP, Castaneda L, Feldman H, Coric V, Zaczek R, Macor JE, Houston J, Berman RM, Tong G.

J Pharmacol Exp Ther. 2013 Mar;344(3):686-95. doi: 10.1124/jpet.112.199356. Epub 2012 Dec 28.

15.

Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.

Gerritz SW, Zhai W, Shi S, Zhu S, Toyn JH, Meredith JE Jr, Iben LG, Burton CR, Albright CF, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Metzler W, Cook LS, Padmanabha R, Lentz KA, Sofia MJ, Poss MA, Macor JE, Thompson LA 3rd.

J Med Chem. 2012 Nov 8;55(21):9208-23. doi: 10.1021/jm300931y. Epub 2012 Oct 2.

PMID:
23030502
16.

A placebo-controlled, multiple ascending dose study to evaluate the safety, pharmacokinetics and pharmacodynamics of avagacestat (BMS-708163) in healthy young and elderly subjects.

Dockens R, Wang JS, Castaneda L, Sverdlov O, Huang SP, Slemmon R, Gu H, Wong O, Li H, Berman RM, Smith C, Albright CF, Tong G.

Clin Pharmacokinet. 2012 Oct 1;51(10):681-93.

PMID:
23018531
17.

Hyperdynamic microtubules, cognitive deficits, and pathology are improved in tau transgenic mice with low doses of the microtubule-stabilizing agent BMS-241027.

Barten DM, Fanara P, Andorfer C, Hoque N, Wong PY, Husted KH, Cadelina GW, Decarr LB, Yang L, Liu V, Fessler C, Protassio J, Riff T, Turner H, Janus CG, Sankaranarayanan S, Polson C, Meredith JE, Gray G, Hanna A, Olson RE, Kim SH, Vite GD, Lee FY, Albright CF.

J Neurosci. 2012 May 23;32(21):7137-45. doi: 10.1523/JNEUROSCI.0188-12.2012.

18.

A contrast in safety, pharmacokinetics and pharmacodynamics across age groups after a single 50 mg oral dose of the γ-secretase inhibitor avagacestat.

Tong G, Wang JS, Sverdlov O, Huang SP, Slemmon R, Croop R, Castaneda L, Gu H, Wong O, Li H, Berman RM, Smith C, Albright CF, Dockens R.

Br J Clin Pharmacol. 2013 Jan;75(1):136-45. doi: 10.1111/j.1365-2125.2012.04339.x.

19.

Multicenter, randomized, double-blind, placebo-controlled, single-ascending dose study of the oral γ-secretase inhibitor BMS-708163 (Avagacestat): tolerability profile, pharmacokinetic parameters, and pharmacodynamic markers.

Tong G, Wang JS, Sverdlov O, Huang SP, Slemmon R, Croop R, Castaneda L, Gu H, Wong O, Li H, Berman RM, Smith C, Albright CF, Dockens RC.

Clin Ther. 2012 Mar;34(3):654-67. doi: 10.1016/j.clinthera.2012.01.022. Epub 2012 Feb 28.

PMID:
22381714
20.

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.

Thompson LA, Shi J, Decicco CP, Tebben AJ, Olson RE, Boy KM, Guernon JM, Good AC, Liauw A, Zheng C, Copeland RA, Combs AP, Trainor GL, Camac DM, Muckelbauer JK, Lentz KA, Grace JE, Burton CR, Toyn JH, Barten DM, Marcinkeviciene J, Meredith JE, Albright CF, Macor JE.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2.

PMID:
21974952

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