Display Settings:

Format
Items per page
Sort by

Send to:

Choose Destination

Results: 1 to 20 of 85

1.

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.

PMID:
23412139
[PubMed]
Free PMC Article
2.

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.

May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, Monk SA, Mathes BM, Mergott DJ, Watson BM, Stout SL, Timm DE, Smith Labell E, Gonzales CR, Nakano M, Jhee SS, Yen M, Ereshefsky L, Lindstrom TD, Calligaro DO, Cocke PJ, Greg Hall D, Friedrich S, Citron M, Audia JE.

J Neurosci. 2011 Nov 16;31(46):16507-16. doi: 10.1523/JNEUROSCI.3647-11.2011.

PMID:
22090477
[PubMed - indexed for MEDLINE]
Free Article
3.

Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors.

Wood S, Wen PH, Zhang J, Zhu L, Luo Y, Babu-Khan S, Chen K, Pham R, Esmay J, Dineen TA, Kaller MR, Weiss MM, Hitchcock SA, Citron M, Zhong W, Hickman D, Williamson T.

J Pharmacol Exp Ther. 2012 Nov;343(2):460-7. doi: 10.1124/jpet.112.197954. Epub 2012 Aug 21.

PMID:
22911925
[PubMed - indexed for MEDLINE]
Free Article
4.
5.

Iminoheterocycle as a druggable motif: BACE1 inhibitors and beyond.

Zhu Z.

Trends Pharmacol Sci. 2012 May;33(5):233-40. doi: 10.1016/j.tips.2012.02.003. Epub 2012 Apr 4.

PMID:
22480948
[PubMed - indexed for MEDLINE]
6.

Differential effects of gamma-secretase and BACE1 inhibition on brain Abeta levels in vitro and in vivo.

Elvang AB, Volbracht C, Pedersen LØ, Jensen KG, Karlsson JJ, Larsen SA, Mørk A, Stensbøl TB, Bastlund JF.

J Neurochem. 2009 Sep;110(5):1377-87. doi: 10.1111/j.1471-4159.2009.06215.x. Epub 2009 Jun 10.

PMID:
19519664
[PubMed - indexed for MEDLINE]
7.

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
[PubMed - indexed for MEDLINE]
8.

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
[PubMed - indexed for MEDLINE]
9.

Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.

Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, DeLisle RK, Rizzi JP, Regal K, Sammond D, Groneberg R, Siu M, Purkey H, Lyssikatos JP, Marlow A, Liu X, Tang TP.

J Med Chem. 2013 Apr 25;56(8):3379-403. doi: 10.1021/jm4002154. Epub 2013 Apr 16.

PMID:
23537249
[PubMed - indexed for MEDLINE]
10.

Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.

Huang H, La DS, Cheng AC, Whittington DA, Patel VF, Chen K, Dineen TA, Epstein O, Graceffa R, Hickman D, Kiang YH, Louie S, Luo Y, Wahl RC, Wen PH, Wood S, Fremeau RT Jr.

J Med Chem. 2012 Nov 8;55(21):9156-69. doi: 10.1021/jm300598e. Epub 2012 Sep 11.

PMID:
22928914
[PubMed - indexed for MEDLINE]
11.

Beta-secretase (BACE) as a drug target for Alzheimer's disease.

Vassar R.

Adv Drug Deliv Rev. 2002 Dec 7;54(12):1589-602. Review.

PMID:
12453676
[PubMed - indexed for MEDLINE]
12.

The beta-secretase, BACE: a prime drug target for Alzheimer's disease.

Vassar R.

J Mol Neurosci. 2001 Oct;17(2):157-70. Review.

PMID:
11816789
[PubMed - indexed for MEDLINE]
13.

The Basic Biology of BACE1: A Key Therapeutic Target for Alzheimer's Disease.

Cole SL, Vassar R.

Curr Genomics. 2007 Dec;8(8):509-30. doi: 10.2174/138920207783769512.

PMID:
19415126
[PubMed]
Free PMC Article
14.

The contribution of activated astrocytes to Aβ production: implications for Alzheimer's disease pathogenesis.

Zhao J, O'Connor T, Vassar R.

J Neuroinflammation. 2011 Nov 2;8:150. doi: 10.1186/1742-2094-8-150.

PMID:
22047170
[PubMed - indexed for MEDLINE]
Free PMC Article
15.

Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) as a biological candidate marker of Alzheimer's disease.

Hampel H, Shen Y.

Scand J Clin Lab Invest. 2009;69(1):8-12. doi: 10.1080/00365510701864610. Review.

PMID:
18609117
[PubMed - indexed for MEDLINE]
16.

AZ-4217: a high potency BACE inhibitor displaying acute central efficacy in different in vivo models and reduced amyloid deposition in Tg2576 mice.

Eketjäll S, Janson J, Jeppsson F, Svanhagen A, Kolmodin K, Gustavsson S, Radesäter AC, Eliason K, Briem S, Appelkvist P, Niva C, Berg AL, Karlström S, Swahn BM, Fälting J.

J Neurosci. 2013 Jun 12;33(24):10075-84. doi: 10.1523/JNEUROSCI.1165-13.2013.

PMID:
23761903
[PubMed - indexed for MEDLINE]
Free Article
17.

Virtual screening and structure-based discovery of indole acylguanidines as potent β-secretase (BACE1) inhibitors.

Zou Y, Li L, Chen W, Chen T, Ma L, Wang X, Xiong B, Xu Y, Shen J.

Molecules. 2013 May 16;18(5):5706-22. doi: 10.3390/molecules18055706.

PMID:
23681056
[PubMed - indexed for MEDLINE]
Free Article
18.

Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.

Volgraf M, Chan L, Huestis MP, Purkey HE, Burkard M, Geck Do M, Harris J, Hunt KW, Liu X, Lyssikatos JP, Rana S, Thomas AA, Vigers GP, Siu M.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2477-80. doi: 10.1016/j.bmcl.2014.04.012. Epub 2014 Apr 13.

PMID:
24780121
[PubMed - in process]
19.

In vivo beta-secretase 1 inhibition leads to brain Abeta lowering and increased alpha-secretase processing of amyloid precursor protein without effect on neuregulin-1.

Sankaranarayanan S, Price EA, Wu G, Crouthamel MC, Shi XP, Tugusheva K, Tyler KX, Kahana J, Ellis J, Jin L, Steele T, Stachel S, Coburn C, Simon AJ.

J Pharmacol Exp Ther. 2008 Mar;324(3):957-69. Epub 2007 Dec 21.

PMID:
18156464
[PubMed - indexed for MEDLINE]
Free Article
20.

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.

Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE.

ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10.

PMID:
24900185
[PubMed]
Free PMC Article

Display Settings:

Format
Items per page
Sort by

Send to:

Choose Destination

Supplemental Content

Write to the Help Desk