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Amyloid Precursor Protein Secretases

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Definition: Endopeptidases that are specific for AMYLOID PROTEIN PRECURSOR. Three secretase subtypes referred to as alpha, beta, and gamma have been identified based upon the region of amyloid protein precursor they cleave.      Other names gamma Secretase; beta Secretase; alpha Secretase; Secretase, APP; gamma-Secretase; beta-Secretase; alpha-Secretase; Secretases; Secretase; Amyloid Precursor Protein Secretase; APP Secretase
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
6-hydroxy-4-oxo-N-(10-((1,2,3,4-tetrahydroacridin-9-yl)amino)decyl)-4H-chromene-2-carboxamide  0   *Chromones Tacrine/*analogs & derivatives Butyrylcholinesterase Cholinesterase Inhibitors Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Med Chem. 2012 Feb 9;55(3):1303-17.
(1-(4-methyl-1-(6-(trifluoromethyl)-3-pyridinyl)pentyl)-2-(4-(trifluoromethyl)phenyl)-4-piperidinyl)acetic acid  0   *Acetic Acids *Piperidines Amyloid Precursor Protein Secretases. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1306-11.
2-(3,5-bis(4-(trifluoromethyl)phenyl)phenyl)-4-methylpentanoic acid  0   *Pentanoic Acids Amyloid Precursor Protein Secretases/antagonists & inhibitors. Br J Pharmacol 2011 May;163(2):375-89
SCH 1500022  0   *Cyclic S-Oxides *Heterocyclic Compounds with 4 or More Rings Amyloid Precursor Protein Secretases/antagonists & inhibitors. Biochemistry 2011 Jun 7;50(22):4973-80
GRL 8234  0   *Phthalic Acids *Sulfonamides Amyloid Precursor Protein Secretases/antagonists & inhibitors. FASEB J 2011 Feb;25(2):775-84
presenilin enhancer 2, mouse  EC 3.4.-   *Amyloid Precursor Protein Secretases Protein Subunits. Biochem Biophys Res Commun 2011 Jan 7;404(1):564-8
1-(1-(4-fluorophenyl)ethyl)-3-((3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)methylene)-2-piperidinone  0   *Imidazoles *Piperidines Amyloid Precursor Protein Secretases. J Alzheimers Dis 2010;21(3):1005-12
3-(4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid  0   *Propionic Acids *Sulfones Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Chromatogr B Analyt Technol Biomed Life Sci 2010 Sep 1;878(25):2348-52
BMS 708163  0   *Oxadiazoles *Sulfonamides Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Chromatogr B Analyt Technol Biomed Life Sci 2010 Sep 1;878(25):2319-26
2-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide  0   *Tetrahydronaphthalenes Valine/*analogs & derivatives Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Pharmacol Exp Ther 2010 Jul;334(1):269-77
2,2-dimethyl-N-(6-oxo-6,7-dihydro-5H-dibenzo(b,d)azepin-7-yl)-N'-(2,2,3,3,3-pentafluoropropyl)malonamide  0   *Benzazepines Amyloid Precursor Protein Secretases/antagonists & inhibitors. Cancer Res 2009 Oct 1;69(19):7672-80
2',3',4',5,5',6,7,8,9,10-decahydro-2-(5-(4-fluorophenyl)-1-methylpyrazol-3-yl)-5'-(2,2,2-trifluoroethyl)spiro(6,9-methanobenzocycloocten-11,3'-(1,2,5)thiadiazole) 1',1'-dioxide  0   *Thiadiazoles *Cyclooctanes Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Med Chem 2009 Jun 11;52(11):3441-4
begacestat  0   *Sulfonamides *Thiophenes Amyloid Precursor Protein Secretases. J Med Chem 2008 Dec 11;51(23):7348-51
2-(((3,5-difluorophenyl)acetyl)amino)-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)propanamide  0   *Benzodiazepinones Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Biol Chem 2000 Nov 3;275(44):34086-91
dibenzazepine  0   *Dibenzazepines Amyloid Precursor Protein Secretases/antagonists & inhibitors. Hospital (Rio J) 1967 Sep;72(3):859-77
MRK 003  0   *Cyclic S-Oxides *Thiadiazoles Amyloid Precursor Protein Secretases/antagonists & inhibitors. Chem Biol 2007 Feb;14(2):209-19
benzyloxycarbonyl-isoleucyl-leucinal  0   *Dipeptides Amyloid Precursor Protein Secretases/antagonists & inhibitors. Oncol Rep 2007 Jul;18(1):77-80
benzyloxycarbonyl-leucyl-leucyl-norleucinal  0   *Oligopeptides Amyloid Precursor Protein Secretases/antagonists & inhibitors. Oncol Rep 2007 Jul;18(1):77-80
2-(2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-(3-methyl-4-oxo-4,5-dihydro-3H-benzo(d)(1,2)diazepin-5-yl)propanamide  0   *Benzodiazepinones Alanine/*analogs & derivatives Amyloid Precursor Protein Secretases/antagonists & inhibitors. Bioorg Med Chem Lett 2007 Jul 15;17(14):4006-11
1-(3',4'-dichloro-2-fluoro(1,1'-biphenyl)-4-yl)cyclopropanecarboxylic acid  0   *Cyclopropanes Flurbiprofen/*analogs & derivatives Amyloid Precursor Protein Secretases/antagonists & inhibitors. Pharmacol Res 2007 Apr;55(4):318-28
GRL 7234  0   *Sulfonamides Valine/*analogs & derivatives Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Med Chem 2007 May 17;50(10):2399-407
N-(1-(3,5-difluorobenzyl)-2-hydroxy-3-(3-iodobenzylamino)propyl)-5-methyl-N',N'-dipropylisophthalamide  0   *Phthalic Acids Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Med Chem 2007 Feb 22;50(4):776-81
Bace2 protein, rat  EC 3.4.23.45   *Aspartic Acid Endopeptidases *Amyloid Precursor Protein Secretases.
Bace2 protein, mouse  0   *Aspartic Acid Endopeptidases *Amyloid Precursor Protein Secretases.
BACE2 protein, human  EC 3.4.23.45   *Aspartic Acid Endopeptidases *Amyloid Precursor Protein Secretases.
Bace1 protein, mouse  EC 3.4.23.46   *Aspartic Acid Endopeptidases *Amyloid Precursor Protein Secretases.
Bace protein, rat  EC 3.4.23.46   *Aspartic Acid Endopeptidases *Amyloid Precursor Protein Secretases.
BACE1 protein, human  EC 3.4.23.46   *Aspartic Acid Endopeptidases *Amyloid Precursor Protein Secretases.
ADAM10 protein, human  EC 3.4.24.81   *Membrane Proteins *ADAM Proteins *Amyloid Precursor Protein Secretases.
Adam10 protein, mouse  EC 3.4.24.81   *Membrane Proteins *ADAM Proteins *Amyloid Precursor Protein Secretases.
N2-((2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl)-N1-((7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo(b,d)azepin-7-yl)-L-alaninamide  0   *Azepines Alanine/*analogs & derivatives Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Pharmacol Exp Ther. 2004 Apr;309(1):49-55
PSENEN protein, human  0   *Membrane Proteins *Amyloid Precursor Protein Secretases. J Biol Chem 2002 Oct 18;277(42):39062-5
N-(N-(3,5-difluorophenacetyl)alanyl)phenylglycine tert-butyl ester  0   *Dipeptides Amyloid Precursor Protein Secretases/antagonists & inhibitors. J Neurochem 2001 Jan;76(1):173-81
nicastrin protein  0   *Membrane Glycoproteins *Amyloid Precursor Protein Secretases. Nature. 2000 Sep 7;407(6800):48-54
tumor necrosis factor-alpha convertase  EC 3.4.24.-   *ADAM Proteins Tumor Necrosis Factor-alpha Amyloid Precursor Protein Secretases. Biochem Biophys Res Commun 1996 Aug 14;225(2):400-5

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012
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