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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
Substance
CAS Registry & name
Categories
Source
Drugs
*
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