Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT8JRS7)

• DTT Name: Beta-secretase (BACE)
• Synonyms: Transmembrane aspartic protease; Beta-site amyloid precursor protein cleaving enzyme; Beta-site AbetaPP-cleaving enzyme; BACE1
• Gene Name: NO-GeName
• DTT Type: Clinical trial target; [1]
• Related Disease:
  Osteoarthritis [ICD-11: FA00-FA05]
  Shoulder lesion [ICD-11: FB53]
  Soft tissue disorder [ICD-11: FB56]
  Alzheimer disease [ICD-11: 8A20]
• BioChemical Class: Peptidase
• UniProt ID: NOUNIPROTAC
• TTD ID: T73992
• Function: Responsible for the proteolytic processing of the amyloid precursor protein (app). Cleaves at the amino terminus of the a-beta peptide sequence, between residues 671 and 672 of app, leads to the generation and extracellular release of beta-cleaved soluble liquid.

Molecular Interaction Atlas (MIA) of This DTT

19 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(S)-FLURBIPROFEN	DMF2O4T	Myalgia	FB56.2	Preregistration	[2]
E-2609	DMTNUJ8	Alzheimer disease	8A20	Phase 3	[1]
Lanabecestat	DMFJLB6	Alzheimer disease	8A20	Phase 3	[3], [4]
verubecestat	DM4CGH5	Alzheimer disease	8A20	Phase 3	[5]
AZD3293	DMJQHXD	Alzheimer disease	8A20	Phase 2/3	[6]
JNJ-54861911	DMGPJ5U	Alzheimer disease	8A20	Phase 2/3	[3], [4]
LY2886721	DMV14LM	Alzheimer disease	8A20	Phase 2	[7]
LY3202626	DM7IFNB	Alzheimer disease	8A20	Phase 2	[3], [4]
R-flurbiprofen	DMFIVSR	N. A.	N. A.	Phase 2	[2]
Azd-3839	DM72FOD	Alzheimer disease	8A20	Phase 1	[8]
CTS-21166	DM68I93	Alzheimer disease	8A20	Phase 1	[9]
HPP-854	DMSLDHG	Alzheimer disease	8A20	Phase 1	[5]
LY-2811376	DM8LGWR	Alzheimer disease	8A20	Phase 1	[10], [11]
RG7129	DMTWSM2	Alzheimer disease	8A20	Phase 1	[5]
AZ-4217	DMGPTFL	Rheumatoid arthritis	FA20	Clinical trial	[12]
oxazine 89	DMXFI90	Diabetic nephropathy	GB61.Z	Clinical trial	[13]
PMID22911925C2	DM5UWH3	Diabetic complication	5A2Y	Clinical trial	[14]
PMID23981898C11d	DMX1IZ9	Cardiovascular disease	BA00-BE2Z	Clinical trial	[15]
TAK-070	DMCM5GK	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[16]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SCH-1359113	DMLG682	Alzheimer disease	8A20	Preclinical	[17]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DNP-004089	DMXR3V1	Alzheimer disease	8A20	Terminated	[18]

35 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(-)-CATECHINGALLATE	DMZOGSK	Discovery agent	N.A.	Investigative	[19]
(2S)-2'-methoxy kurarinone	DMZOX43	Discovery agent	N.A.	Investigative	[20]
4-(2-aminoethyl)-2-cyclohexylphenol	DMZSN1Y	Discovery agent	N.A.	Investigative	[21]
4-(2-aminoethyl)-2-ethylphenol	DMF8D5S	Discovery agent	N.A.	Investigative	[21]
4-(4-FLUOROBENZYL)PIPERIDINE	DMW8IN3	Discovery agent	N.A.	Investigative	[21]
5,5-Diphenyl-2-iminohydantoin	DM28LNV	Discovery agent	N.A.	Investigative	[22]
6-[2-(1H-INDOL-6-YL)ETHYL]PYRIDIN-2-AMINE	DMNJPCD	Discovery agent	N.A.	Investigative	[21]
7-Phloroethol	DM19I62	Discovery agent	N.A.	Investigative	[23]
AP-2243	DMRYL9X	Discovery agent	N.A.	Investigative	[24]
AZ3971	DMVMW9S	Discovery agent	N.A.	Investigative	[25]
Bis-7-tacrine	DMVNC1R	Discovery agent	N.A.	Investigative	[26]
Carbocyclic Peptidomimetic	DM87SOX	Discovery agent	N.A.	Investigative	[27]
DIECKOL	DMBCK4G	Discovery agent	N.A.	Investigative	[23]
DIOXINODEHYDROECKOL	DML2B04	Discovery agent	N.A.	Investigative	[23]
Eckol	DMIVY0Q	Discovery agent	N.A.	Investigative	[23]
example 2 (WO2013004676)	DMU25HZ	Discovery agent	N.A.	Investigative	[28]
Glu-Leu-Asp-Leu-(CHOH-CH2)-Ala-Ala-Glu-Phe	DMXBQRJ	Discovery agent	N.A.	Investigative	[29]
GRL-7234	DMR93MK	Discovery agent	N.A.	Investigative	[30]
GSK-188909	DMMWBU6	Discovery agent	N.A.	Investigative	[31]
KMI-172	DMLRVEJ	Discovery agent	N.A.	Investigative	[32]
KMI-494	DMQ4WNB	Discovery agent	N.A.	Investigative	[32]
KMI-538	DMX9EA7	Discovery agent	N.A.	Investigative	[32]
KMI-596	DMXUETW	Discovery agent	N.A.	Investigative	[33]
Kurarinone	DMH0G8W	Discovery agent	N.A.	Investigative	[20]
KUSHENOL A	DMCFHPD	Discovery agent	N.A.	Investigative	[20]
LEACHIANONE A	DMZ21HU	Discovery agent	N.A.	Investigative	[20]
MMI-175	DMH1YN6	Discovery agent	N.A.	Investigative	[34]
N-(1-benzylpiperidin-4-yl)-4-sulfanylbutanamide	DMEKSHG	Discovery agent	N.A.	Investigative	[21]
N~3~-(3-PYRIDIN-3-YLBENZYL)PYRIDINE-2,3-DIAMINE	DML35GB	Discovery agent	N.A.	Investigative	[21]
N~3~-BENZYLPYRIDINE-2,3-DIAMINE	DMOCQ9I	Discovery agent	N.A.	Investigative	[21]
OM00-3	DMXJ2SM	Discovery agent	N.A.	Investigative	[35]
PHLOROFUCOFUROECKOL A	DMO1I6G	Discovery agent	N.A.	Investigative	[23]
PMID21907142CJ	DMST0IN	Discovery agent	N.A.	Investigative	[36]
PMID23412139C16	DM9O8I7	Discovery agent	N.A.	Investigative	[37]
TRIPHLOROETHOL A	DMF8QR6	Discovery agent	N.A.	Investigative	[23]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Rheumatoid arthritis	FA20	Synovial tissue	6.98E-04	1.03	2.84

References

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• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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