Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT69DB8)

DTT Name	Beta-site APP-cleaving enzyme 2 (BACE2)
Synonyms	Theta-secretase; Membrane-associated aspartic protease 1; Memapsin-1; Down region aspartic protease; DRAP; Beta-site amyloid precursor protein cleaving enzyme 2; Beta-site APP cleaving enzyme 2; Beta-secretase 2; Aspartyl protease 1; Aspartic-like protease 56 kDa; Asp 1; ASP21; ASP1; ALP56; AEPLC
Gene Name	BACE2
DTT Type	Clinical trial target	[1]
UniProt ID	BACE2_HUMAN
TTD ID	T01280
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
EC Number	EC 3.4.23.45
Sequence	MGALARALLLPLLAQWLLRAAPELAPAPFTLPLRVAAATNRVVAPTPGPGTPAERHADGL ALALEPALASPAGAANFLAMVDNLQGDSGRGYYLEMLIGTPPQKLQILVDTGSSNFAVAG TPHSYIDTYFDTERSSTYRSKGFDVTVKYTQGSWTGFVGEDLVTIPKGFNTSFLVNIATI FESENFFLPGIKWNGILGLAYATLAKPSSSLETFFDSLVTQANIPNVFSMQMCGAGLPVA GSGTNGGSLVLGGIEPSLYKGDIWYTPIKEEWYYQIEILKLEIGGQSLNLDCREYNADKA IVDSGTTLLRLPQKVFDAVVEAVARASLIPEFSDGFWTGSQLACWTNSETPWSYFPKISI YLRDENSSRSFRITILPQLYIQPMMGAGLNYECYRFGISPSTNALVIGATVMEGFYVIFD RAQKRVGFAASPCAEIAGAAVSEISGPFSTEDVASNCVPAQSLSEPILWIVSYALMSVCG AILLVLIVLLLLPFRCQRRPRDPEVVNDESSLVRHRWK
Function	Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves APP, between residues 690 and 691, leading to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase. It has also been shown that it can cleave APP between residues 671 and 672. Responsible also for the proteolytic processing of CLTRN in pancreatic beta cells.
KEGG Pathway	Alzheimer disease (hsa05010 )
BioCyc Pathway	MetaCyc:G66-33964-MON

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
example 98 (WO2011020806)	DM2N653	Focal segmental glomerulosclerosis	MF8Y	Clinical trial	[1]
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6 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2ewy	DMNOAJG	Discovery agent	N.A.	Investigative	[2]
example 2 (WO2013004676)	DMU25HZ	Discovery agent	N.A.	Investigative	[3]
example 20 (WO2010128058)	DMF9W41	Discovery agent	N.A.	Investigative	[4]
example 41 (WO2012028563)	DM2N9Y8	Discovery agent	N.A.	Investigative	[4]
example 92 (WO2012095521)	DMU42CR	Discovery agent	N.A.	Investigative	[4]
PMID21907142CJ	DMST0IN	Discovery agent	N.A.	Investigative	[5]
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⏷ Show the Full List of 6 Investigative Drug(s)

References

1	BACE2 as a new diabetes target: a patent review (2010 - 2012). Expert Opin Ther Pat. 2013 May;23(5):649-63.
2	Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor. J Mol Biol. 2006 Jan 13;355(2):249-61.
3	Cyclopropyl-Fused 1,3-Thiazepines as BACE1 and BACE2 Inhibitors. ACS Med Chem Lett. 2013 Mar 15;4(4):379-80.
4	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2331).
5	Bace2 is a beta cell-enriched protease that regulates pancreatic beta cell function and mass. Cell Metab. 2011 Sep 7;14(3):365-77.