Page last updated: 2024-08-07 13:50:00
Beta-secretase 2
A beta-secretase 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y5Z0]
Synonyms
EC 3.4.23.45;
Aspartic-like protease 56 kDa;
Aspartyl protease 1;
ASP1;
Asp 1;
Beta-site amyloid precursor protein cleaving enzyme 2;
Beta-site APP cleaving enzyme 2;
Down region aspartic protease;
DRAP;
Memapsin-1;
Research
Bioassay Publications (10)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 4 (40.00) | 29.6817 |
2010's | 5 (50.00) | 24.3611 |
2020's | 1 (10.00) | 2.80 |
Compounds (7)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
om99-2 | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
om00-3 | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
l 685458 | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
gsk188909 | Homo sapiens (human) | IC50 | 0.6026 | 3 | 5 |
ly2811376 | Homo sapiens (human) | IC50 | 1.5840 | 2 | 2 |
azd3839 | Homo sapiens (human) | IC50 | 0.0009 | 1 | 1 |
azd3839 | Homo sapiens (human) | Ki | 0.3700 | 1 | 1 |
ly2886721 | Homo sapiens (human) | IC50 | 0.0102 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
ly2811376 | Homo sapiens (human) | INH | 2.8000 | 1 | 1 |
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.Bioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Structure-based design of β-site APP cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer's disease.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Toward β-Secretase-1 Inhibitors with Improved Isoform Selectivity.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Design and synthesis of β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of β-amyloid peptides.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Enables
This protein enables 2 target(s):
Target | Category | Definition |
aspartic-type endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a mechanism in which a water molecule bound by the side chains of aspartic residues at the active center acts as a nucleophile. [ISBN:0198506732] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
Located In
This protein is located in 5 target(s):
Target | Category | Definition |
endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
melanosome membrane | cellular component | The lipid bilayer surrounding a melanosome. [GOC:mah] |
Active In
This protein is active in 3 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
trans-Golgi network | cellular component | The network of interconnected tubular and cisternal structures located within the Golgi apparatus on the side distal to the endoplasmic reticulum, from which secretory vesicles emerge. The trans-Golgi network is important in the later stages of protein secretion where it is thought to play a key role in the sorting and targeting of secreted proteins to the correct destination. [GOC:vw, ISBN:0815316194] |
endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
Involved In
This protein is involved in 8 target(s):
Target | Category | Definition |
proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
membrane protein ectodomain proteolysis | biological process | The proteolytic cleavage of transmembrane proteins and release of their ectodomain (extracellular domain). [GOC:jl, http://www.copewithcytokines.de/] |
protein processing | biological process | Any protein maturation process achieved by the cleavage of a peptide bond or bonds within a protein. Protein maturation is the process leading to the attainment of the full functional capacity of a protein. [GOC:curators, GOC:jl, GOC:jsg] |
peptide hormone processing | biological process | The generation of a mature peptide hormone by posttranslational processing of a prohormone. [GOC:mah] |
melanosome organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a melanosome. A melanosome is a tissue-specific, membrane-bounded cytoplasmic organelle within which melanin pigments are synthesized and stored. [GOC:vk] |
glucose homeostasis | biological process | Any process involved in the maintenance of an internal steady state of glucose within an organism or cell. [GOC:go_curators] |
negative regulation of amyloid precursor protein biosynthetic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of amyloid precursor protein (APP), the precursor of amyloid-beta. [GOC:go_curators] |
amyloid-beta metabolic process | biological process | The chemical reactions and pathways involving amyloid-beta, a glycoprotein associated with Alzheimer's disease, and its precursor, amyloid precursor protein (APP). [GOC:ai] |