Literature summary for 3.4.23.46 extracted from

Ghosh, A.K.; Kumaragurubaran, N.; Hong, L.; Koelsh, G.; Tang, J.
Memapsin 2 (beta-secretase) inhibitors: drug development (2008), Curr. Alzheimer Res., 5, 121-131.

Search for more literature for 3.4.23.46

Application

Application	Comment	Organism
pharmacology	development of inhibitor drugs for the treatment of Alzheimer disease	Homo sapiens
pharmacology	development of inhibitor drugs for the treatment of Alzheimer disease	Mus musculus

Crystallization (Commentary)

Crystallization (Comment)	Organism
stereoview of the X-ray crystal structure of inhibitor complex with memapsin 2 indicated	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
GRL-8234	i.e. inhibitor 24, inhibitory and cellular assays described	Homo sapiens
GRL-8234	i.e. inhibitor 24, inhibitory and cellular assays described	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P56817	-	-
Mus musculus	P56818	transgenic mice strain Tg2576	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
CHO cell	inhibitor drugs tested	Homo sapiens	-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg]	Specific Activity Maximum [µmol/min/mg]	Comment	Organism
additional information	-	synthesis, structure and potencies of memapsin 2 inhibitors shown, memapsin 2 enzyme inhibitory and cellular assays described, up to 65% reduction of plasma amyloid-beta peptide in transgenic mice indicated, ligand-binding site interactions indicated by stereoview of X-ray structure	Homo sapiens
additional information	-	synthesis, structure and potencies of memapsin 2 inhibitors shown, up to 65% reduction of plasma amyloid-beta peptide in transgenic mice indicated	Mus musculus

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	properties of memapsin 2 inhibitors analyzed by cellular assay	Mus musculus	?	-	?
additional information	properties of memapsin 2 inhibitors analyzed by inhibitory and cellular assays	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
BACE1	-	Homo sapiens
BACE1	-	Mus musculus
beta-secretase	-	Homo sapiens
beta-secretase	-	Mus musculus
memapsin 2	-	Homo sapiens
memapsin 2	-	Mus musculus

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0018	-	GRL-8234	i.e. inhibitor 24, memapsin 2 enzyme inhibition assay	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.001	-	i.e. inhibitor 24, in Chinese hamster ovary cells	Homo sapiens	GRL-8234

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Release 2023.1 (January 2023)