Literature summary for 3.4.24.65 extracted from

Devel, L.; Rogakos, V.; David, A.; Makaritis, A.; Beau, F.; Cuniasse, P.; Yiotakis, A.; Dive, V.
Development of selective inhibitors and substrate of matrix metalloproteinase-12 (2006), J. Biol. Chem., 281, 11152-11160.

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Inhibitors

Inhibitors	Comment	Organism	Structure
additional information	role of the P'3 position in inhibitor selectivity, overview, interaction of compound 1 with the catalytic domain of MMP12, molecular modeling, overview	Homo sapiens
N-(3-[(4-bromophenyl)(hydroxy)phosphoryl]-2-[3-[4-(dimethylamino)phenyl]isoxazol-5-yl]propanoyl)-L-alpha-glutamyl-L-alpha-glutamine	-	Homo sapiens
N-[3-[(4-bromophenyl)(hydroxy)phosphoryl]-2-[3-(3'-chlorobiphenyl-4-yl)isoxazol-5-yl]propanoyl]-L-alpha-glutamyl-L-alpha-glutamine	-	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Ca2+	-	Homo sapiens
Zn2+	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
commercial preparation	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 + H2O	-	Homo sapiens	Mca-Pro-Leu-Gly + Leu-Dpa-Ala-Arg-NH2	-	?
Mca-Pro-Leu-Gly-Leu-Glu-Glu-Ala-Dpa-NH2 + H2O	selective cleavage, the Glu-Glu motif interacts with the S'2 and S'3 subsites of MMP-12	Homo sapiens	Mca-Pro-Leu-Gly + Leu-Glu-Glu-Ala-Dpa-NH2	-	?

Synonyms

Synonyms	Comment	Organism
Matrix metalloproteinase-12	-	Homo sapiens
MMP-12	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
25	-	assay at	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
6.8	-	assay at	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.00000019	-	N-[3-[(4-bromophenyl)(hydroxy)phosphoryl]-2-[3-(3'-chlorobiphenyl-4-yl)isoxazol-5-yl]propanoyl]-L-alpha-glutamyl-L-alpha-glutamine	-	Homo sapiens
0.0000044	-	N-(3-[(4-bromophenyl)(hydroxy)phosphoryl]-2-[3-[4-(dimethylamino)phenyl]isoxazol-5-yl]propanoyl)-L-alpha-glutamyl-L-alpha-glutamine	-	Homo sapiens

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Release 2023.1 (January 2023)