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Literature summary for 3.4.24.65 extracted from

  • Mannino, C.; Nievo, M.; Machetti, F.; Papakyriakou, A.; Calderone, V.; Fragai, M.; Guarna, A.
    Synthesis of bicyclic molecular scaffolds (BTAa): an investigation towards new selective MMP-12 inhibitors (2006), Bioorg. Med. Chem., 14, 7392-7403.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of a cDNA encoding the fragment Gly106-Gly263 of the enzyme F171D mutant in Escherichia coli strain BL21 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
purified MMP-12 bound to hydroxamic acid, hanging drop vapour diffusion method, 20°C, from protein solution containing 10 mg/ml protein in 0.1 M Tris-HCl, pH 8.0, 30% PEG 6000, 200 mM hydroxamic acid, and 1.0 M LiCl, a few days, X-ray diffraction structure determination and analysis at 1.3 A resolution Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1S,5S,7R)-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-3,7-dicarboxylic acid 7-[(biphenyl-4-ylmethyl)-amide] 3-hydroxyamide
-
Homo sapiens
(1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid
-
Homo sapiens
(1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide
-
Homo sapiens
(1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid
-
Homo sapiens
(1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide
-
Homo sapiens
additional information inhibitor design and synthesis based on a 3-aza-6,8-dioxa-bicyclo[3.2.1]octane scaffold, library construction and screening, determination of affinity for the catalytic domain of MMP-12 by NMR, overview Homo sapiens
N-isobutyl-N-[4-methoxyphenylsulfonyl] glycyl hydroxamic acid
-
Homo sapiens

Metals/Ions

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant F171D mutant fragment Gly106-Gly263 from Escherichia coli strain BL21 by gel filtration and anion exchange chromatography Homo sapiens

Renatured (Commentary)

Renatured (Comment) Organism
recombinant fragment of mutant F171D from Escherichia coli inclusion bodies by solubilization in 20 mM Tris-HCl and 8 M urea at pH 8.0, refolding by multi-step dialysis, overview Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining

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 ?
-
?

Synonyms

Synonyms Comment Organism
Human macrophage metalloelastase
-
Homo sapiens
macrophage metalloelastase
-
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
7
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.954
-
pH 7.0, 25°C, recombinant enzyme Homo sapiens (1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid
149
-
pH 7.0, 25°C, recombinant enzyme Homo sapiens (1S,5S,7R)-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-3,7-dicarboxylic acid 7-[(biphenyl-4-ylmethyl)-amide] 3-hydroxyamide
399
-
pH 7.0, 25°C, recombinant enzyme Homo sapiens (1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide
425
-
pH 7.0, 25°C, recombinant enzyme Homo sapiens (1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide
835
-
pH 7.0, 25°C, recombinant enzyme Homo sapiens (1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid