3.4.24.65: macrophage elastase

This is an abbreviated version!
For detailed information about macrophage elastase, go to the full flat file.

Word Map on EC 3.4.24.65

3.4.24.65

metalloproteinases

mmp-9

pulmonary

emphysema

collagen

alveolar

elastin

fibrosis

smoke

airway

timp-1

cigarette

lavage

bronchoalveolar

endothelial

metastasis

aortic

tnf

artery

chemokine

monocyte

smoking

plaque

aneurysm

angiogenesis

atherosclerotic

zymography

smoke-induced

elastolytic

proteinases

plasminogen

asthma

rupture

angiostatin

bal

instil

urokinase-type

matrilysin

airspace

mt1-mmp

cs-induced

elastases

smoke-exposed

emphysematous

diagnostics

drug development

elastase-induced

collagenase-3

cs-exposed

airflow

medicine

pharmacology

matrix-degrading

analysis

Reaction

Hydrolysis of soluble and insoluble elastin. Specific cleavages are also produced at -Ala14-/-Leu- and -Tyr16-/-Leu- in the B chain of insulin =

Synonyms

HME, hMMP-12, human macrophage elastase, Human macrophage metalloelastase, human metalloelastase, Macrophage elastase, macrophage matrix metalloproteinase, macrophage metalloelastase, macrophage-specific metalloelastase, matrix metalloproteinase 12, Matrix metalloproteinase-12, ME, Metalloelastase, MME, MMP-12, MMP12, More, mouse macrophage metalloelastase, rHME

ECTree

3.4 Acting on peptide bonds (peptidases)

3.4.24 Metalloendopeptidases

3.4.24.65 macrophage elastase

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Results	in table
2	Activating Compound
9	AA Sequence
16	Application
2	CAS Registry Number
18	Cloned(Commentary)
3	Crystallization (Commentary)
2467	Disease/ Diagnostics
7	Expression
17	General Information
6	General Stability
14	IC50 Value
45	Inhibitors
121	kcat/KM [mM/s]
2	Ki Value [mM]
48	KM Value [mM]
21	Localization
11	Metals/Ions
20	Molecular Weight [Da]
31	Natural Substrates/ Products (Substrates)
192	Organism
131	PDB ID
12	pH Optimum
8	Posttranslational Modification
33	Protein Variants
11	Purification (Commentary)
1	Reaction
1	Reaction Type
53	Reference
2	Renatured (Commentary)
72	Source Tissue
3	Specific Activity [micromol/min/mg]
1	Storage Stability
141	Substrates and Products (Substrate)
15	Subunits
94	Synonyms
14	Temperature Optimum [°C]
48	Turnover Number [1/s]

Inhibitors

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Inhibitors on EC 3.4.24.65 - macrophage elastase

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(1S,5S,7R)-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-3,7-dicarboxylic acid 7-[(biphenyl-4-ylmethyl)-amide] 3-hydroxyamide

-

-

(1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid

-

-

(1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide

-

-

(1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid

-

-

(1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide

-

-

(3R)-3-([[4-(4'-acetylbiphenyl-4-yl)-5-fluorothiophen-2-yl]carbonyl]amino)-3-phenylpropanoic acid

-

-

(3R)-3-[([5-fluoro-4-[4-(pyridin-4-yl)phenyl]thiophen-2-yl]carbonyl)amino]-3-phenylpropanoic acid

-

-

(3R)-3-[([5-fluoro-4-[4-(trifluoromethoxy)phenyl]thiophen-2-yl]carbonyl)amino]-3-phenylpropanoic acid

-

-

alpha2-Macroglobulin

show

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batimastat

BB-94

CGS-27023A

-

a hydroxamate inhibitor

CGS27023A

-

-

dexamethasone

-

in vivo inhibition of the human enzyme in mice leading to inhibited cytokine release and neutrophil influx, overview

dithiothreitol

-

-

EDTA

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EGTA

-

less effective than EDTA, Ca2+ at a 3:1 ratio of Ca2+/EDTA protects and reverses partially, Zn2+ at a 1:10 ratio of Zn2+/EGTA protects and reverses

GM6001

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marimastat

-

in vivo inhibition of the human enzyme in mice leading to inhibited macrophage recruitment, neutrophil influx, and cytokine release, overview

N-(3-[(4-bromophenyl)(hydroxy)phosphoryl]-2-[3-[4-(dimethylamino)phenyl]isoxazol-5-yl]propanoyl)-L-alpha-glutamyl-L-alpha-glutamine

-

-

N-isobutyl-N-[4-methoxyphenylsulfonyl] glycyl hydroxamic acid

-

-

N-[(1R)-3-amino-3-oxo-1-phenylpropyl]-5-fluoro-4-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide

-

-

N-[(2S,4S)-1-(ethoxymethoxy)-5-(hydroxyamino)-4-methyl-5-oxo-2-pentanyl]-4-phenoxybenzamide

i.e. ONO-4817, an MMP inhibitor

N-[3-[(4-bromophenyl)(hydroxy)phosphoryl]-2-[3-(3'-chlorobiphenyl-4-yl)isoxazol-5-yl]propanoyl]-L-alpha-glutamyl-L-alpha-glutamine

-

-

organic solvents

-

enzyme form B, above 0.5% v/v

-

Rabbit antiserum against purified elastase form B

-

-

-

rolipram

-

in vivo inhibition of the human enzyme in mice leading to inhibited neutrophil influx, overview

TIMP-1

-

a major fibrogenic effector in lungs. Indeed, upon fibrogenic stimuli, large amounts of TIMP-1 in the remodeling tissue are believed to contribute to the creation of a non-degrading environment, leading to the alteration of protease-anti-protease balance, extracellular matrix accumulation, and tissue fibrosis. MMP-12 deficiency does not seem to be involved in TIMP-1 regulation

-

tissue inhibitor of metalloproteinase

show

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trans-4-[([[4-(4'-acetylbiphenyl-4-yl)-5-fluorothiophen-2-yl]carbonyl]amino)methyl]cyclohexanecarboxylic acid

-

-

trans-4-[[([3-[4-(trifluoromethoxy)phenyl]-1,2-thiazol-5-yl]carbonyl)amino]methyl]cyclohexanecarboxylic acid

-

-

trans-4-[[([4-[4-(trifluoromethoxy)phenyl]thiophen-2-yl]carbonyl)amino]methyl]cyclohexanecarboxylic acid

-

-

trans-4-[[([5-fluoro-4-[4-(trifluoromethoxy)phenyl]thiophen-2-yl]carbonyl)amino]methyl]cyclohexanecarboxylic acid

-

-

trans-4-[[([5-[4-(trifluoromethoxy)phenyl]-1,2-thiazol-3-yl]carbonyl)amino]methyl]cyclohexanecarboxylic acid

-

-

Zn2+

-

at a 3fold molar excess of Zn2+ over chelating agent

additional information

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Release 2023.1 (January 2023)