Page last updated: 2024-10-24

positive regulation of metalloendopeptidase activity

Definition

Target type: biologicalprocess

Any process that activates or increases the frequency, rate or extent of metalloendopeptidase activity. [GO_REF:0000059, GOC:BHF, GOC:BHF_miRNA, GOC:rph, GOC:TermGenie, PMID:18591254]

Positive regulation of metalloendopeptidase activity is a crucial biological process that controls the activity of metalloendopeptidases, a class of enzymes that cleave peptide bonds in proteins using a metal ion as a cofactor. These enzymes play essential roles in various biological processes, including protein degradation, signal transduction, and tissue remodeling.

The regulation of metalloendopeptidase activity is complex and involves a variety of mechanisms, including:

1. **Transcriptional regulation:** The expression of metalloendopeptidase genes can be modulated by transcription factors that bind to regulatory sequences in the gene promoters.
2. **Post-translational modifications:** Metalloendopeptidases can be regulated by post-translational modifications such as phosphorylation, glycosylation, and ubiquitination. These modifications can alter the enzyme's activity, stability, or localization.
3. **Interactions with inhibitors and activators:** Metalloendopeptidase activity can be regulated by specific inhibitors and activators that bind to the enzyme and either block or enhance its activity.
4. **Cellular localization:** The subcellular localization of metalloendopeptidases can influence their activity. For example, some metalloendopeptidases are localized to specific organelles, such as lysosomes or the plasma membrane, where they have specific functions.

The positive regulation of metalloendopeptidase activity ensures that these enzymes are activated at the appropriate time and place to perform their specific functions. This regulation is essential for maintaining cellular homeostasis and proper biological function.

Examples of metalloendopeptidases with important roles in positive regulation include:

* **Angiotensin-converting enzyme (ACE):** ACE is a key enzyme in the renin-angiotensin system that regulates blood pressure.
* **Matrix metalloproteinases (MMPs):** MMPs play a critical role in tissue remodeling and repair, and their activity is tightly regulated to prevent uncontrolled degradation of the extracellular matrix.
* **Thermolysin:** Thermolysin is a bacterial metalloendopeptidase that has been used as a model system to study the mechanism of metalloendopeptidase activity.

Understanding the mechanisms of positive regulation of metalloendopeptidase activity is crucial for developing therapeutic strategies for a variety of diseases, including cardiovascular disease, cancer, and neurodegenerative disorders.'
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Proteins (1)

ProteinDefinitionTaxonomy
Signal transducer and activator of transcription 3A signal transducer and activator of transcription 3 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P40763]Homo sapiens (human)

Compounds (28)

CompoundDefinitionClassesRoles
niclosamideniclosamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-chlorosalicylic acid with the amino group of 2-chloro-4-nitroaniline. It is an oral anthelmintic drug approved for use against tapeworm infections.

Niclosamide: An antihelmintic that is active against most tapeworms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p48)
benzamides;
C-nitro compound;
monochlorobenzenes;
salicylanilides;
secondary carboxamide
anthelminthic drug;
anticoronaviral agent;
antiparasitic agent;
apoptosis inducer;
molluscicide;
piscicide;
STAT3 inhibitor
oleanolic acidhydroxy monocarboxylic acid;
pentacyclic triterpenoid
plant metabolite
nitazoxanidenitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrugbenzamides;
carboxylic ester
loganinbeta-D-glucoside;
cyclopentapyran;
enoate ester;
iridoid monoterpenoid;
methyl ester;
monosaccharide derivative;
secondary alcohol
anti-inflammatory agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
EC 3.4.23.46 (memapsin 2) inhibitor;
neuroprotective agent;
plant metabolite
tetrahydrocurcumintetrahydrocurcumin : A beta-diketone that is curcumin in which both of the double bonds have been reduced to single bonds.beta-diketone;
diarylheptanoid;
polyphenol
metabolite
cryptotanshinonecryptotanshinone: from Salvia miltiorrhizaabietane diterpenoidanticoronaviral agent
ar-turmerone(+)-(S)-ar-turmerone : A sesquiterpenoid that is 2-methylhept-2-en-4-one substituted by a 4-methylphenyl group at position 6. It has been isolated from Peltophorum dasyrachis.

ar-turmerone: potent antivenom against snake bites; isolated form Curcuma longa; structure given in first source
enone;
sesquiterpenoid
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
plant metabolite
swerosideglycoside
nsc 74859NSC 74859: inhibits Stat3 binding activity; structure in first source

S3I-201 : An amidobenzoic acid obtained by formal condensation of the carboxy group of [(4-methylbenzene-1-sulfonyl)oxy]acetic acid with the amino group of 4-amino-2-hydroxybenzoic acid.
amidobenzoic acid;
monohydroxybenzoic acid;
tosylate ester
STAT3 inhibitor
telocinobufagintelocinobufagin: structuresteroid lactone
tizoxanidetizoxanide: major metabolite of nitazoxanide; structure in first sourcesalicylamides
bardoxolone methylmethyl 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oate: structure in first sourcecyclohexenones
bisabololKamillosan: drug combination containing chamomile and bisabolol; used to treat dermatitissesquiterpenoid
ganoderic acid atriterpenoid
piplartinepiplartine: Antineoplastic Agent, Phytogenic; alkaloid from Piper; structure in first sourcecinnamamides;
dicarboximide
stattic1-benzothiophenes;
C-nitro compound;
sulfone
antineoplastic agent;
radiosensitizing agent;
STAT3 inhibitor
stx-0119STX-0119: antineoplastic; structure in first source
genistein7-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
andrographolidecarbobicyclic compound;
gamma-lactone;
labdane diterpenoid;
primary alcohol;
secondary alcohol
anti-HIV agent;
anti-inflammatory drug;
antineoplastic agent;
metabolite
nifuroxazidenifuroxazide: structurebenzoic acids
hylin
2-acetylfuranonaphthoquinone2-acetylfuranonaphthoquinone: has antineoplastic activity; structure in first source
5,15-diphenylporphine5,15-diphenylporphine: structure in first source
wp1066
azd 1480
bp-1-102BP-1-102: a STAT3 inhibitor; structure in first source
phaeosphaeride aphaeosphaeride A: inhibits STAT3-dependent signaling; structure in first source
hydrazinocurcuminhydrazinocurcumin : A pyrazole obtained by cyclocodensation of the two carbonyl groups of curcumin with hydrazine.

hydrazinocurcumin: structure in first source
aromatic ether;
olefinic compound;
polyphenol;
pyrazoles
angiogenesis modulating agent;
antineoplastic agent;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor