Page last updated: 2024-10-24

regulation of cysteine-type endopeptidase activity

Definition

Target type: biologicalprocess

Any process that modulates the frequency, rate or extent of cysteine-type endopeptidase activity. [GOC:obol, GOC:yaf]

Regulation of cysteine-type endopeptidase activity encompasses a multifaceted and intricate process that ensures the precise control of these enzymes, essential for a wide array of cellular functions. Cysteine-type endopeptidases, also known as cysteine proteases, are a family of enzymes that utilize a cysteine residue within their active site for catalysis. Their activity is tightly regulated to prevent uncontrolled proteolysis, which could lead to cellular damage and dysfunction.

The regulation of cysteine-type endopeptidase activity involves multiple mechanisms, including:

* **Transcriptional regulation:** The expression levels of cysteine-type endopeptidases are controlled at the transcriptional level. Transcription factors can bind to specific DNA sequences in the promoter regions of genes encoding these enzymes, either activating or repressing their expression. This allows cells to adjust the production of these enzymes in response to changing cellular needs.

* **Post-translational modifications:** After translation, cysteine-type endopeptidases can undergo various post-translational modifications, such as phosphorylation, glycosylation, or ubiquitination. These modifications can alter the activity, localization, or stability of the enzyme.

* **Activation and inactivation:** Cysteine-type endopeptidases are often produced in inactive forms, known as zymogens. Activation requires proteolytic cleavage, typically by other proteases, to expose the active site. Inactivation can occur through the formation of inactive complexes with specific inhibitors, such as cystatins.

* **Subcellular localization:** The localization of cysteine-type endopeptidases within cells is tightly regulated. These enzymes can be targeted to specific organelles or compartments, where their activity is required. This localization helps to prevent unwanted proteolysis and ensures that the enzymes are active in the appropriate cellular context.

* **Feedback regulation:** Cysteine-type endopeptidases can also be regulated by feedback mechanisms. The products of their enzymatic activity may act as substrates for other enzymes or as inhibitors of the proteases themselves. This allows for fine-tuning of the proteolytic process and prevents excessive proteolysis.

In summary, the regulation of cysteine-type endopeptidase activity is a complex process that involves multiple levels of control, from transcriptional regulation to post-translational modifications, activation/inactivation, subcellular localization, and feedback regulation. This intricate regulatory network ensures the precise control of these enzymes, enabling their essential roles in diverse cellular processes.'
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Proteins (3)

ProteinDefinitionTaxonomy
Baculoviral IAP repeat-containing protein 2A baculoviral IAP repeat-containing protein 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13490]Homo sapiens (human)
Baculoviral IAP repeat-containing protein 3A baculoviral IAP repeat-containing protein 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13489]Homo sapiens (human)
Proteasome subunit beta type-9A proteasome subunit beta type-9 that is encoded in the genome of human. [PRO:DNx]Homo sapiens (human)

Compounds (24)

CompoundDefinitionClassesRoles
chlorpromazinechlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.

Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.
organochlorine compound;
phenothiazines;
tertiary amine
anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
bortezomibamino acid amide;
L-phenylalanine derivative;
pyrazines
antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
sdz 283-910SDZ 283-910: structure in first source
benzyloxycarbonylleucyl-leucyl-leucine aldehydebenzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor

N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.
amino aldehyde;
carbamate ester;
tripeptide
proteasome inhibitor
benzyloxycarbonyl-phe-ala-fluormethylketonecathepsin B inhibitor : A cysteine protease inhibitor which inhibits cathepsin B (EC 3.4.22.1).
am 404anilide
lactacystinlactam;
S-substituted L-cysteine
clasto-lactacystin beta-lactoneclasto-lactacystin beta-lactone: active metabolite of lactacystin; inhibits 20 S proteasome; structure in first source
(-)-n-((2s,3r)-3-amino-2-hydroxy-4-phenyl-butyryl)-l-leucine methyl ester
marizomibmarizomib: a proteasome inhibitor from a marine bacterium Salinospora; structure in first sourcebeta-lactone;
gamma-lactam;
organic heterobicyclic compound;
organochlorine compound;
salinosporamide
antineoplastic agent;
proteasome inhibitor
lbw242LBW242: proapoptotic IAP inhibitor; low MW Smac (Second mitochondria-derived activator of caspases) mimetic; structure in first source
carfilzomibepoxide;
morpholines;
tetrapeptide
antineoplastic agent;
proteasome inhibitor
tyropeptin atyropeptin A: proteasome inhibitors produced by Kitasatospora sp. MK993-dF2; structure in first sourcedipeptide
sm 164SM 164: a bivalent Smac mimetic with antineoplastic activity; structure in first sourcebenzenes;
organic heterobicyclic compound;
secondary carboxamide;
triazoles
antineoplastic agent;
apoptosis inducer;
radiosensitizing agent
pr-957
lcl1611,3-thiazoles;
aromatic ketone;
L-alanine derivative;
monofluorobenzenes;
N-acylpyrrolidine
antineoplastic agent;
apoptosis inducer
delanzomibC-terminal boronic acid peptide;
phenylpyridine;
secondary alcohol;
threonine derivative
antineoplastic agent;
apoptosis inducer;
proteasome inhibitor
at 406
belactosin abelactosin A: isolated from Streptomyces; structure in first source
oprozomibONX 0912: antineoplastic; an orally active proteasome inhibitor; structure in first source
ixazomibixazomib : A glycine derivative that is the amide obtained by formal condensation of the carboxy group of N-(2,5-dichlorobenzoyl)glycine with the amino group of [(1R)-1-amino-3-methylbutyl]boronic acid. The active metabolite of ixazomib citrate, it is used in combination therapy for treatment of multiple myeloma.

ixazomib: a proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708; structure in first source
benzamides;
boronic acids;
dichlorobenzene;
glycine derivative
antineoplastic agent;
apoptosis inducer;
drug metabolite;
orphan drug;
proteasome inhibitor
gdc-0152GDC-0152: structure in first source
birinapantbirinapant: a Smac mimetic with antineoplastic activitydipeptide
nvp-cgm097NVP-CGM097: an MDM2 and HDM2 inhibitor; structure in first source