Target type: molecularfunction
Binds to and increases the activity of a deubiquitinase. [GOC:sart, ISBN:0120793709]
Deubiquitinase activator activity refers to the enzymatic function of proteins that enhance the activity of deubiquitinases (DUBs). DUBs are a diverse group of proteases that remove ubiquitin (Ub) chains from target proteins. Ubiquitination, the process of attaching Ub chains to proteins, is a critical cellular regulatory mechanism involved in a wide range of cellular processes including protein degradation, signal transduction, DNA repair, and immune responses.
Deubiquitinase activators can act on DUBs in several ways to enhance their activity:
1. **Regulation of DUB stability:** Some activators bind to and stabilize DUBs, preventing their degradation and increasing their effective concentration.
2. **Modification of DUBs:** Certain activators can modify DUBs through phosphorylation, acetylation, or other post-translational modifications, altering their activity or substrate specificity.
3. **Releasing DUBs from inhibitory complexes:** Some activators can release DUBs from inhibitory complexes, allowing them to interact with their substrates.
4. **Providing a scaffolding function:** Activators can act as scaffolds, bringing DUBs and their substrates into proximity, thereby facilitating the deubiquitination process.
5. **Allosteric activation:** Some activators bind to DUBs at sites distinct from the active site, causing conformational changes that enhance catalytic activity.
By regulating the activity of DUBs, deubiquitinase activators play a crucial role in maintaining cellular homeostasis and controlling a vast array of cellular processes. They have emerged as promising therapeutic targets for diseases ranging from cancer to neurodegenerative disorders.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| WD repeat-containing protein 48 | A WD repeat-containing protein 48 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8TAF3] | Homo sapiens (human) |
| Transitional endoplasmic reticulum ATPase | A transitional endoplasmic reticulum ATPase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P55072] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| clotrimazole | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic | |
| trifluoperazine | N-alkylpiperazine; N-methylpiperazine; organofluorine compound; phenothiazines | antiemetic; calmodulin antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; phenothiazine antipsychotic drug | |
| pimozide | pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group. Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403) | benzimidazoles; heteroarylpiperidine; organofluorine compound | antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| Methylenedioxycinnamic acid | hydroxycinnamic acid | ||
| 3,4-methylenedioxy-beta-nitrostyrene | 3,4-methylenedioxy-beta-nitrostyrene: tyrosine kinase inhibitor that prevents platelet glycoprotein IIb/IIIa activation; structure in first source | ||
| 4-(4-(4-chloro-phenyl)thiazol-2-ylamino)phenol | substituted aniline | ||
| nih-12848 | NIH-12848: inhibits phosphatidylinositol 5-phosphate 4-kinase gamma; structure in first source | ||
| gw 7647 | GW 7647 : A monocarboxylic acid that is 2-(phenylsulfanyl)isobutyric acid in which the phenyl group is substituted at the para- position by a 3-aza-7-cyclohexylhept-1-yl group in which the nitrogen is acylated by a (cyclohexylamino)carbonyl group. GW 7647: a PPAR-alpha agonist; structure in first source | aryl sulfide; monocarboxylic acid; ureas | PPARalpha agonist |
| rottlerin | rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis. rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1); | aromatic ketone; benzenetriol; chromenol; enone; methyl ketone | anti-allergic agent; antihypertensive agent; antineoplastic agent; apoptosis inducer; K-ATP channel agonist; metabolite |
| flupenthixol | cis-flupenthixol : A flupenthixol in which the double bond adopts a cis-configuration. | flupenthixol | dopaminergic antagonist |
| ML240 | ML240 : A member of the class of quinazolines that is quinazoline which is substituted at positions 2, 5 and 8 by 2-amino-1H-benzimidazol-1-yl, benzylnitrilo and methoxy groups, respectively. It is a ATP-competetive inhibitor of AAA ATPase p97, also known as valosin-containing protein (VCP). | aromatic amine; aromatic ether; benzimidazoles; primary amino compound; quinazolines; secondary amino compound | antineoplastic agent |
| ganciclovir | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |