Page last updated: 2024-10-24

positive regulation of deacetylase activity

Definition

Target type: biologicalprocess

Any process that activates or increases the frequency, rate or extent of deacetylase activity, the catalysis of the hydrolysis of an acetyl group or groups from a substrate molecule. [GOC:BHF, GOC:dph, GOC:tb]

Positive regulation of deacetylase activity refers to the cellular processes that enhance or stimulate the activity of deacetylases. Deacetylases are enzymes that remove acetyl groups from proteins, a process known as deacetylation. Deacetylation can alter the structure and function of proteins, affecting a wide range of cellular processes.

The positive regulation of deacetylase activity can be achieved through various mechanisms, including:

* **Increased expression of deacetylases:** This can be achieved through transcriptional upregulation of the genes encoding deacetylases, leading to increased synthesis of these enzymes.
* **Activation of deacetylases:** Deacetylases can be activated by various factors, such as post-translational modifications like phosphorylation or acetylation themselves. These modifications can alter the conformation of the enzyme, promoting its catalytic activity.
* **Removal of inhibitory factors:** Deacetylases can be inhibited by certain proteins or molecules. The removal or inactivation of these inhibitory factors can lead to increased deacetylase activity.
* **Recruitment of deacetylases to specific targets:** Deacetylases are often recruited to specific regions of chromatin or proteins by other proteins or complexes. This recruitment ensures that deacetylation occurs at the appropriate location and targets.

The positive regulation of deacetylase activity plays a crucial role in various cellular processes, including:

* **Gene expression:** Deacetylation can alter the accessibility of DNA to transcription factors, affecting gene expression.
* **Cell growth and proliferation:** Deacetylation can regulate the activity of proteins involved in cell cycle progression and proliferation.
* **Cellular signaling:** Deacetylation can influence the activity of signaling pathways by modifying the function of signaling proteins.
* **Immune responses:** Deacetylation is involved in the regulation of immune cell differentiation and activation.
* **Development:** Deacetylation plays a role in various developmental processes, including embryogenesis and organogenesis.

Overall, the positive regulation of deacetylase activity is a complex and highly regulated process that is essential for maintaining cellular homeostasis and normal physiological function.'
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Proteins (1)

ProteinDefinitionTaxonomy
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaA protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P49354]Homo sapiens (human)

Compounds (30)

CompoundDefinitionClassesRoles
1,10-phenanthroline1,10-phenanthroline: RN given refers to parent cpd; inhibits Zn-dependent metalloproteinasesphenanthrolineEC 2.7.1.1 (hexokinase) inhibitor;
EC 3.4.19.3 (pyroglutamyl-peptidase I) inhibitor
2,2'-dipyridyl2,2'-bipyridine : A bipyridine in which the two pyridine moieties are linked by a bond between positions C-2 and C-2'.

2,2'-Dipyridyl: A reagent used for the determination of iron.
bipyridinechelator;
ferroptosis inhibitor
ethylenediamineethylenediamine : An alkane-alpha,omega-diamine in which the alkane is ethane.

ethylenediamine: RN given refers to parent cpd; edamine is the recommended contraction for the ethylenediamine radical
alkane-alpha,omega-diamineGABA agonist
cortisone acetateCortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders.corticosteroid hormone
gliotoxingliotoxin : A pyrazinoindole with a disulfide bridge spanning a dioxo-substituted pyrazine ring; mycotoxin produced by several species of fungi.

Gliotoxin: A fungal toxin produced by various species of Trichoderma, Gladiocladium fimbriatum, Aspergillus fumigatus, and Penicillium. It is used as an immunosuppressive agent.
dipeptide;
organic disulfide;
organic heterotetracyclic compound;
pyrazinoindole
antifungal agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
immunosuppressive agent;
mycotoxin;
proteasome inhibitor
sch 37370N-acetyldesloratadine: dual antagonist of platelet-activating factor and histamine
desloratadinedesloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.

desloratadine: major metabolite of loratadine
benzocycloheptapyridineanti-allergic agent;
cholinergic antagonist;
drug metabolite;
H1-receptor antagonist
b 581B 581 : A dipeptide obtained from the tetrapeptide Cys-Val-Phe-Met by reduction of the amide carbonyl groups of the Cys and Val residues.

B 581: blocks farnesylated but not geranylgeranylated or myristylated, oncogenic Ras signaling & transformation
dipeptideEC 2.5.1.58 (protein farnesyltransferase) inhibitor;
peptidomimetic
r115777
lonafarniblonafarnib : A 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide that has R configuration. It is used as oral farnesyltransferase inhibitor.

lonafarnib: inhibitor of farnesyl protein transferase
4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamideantineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor
tipifarnibimidazoles;
monochlorobenzenes;
primary amino compound;
quinolone
antineoplastic agent;
apoptosis inducer;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor
l 778,123L-778,123 (free base) : A member of the class of imidazoles that is 1H-imidazole substituted by (4-cyanophenyl)methyl and [4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl groups at positions 1 and 5, respectively. It is a dual inhibitor of FPTase and GGPTase-I.imidazoles;
monochlorobenzenes;
nitrile;
piperazinone;
tertiary amino compound
antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor
halenaquinonehalenaquinone: RN given refers to (S)-isomer; structure in first source
fti 276FTI 276: a ras CAAX (C - Cys; A - aliphatic amino acid; X - Ser or Met) peptidomimetic; inhibits farnesyltransferase; FTI-277 is the methyl ester derivative of FTI-276methionine derivative
lb42908LB42908 : A member of the class of pyrrolecarboxamides that is 1H-pyrrole substituted by [1-(3a,7a-dihydro-1,3-benzodioxol-5-ylmethyl)-1H-imidazol-5-yl]methyl, (4-methylpiperazin-1-yl)carbonyl, and naphthalen-1-yl groups at positions 1, 3 and 4, respectively. It is a potent inhibitor of Ras farnesyltransferase (IC50= 0.9nM against H-Ras and 2.4nM against K-Ras) with potential anticancer activity.

LB42908: structure in first source
farnesyl pyrophosphate2-trans,6-trans-farnesyl diphosphate : The trans,trans-stereoisomer of farnesyl diphosphate.

farnesyl pyrophosphate: a sesquiterpene that dimerizes to SQUALENE; RN given refers to cpd without isomeric designation
farnesyl diphosphateEscherichia coli metabolite;
mouse metabolite
a 228839A 228839: an immunosuppressive agent; structure in first source
bms 2146627-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine: a farnesyltransferase inhibitor; structure in first source

BMS-214662 : A member of the class of benzodiazepines that is 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine substituted by (1H-imidazol-5-yl)methyl, benzyl, (thiophen-2-yl)sulfonyl, and cyano groups at positions 1, 3R, 4 and 7, respectively. It is a potent inhibitor of farnesyltransferase (IC50 = 1.35nM) which was under clinical development for the treatment of solid tumors.
benzenes;
benzodiazepine;
imidazoles;
nitrile;
sulfonamide;
thiophenes
antineoplastic agent;
apoptosis inducer;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor
fti 277
ggti 286GGTI 286: the methyl ester of GGTI-287; inhibits geranylgeranyltransferase
chaetomellic acid achaetomellic acid A: structure given in first source; an inhibitor of farnesyl-protein transferase
kurasoin akurasoin A: protein farnesyltransferase inhibitor; isolated from Paecilomyces; structure in first source
kurasoin bkurasoin B: protein farnesyltransferase inhibitor; isolated from Paecilomyces; structure in first source
manumycinmanumycin A : A polyketide with formula C31H38N2O7 initially isolated from Streptomyces parvulus as a result of a random screening program for farnesyl transferase (FTase) inhibitors. It is a natural product that exhibits anticancer and antibiotic properties.

manumycin: an NSAID; RN given for (1S-(1alpha,3(2E,4E,6S*),5alpha,5(1E,3E,5E),6alpha))-isomer; a farnesyl protein transferase inhibitor; from Streptomyces parvulus; MF C31-H38-N2-O7; structure given in first source
enamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol
antiatherosclerotic agent;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
marine metabolite
clavaric acidclavaric acid: inhibits farnesyl-protein transferase; isolated from Clavariadelphus truncatus; structure in first source
ggti 298GGTI 298: inhibits geranylgeranyltransferase-I; structure in first sourceleucine derivative
sch 44342SCH 44342: inhibits farnesyl protein transferase; structure in first source
lb42708LB42708: farnesyltransferase inhibitor; structure in first source
actinoplanic acid aactinoplanic acid A: isolated from Actinoplanes; inhibits farnesyl-protein transferase; structure in first source
moverastin amoverastin A: inhibits cancer cell migration; isolated from Aspergillus; structure in first source