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7-(Nalpha-acetyl-glycyl-L-alanyl-Nepsilon-acetyl-L-lysyl)amino-4-methylcoumarin + H2O
?
low activity
-
-
?
7-(Nalpha-acetyl-L-arginyl-glycyl-Nepsilon-acetyl-L-lysyl)-amino-4-methylcoumarin + H2O
?
low activity
-
-
?
acetylcadaverine + H2O
acetate + cadaverine
high acitivity
-
-
?
acetylputrescine + H2O
acetate + putrescine
high acitivity
-
-
?
N-(8-aminooctyl)acetamide + H2O
octane-1,8-diamine + acetate
moderate activity
-
-
?
N-butylacetamide + H2O
butan-1-amine + acetate
low activity
-
-
?
N1,N8-diacetylspermidine + 2 H2O
2 acetate + spermidine
moderate activity
-
-
?
N1-acetylspermine + H2O
acetate + spermine
low activity
-
-
?
N8-acetylspermidine + H2O
acetate + spermidine
Nalpha,Nepsilon-diacetyl-L-lysinamide + H2O
?
low activity
-
-
?
Nalpha-acetyl-L-alanyl-Nepsilon-acetyl-L-lysyl-L-alaninamide + H2O
?
low activity
-
-
?
diacetylspermidine + H2O
acetate + spermidine
-
81.9% activity of that of N8-acetylspermidine
-
?
N1-acetylspermidine + H2O
acetate + spermidine
-
low activity
-
?
N8-acetylspermidine + H2O
acetate + spermidine
-
highest activity
-
?
additional information
?
-
N8-acetylspermidine + H2O
acetate + spermidine
-
-
-
?
N8-acetylspermidine + H2O
acetate + spermidine
-
-
-
-
?
N8-acetylspermidine + H2O
acetate + spermidine
best substrate
-
-
?
additional information
?
-
histone deacetylase 10 (HDAC10) from Homo sapiens is a highly specific N8-acetylspermidine deacetylase. No activity with N1-acetylspermidine and N1-acetylspermine
-
-
?
additional information
?
-
-
histone deacetylase 10 (HDAC10) from Homo sapiens is a highly specific N8-acetylspermidine deacetylase. No activity with N1-acetylspermidine and N1-acetylspermine
-
-
?
additional information
?
-
the conserved glutamate gatekeeper and a sterically constricted active site confer specificity for N8-acetylspermidine hydrolysis and disfavour acetyllysine hydrolysis. Analysis of the intermolecular interactions of N8-acetylspermidine in the active site of hHDAC10 based on the structure of the Danio rerio enzyme-inhibitor crystal structure zHDAC10-AAT complex. No activity with N-(3-aminopropyl)acetamide, TK(ac)PIW, AK(ac)P, GAK(ac), AK(ac), K(ac)NL, K(ac)NL, and GAK(ac)NLQ
-
-
?
additional information
?
-
-
the conserved glutamate gatekeeper and a sterically constricted active site confer specificity for N8-acetylspermidine hydrolysis and disfavour acetyllysine hydrolysis. Analysis of the intermolecular interactions of N8-acetylspermidine in the active site of hHDAC10 based on the structure of the Danio rerio enzyme-inhibitor crystal structure zHDAC10-AAT complex. No activity with N-(3-aminopropyl)acetamide, TK(ac)PIW, AK(ac)P, GAK(ac), AK(ac), K(ac)NL, K(ac)NL, and GAK(ac)NLQ
-
-
?
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7-[(3-aminopropyl)amino]-1,1,1-trifluoroheptan-2-one
2-mercaptoethanol
-
slight inhibition at 1 mM
8-hydroxyquinoline
-
slight inhibition at 1 mM
Acriflavin
-
strong inhibition at 1 mM
Cu2+
-
nearly complete inhibition at 1 mM
dithiothreitol
-
remarkable inhibition at 1 mM
Fe2+
-
strong inhibition at 1 mM
iodoacetamide
-
slight inhibition at 1 mM
NaN3
-
slight inhibition at 1 mM
p-chloromercuribenzoic acid
-
complete inhibition at 1 mM
Pargyline
-
slight inhibition at 1 mM
Quinacrine
-
strong inhibition at 1 mM
Semicarbazide
-
slight inhibition at 1 mM
7-[(3-aminopropyl)amino]-1,1,1-trifluoroheptan-2-one
AAT, binds as a tetrahedral gem-diolate to both APAH (acetylpolyamine amidohydrolase, EC 3.5.1.62) and HDAC10, thereby mimicking the tetrahedral intermediate and its flanking transition states in catalysis
7-[(3-aminopropyl)amino]-1,1,1-trifluoroheptan-2-one
AAT, the inhibitor binds as a transition state analogue
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Adenocarcinoma of Lung
HDAC10 Regulates Cancer Stem-Like Cell Properties in KRAS-Driven Lung Adenocarcinoma.
Adrenal Cortex Neoplasms
Comprehensive DNA methylation analysis of benign and malignant adrenocortical tumors.
Carcinogenesis
HDAC10 expression is associated with DNA mismatch repair gene and is a predictor of good prognosis in colon carcinoma.
Carcinogenesis
HDAC10 Regulates Cancer Stem-Like Cell Properties in KRAS-Driven Lung Adenocarcinoma.
Carcinogenesis
Histone deacetylase 10 exerts anti-tumor effects on cervical cancer via a novel microRNA-223/TXNIP/Wnt/?-catenin pathway.
Carcinogenesis
Histone deacetylase 10 exerts antitumor effects on cervical cancer via a novel microRNA-223/TXNIP/Wnt/?-catenin pathway.
Carcinoma
HDAC10 as a potential therapeutic target in ovarian cancer.
Carcinoma
HDAC10 expression is associated with DNA mismatch repair gene and is a predictor of good prognosis in colon carcinoma.
Carcinoma
HDAC10 Is Positively Associated With PD-L1 Expression and Poor Prognosis in Patients With NSCLC.
Carcinoma
Histone Deacetylase (HDAC) 10 Suppresses Cervical Cancer Metastasis through Inhibition of Matrix Metalloproteinase (MMP) 2 and 9 Expression.
Carcinoma
Histone deacetylase 10 suppresses proliferation and invasion by inhibiting the phosphorylation of ?-catenin and serves as an independent prognostic factor for human clear cell renal cell carcinoma.
Carcinoma, Hepatocellular
Growth attenuation is associated with histone deacetylase 10-induced autophagy in the liver.
Carcinoma, Renal Cell
Histone deacetylase 10 suppresses proliferation and invasion by inhibiting the phosphorylation of ?-catenin and serves as an independent prognostic factor for human clear cell renal cell carcinoma.
Carcinoma, Squamous Cell
Histone Deacetylase (HDAC) 10 Suppresses Cervical Cancer Metastasis through Inhibition of Matrix Metalloproteinase (MMP) 2 and 9 Expression.
Colitis
HDAC10 deletion promotes Foxp3+ T-regulatory cell function.
Colonic Neoplasms
HDAC10 expression is associated with DNA mismatch repair gene and is a predictor of good prognosis in colon carcinoma.
Kidney Neoplasms
DDX39B Predicts Poor Survival and Associated with Clinical Benefit of Anti-PD-L1 Therapy in ccRCC.
Leukemia, Lymphocytic, Chronic, B-Cell
Expression and Function of Histone Deacetylase 10 (HDAC10) in B Cell Malignancies.
Lung Neoplasms
4-hydroxyphenylpyruvate dioxygenase promotes lung cancer growth via pentose phosphate pathway (PPP) flux mediated by LKB1-AMPK/HDAC10/G6PD axis.
Lung Neoplasms
HDAC10 Is Positively Associated With PD-L1 Expression and Poor Prognosis in Patients With NSCLC.
Lung Neoplasms
HDAC10 promotes lung cancer proliferation via AKT phosphorylation.
Lung Neoplasms
HDAC10 Regulates Cancer Stem-Like Cell Properties in KRAS-Driven Lung Adenocarcinoma.
Lymphatic Metastasis
Histone Deacetylase (HDAC) 10 Suppresses Cervical Cancer Metastasis through Inhibition of Matrix Metalloproteinase (MMP) 2 and 9 Expression.
Lymphoma
Expression and Function of Histone Deacetylase 10 (HDAC10) in B Cell Malignancies.
Lymphoma, Mantle-Cell
Expression and Function of Histone Deacetylase 10 (HDAC10) in B Cell Malignancies.
Malnutrition
Growth attenuation is associated with histone deacetylase 10-induced autophagy in the liver.
Neoplasm Metastasis
Histone Deacetylase (HDAC) 10 Suppresses Cervical Cancer Metastasis through Inhibition of Matrix Metalloproteinase (MMP) 2 and 9 Expression.
Neoplasm Metastasis
Histone deacetylase 10 exerts anti-tumor effects on cervical cancer via a novel microRNA-223/TXNIP/Wnt/?-catenin pathway.
Neoplasm Metastasis
Histone deacetylase 10 exerts antitumor effects on cervical cancer via a novel microRNA-223/TXNIP/Wnt/?-catenin pathway.
Neoplasm Metastasis
Histone deacetylase 10 suppresses proliferation and invasion by inhibiting the phosphorylation of ?-catenin and serves as an independent prognostic factor for human clear cell renal cell carcinoma.
Neoplasm Metastasis
Suppression of lung cancer cell invasion and metastasis by connexin43 involves the secretion of follistatin-like 1 mediated via histone acetylation.
Neoplasms
4-hydroxyphenylpyruvate dioxygenase promotes lung cancer growth via pentose phosphate pathway (PPP) flux mediated by LKB1-AMPK/HDAC10/G6PD axis.
Neoplasms
Binding of N8-Acetylspermidine Analogues to Histone Deacetylase 10 Reveals Molecular Strategies for Blocking Polyamine Deacetylation.
Neoplasms
Decreased expression of histone deacetylase 10 predicts poor prognosis of gastric cancer patients.
Neoplasms
Expression and Function of Histone Deacetylase 10 (HDAC10) in B Cell Malignancies.
Neoplasms
HDAC10 as a potential therapeutic target in ovarian cancer.
Neoplasms
HDAC10 expression is associated with DNA mismatch repair gene and is a predictor of good prognosis in colon carcinoma.
Neoplasms
HDAC10 promotes lung cancer proliferation via AKT phosphorylation.
Neoplasms
HDAC10 Regulates Cancer Stem-Like Cell Properties in KRAS-Driven Lung Adenocarcinoma.
Neoplasms
Histone Deacetylase (HDAC) 10 Suppresses Cervical Cancer Metastasis through Inhibition of Matrix Metalloproteinase (MMP) 2 and 9 Expression.
Neoplasms
Histone deacetylase 10 exerts anti-tumor effects on cervical cancer via a novel microRNA-223/TXNIP/Wnt/?-catenin pathway.
Neoplasms
Histone deacetylase 10 exerts antitumor effects on cervical cancer via a novel microRNA-223/TXNIP/Wnt/?-catenin pathway.
Neoplasms
Histone deacetylase 10 promotes autophagy-mediated cell survival.
Neoplasms
Histone deacetylase 10 suppresses proliferation and invasion by inhibiting the phosphorylation of ?-catenin and serves as an independent prognostic factor for human clear cell renal cell carcinoma.
Neoplasms
Histone deacetylase 10, a potential epigenetic target for therapy.
Neoplasms
Histone deacetylase 10-promoted autophagy as a druggable point of interference to improve the treatment response of advanced neuroblastomas.
Neoplasms
Selective Inhibitors of Histone Deacetylase 10 (HDAC-10).
Neoplasms
The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines.
Neoplasms
X-ray Crystallographic Snapshots of Substrate Binding in the Active Site of Histone Deacetylase 10.
Neuroblastoma
Binding of N8-Acetylspermidine Analogues to Histone Deacetylase 10 Reveals Molecular Strategies for Blocking Polyamine Deacetylation.
Neuroblastoma
Dual role of HDAC10 in lysosomal exocytosis and DNA repair promotes neuroblastoma chemoresistance.
Neuroblastoma
Histone deacetylase 10 promotes autophagy-mediated cell survival.
Neuroblastoma
Histone deacetylase 10-promoted autophagy as a druggable point of interference to improve the treatment response of advanced neuroblastomas.
Neuroblastoma
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
Neuroblastoma
Selective Inhibitors of Histone Deacetylase 10 (HDAC-10).
Neuroblastoma
The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines.
Ovarian Neoplasms
HDAC10 as a potential therapeutic target in ovarian cancer.
Pulmonary Disease, Chronic Obstructive
Gene expression profile of human lung in a relatively early stage of COPD with emphysema.
Stomach Neoplasms
Decreased expression of histone deacetylase 10 predicts poor prognosis of gastric cancer patients.
Stomach Neoplasms
Inhibition of histone deacetylase 10 induces thioredoxin-interacting protein and causes accumulation of reactive oxygen species in SNU-620 human gastric cancer cells.
Uterine Cervical Neoplasms
Histone Deacetylase (HDAC) 10 Suppresses Cervical Cancer Metastasis through Inhibition of Matrix Metalloproteinase (MMP) 2 and 9 Expression.
Uterine Cervical Neoplasms
Histone deacetylase 10 exerts anti-tumor effects on cervical cancer via a novel microRNA-223/TXNIP/Wnt/?-catenin pathway.
Uterine Cervical Neoplasms
Histone deacetylase 10 exerts antitumor effects on cervical cancer via a novel microRNA-223/TXNIP/Wnt/?-catenin pathway.
Uterine Cervical Neoplasms
Oncogenic miRNA-1908 targets HDAC10 and promotes the aggressive phenotype of cervical cancer cell.
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0.01
7-(Nalpha-acetyl-glycyl-L-alanyl-Nepsilon-acetyl-L-lysyl)amino-4-methylcoumarin
pH 8.0, 22°C, recombinant enzyme
0.11
7-(Nalpha-acetyl-L-arginyl-glycyl-Nepsilon-acetyl-L-lysyl)-amino-4-methylcoumarin
pH 8.0, 22°C, recombinant enzyme
0.11
Acetylcadaverine
pH 8.0, 22°C, recombinant enzyme
0.17
acetylputrescine
pH 8.0, 22°C, recombinant enzyme
0.16
N-(8-aminooctyl)acetamide
pH 8.0, 22°C, recombinant enzyme
0.15
N1,N8-diacetylspermidine
pH 8.0, 22°C, recombinant enzyme
0.18
N1-acetylspermine
pH 8.0, 22°C, recombinant enzyme
0.1
N8-Acetylspermidine
pH 8.0, 22°C, recombinant enzyme
0.14
Nalpha,Nepsilon-diacetyl-L-lysinamide
pH 8.0, 22°C, recombinant enzyme
0.06
Nalpha-acetyl-L-alanyl-Nepsilon-acetyl-L-lysyl-L-alaninamide
pH 8.0, 22°C, recombinant enzyme
0.211
N8-Acetylspermidine
-
-
additional information
additional information
-
additional information
additional information
steady-state kinetics
-
additional information
additional information
-
steady-state kinetics
-
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0.00038
7-(Nalpha-acetyl-glycyl-L-alanyl-Nepsilon-acetyl-L-lysyl)amino-4-methylcoumarin
pH 8.0, 22°C, recombinant enzyme
0.008
7-(Nalpha-acetyl-L-arginyl-glycyl-Nepsilon-acetyl-L-lysyl)-amino-4-methylcoumarin
pH 8.0, 22°C, recombinant enzyme
0.14
Acetylcadaverine
pH 8.0, 22°C, recombinant enzyme
0.35
acetylputrescine
pH 8.0, 22°C, recombinant enzyme
0.1
N-(8-aminooctyl)acetamide
pH 8.0, 22°C, recombinant enzyme
0.14
N1,N8-diacetylspermidine
pH 8.0, 22°C, recombinant enzyme
0.011
N1-acetylspermine
pH 8.0, 22°C, recombinant enzyme
0.28
N8-Acetylspermidine
pH 8.0, 22°C, recombinant enzyme
0.0092
Nalpha,Nepsilon-diacetyl-L-lysinamide
pH 8.0, 22°C, recombinant enzyme
0.0006
Nalpha-acetyl-L-alanyl-Nepsilon-acetyl-L-lysyl-L-alaninamide
pH 8.0, 22°C, recombinant enzyme
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0.038
7-(Nalpha-acetyl-glycyl-L-alanyl-Nepsilon-acetyl-L-lysyl)amino-4-methylcoumarin
pH 8.0, 22°C, recombinant enzyme
0.072
7-(Nalpha-acetyl-L-arginyl-glycyl-Nepsilon-acetyl-L-lysyl)-amino-4-methylcoumarin
pH 8.0, 22°C, recombinant enzyme
1.27
Acetylcadaverine
pH 8.0, 22°C, recombinant enzyme
2.06
acetylputrescine
pH 8.0, 22°C, recombinant enzyme
0.93
N-(8-aminooctyl)acetamide
pH 8.0, 22°C, recombinant enzyme
0.14
N1,N8-diacetylspermidine
pH 8.0, 22°C, recombinant enzyme
0.061
N1-acetylspermine
pH 8.0, 22°C, recombinant enzyme
2.8
N8-Acetylspermidine
pH 8.0, 22°C, recombinant enzyme
0.066
Nalpha,Nepsilon-diacetyl-L-lysinamide
pH 8.0, 22°C, recombinant enzyme
0.01
Nalpha-acetyl-L-alanyl-Nepsilon-acetyl-L-lysyl-L-alaninamide
pH 8.0, 22°C, recombinant enzyme
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evolution
the enzyme adopts the characteristic arginase-deacetylase fold and employ a Zn2+-activated water molecule for catalysis. The active sites of HDAC10 and APAH (acetylpolyamine amidohydrolase, EC 3.5.1.62) are sterically constricted to enforce specificity for long, slender polyamine substrates and exclude bulky peptides and proteins containing acetyl-L-lysine. The tertiary structure (a unique 310 helix defined by the P(E,A)CE motif) provides the steric constriction that directs the polyamine substrate specificity of HDAC10. Structure and catalytic mechanism of polyamine deacetylases, comparison of HDAC and APAH, overview
physiological function
cationic polyamines such as spermidine and spermine are critical in all forms of life, as they regulate the function of biological macromolecules. Intracellular polyamine metabolism is regulated by reversible acetylation and dysregulated polyamine metabolism is associated with neoplastic diseases such as colon cancer, prostate cancer and neuroblastoma. Both HDAC10 and its product spermidine are known to promote cellular survival through autophagy
physiological function
HDAC10 and spermidine act as mediators of autophagy
additional information
nucleophilic attack of Zn2+-bound water at the amide carbonyl group polarized by Zn2+ and the catalytic tyrosine is facilitated by a general base. The Zn2+ ion, tyrosine, and tandem histidine residues contribute to transition state stabilization in each deacetylase. Collapse of the tetrahedral intermediate requires a proton donor, and the second histidine of the tandem pair must serve as the general acid due to its proximity to the leaving amino group. Structure-function analysis of substrate specificity, overview
additional information
-
nucleophilic attack of Zn2+-bound water at the amide carbonyl group polarized by Zn2+ and the catalytic tyrosine is facilitated by a general base. The Zn2+ ion, tyrosine, and tandem histidine residues contribute to transition state stabilization in each deacetylase. Collapse of the tetrahedral intermediate requires a proton donor, and the second histidine of the tandem pair must serve as the general acid due to its proximity to the leaving amino group. Structure-function analysis of substrate specificity, overview
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Suzuke, O.; Kumazawa, T.; Seno, H.; Matsumoto, T.
Acetylspermidine deacetylase activities in human organs
Med. Sci. Res.
15
675-676
1987
Homo sapiens
-
brenda
Shinsky, S.A.; Christianson, D.W.
Polyamine deacetylase structure and catalysis prokaryotic acetylpolyamine amidohydrolase and eukaryotic HDAC10
Biochemistry
57
3105-3114
2018
Danio rerio (F1QCV2), Danio rerio, Homo sapiens (Q969S8), Homo sapiens
brenda
Hai, Y.; Shinsky, S.A.; Porter, N.J.; Christianson, D.W.
Histone deacetylase 10 structure and molecular function as a polyamine deacetylase
Nat. Commun.
8
15368
2017
Danio rerio (F1QCV2), Danio rerio, Homo sapiens (Q969S8), Homo sapiens
brenda