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Literature summary for 2.1.1.368 extracted from

  • Basavapathruni, A.; Gureasko, J.; Porter Scott, M.; Hermans, W.; Godbole, A.; Leland, P.A.; Boriack-Sjodin, P.A.; Wigle, T.J.; Copeland, R.A.; Riera, T.V.
    Characterization of the enzymatic activity of SETDB1 and its 1 1 complex with ATF7IP (2016), Biochemistry, 55, 1645-1651 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
ATF7IP SETDB1 partner protein. SETDB1 and the SETDB1:ATF7IP complex efficiently catalyze both monomethylation and dimethylation of H3K9 peptide substrates. The activity of the binary complex is 4fold lower than SETDB1 alone Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.28
-
[histone H3 peptide 1-15]-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.41
-
[histone H3 peptide 1-15]-L-lysine9 pH 7.6, 23°C Homo sapiens
0.41
-
[histone H3 peptide 1-15]-N6-methyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.53
-
S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.54
-
S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-N6-methyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.56
-
S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-N6-methyl-L-lysine9, pH 7.6, 23°C Homo sapiens
0.59
-
[histone H3 peptide 1-15]-N6-methyl-L-lysine9 pH 7.6, 23°C Homo sapiens
0.68
-
S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-L-lysine9, pH 7.6, 23°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q15047 cf. EC 2.1.1.366
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information H3K9 methylation by SETDB1 occurs in a distributive manner Homo sapiens ?
-
-
S-adenosyl-L-methionine + [histone H3 peptide 1-15]-L-lysine9
-
Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6-methyl-L-lysine9
-
?
S-adenosyl-L-methionine + [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9
-
Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6,N6,N6-trimethyl-L-lysine9
-
?
S-adenosyl-L-methionine + [histone H3 peptide 1-15]-N6-methyl-L-lysine9
-
Homo sapiens S-adenosyl-L-homocysteine + [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.027
-
[histone H3 peptide 1-15]-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.045
-
[histone H3 peptide 1-15]-N6-methyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.072
-
S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.09
-
S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6-methyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.192
-
[histone H3 peptide 1-15]-L-lysine9 pH 7.6, 23°C Homo sapiens
0.293
-
[histone H3 peptide 1-15]-N6-methyl-L-lysine9 pH 7.6, 23°C Homo sapiens
0.337
-
S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-L-lysine9, pH 7.6, 23°C Homo sapiens
0.352
-
S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6-methyl-L-lysine9, pH 7.6, 23°C Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.095
-
[histone H3 peptide 1-15]-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.11
-
[histone H3 peptide 1-15]-N6-methyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.135
-
S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.167
-
S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-N6-methyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.467
-
[histone H3 peptide 1-15]-L-lysine9 pH 7.6, 23°C Homo sapiens
0.495
-
S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-L-lysine9, pH 7.6, 23°C Homo sapiens
0.497
-
[histone H3 peptide 1-15]-N6-methyl-L-lysine9 pH 7.6, 23°C Homo sapiens
0.628
-
S-adenosyl-L-methionine substrate [histoneH3 peptide 1-15]-N6-methyl-L-lysine9, pH 7.6, 23°C Homo sapiens