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Literature summary for 2.1.1.366 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
Search for more literature for 2.1.1.366

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
0.39
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.43
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 pH 7.6, 23°C Homo sapiens
0.52
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.66
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, pH 7.6, 23°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q15047
-
-

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
0.005
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.013
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.038
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 pH 7.6, 23°C Homo sapiens
0.065
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-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
0.013
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.026
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, SETDB1:ATF7IP complex, pH 7.6, 23°C Homo sapiens
0.089
-
 [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9 pH 7.6, 23°C Homo sapiens
0.098
-
 S-adenosyl-L-methionine substrate [histone H3 peptide 1-15]-N6,N6-dimethyl-L-lysine9, pH 7.6, 23°C Homo sapiens