Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.3.1.B43 extracted from

  • Suenkel, B.; Fischer, F.; Steegborn, C.
    Inhibition of the human deacylase Sirtuin 5 by the indole GW5074 (2012), Bioorg. Med. Chem. Lett., 23, 143-146.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-(3,5-dibromo-4-hydroxybenzyliden)-5-iodo-1,3-dihydroindol-2-one i.e. GW5074, potent inhibitor for desuccinylation activity of Sirt5. 0.1 mM inhibitor reduces Sirt5 desuccinylation activity (substrate: SKEYFS-(succinylLys)-QK) to about 15%. Weaker effects in Sirt5 deacetylation assays. Deacetylation activity is reduced to about 30% in presence of 0.1 mM inhibitor Homo sapiens
suramin
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NXA8
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
NAD+ + FKRGVL(N6-acetyl)KEYGVKV acetylated peptide derived from carbamoylphosphate synthetase 1 (CPS1) Homo sapiens nicotinamide + FKRGVLKEYGVKV + 2'-O-acetyl-ADP-ribose
-
?
NAD+ + SKEYFS(N6-succinyl)KQK
-
Homo sapiens nicotinamide + SKEYFSKQK + 2'-O-acetyl-ADP-ribose
-
?
NAD+ + [peptide derived from carbamoyl phosphate synthetase 1]-N6-acetyl-L-lysine
-
Homo sapiens nicotinamide + [peptide derived from carbamoyl phosphate synthetase 1]-L-lysine + 2'-O-acetyl-ADP-ribose
-
?

Synonyms

Synonyms Comment Organism
SIRT5
-
Homo sapiens
sirtuin 5
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0142
-
pH 7.5, temperature not specified in the publication, substrate: acetylated peptide derived from carbamoylphosphate synthetase 1 (CPS1) Homo sapiens suramin
0.0195
-
pH 7.5, temperature not specified in the publication, substrate: SKEYFS-(succinylLys)-QK Homo sapiens 3-(3,5-dibromo-4-hydroxybenzyliden)-5-iodo-1,3-dihydroindol-2-one
0.097
-
pH 7.5, temperature not specified in the publication, substrate: FKRGVL-(acetylLys)-EYGVKV Homo sapiens 3-(3,5-dibromo-4-hydroxybenzyliden)-5-iodo-1,3-dihydroindol-2-one