Literature summary for 2.3.1.B41 extracted from

You, W.; Steegborn, C.
Structural basis of sirtuin 6 inhibition by the hydroxamate trichostatin A implications for protein deacylase drug development (2018), J. Med. Chem., 61, 10922-10928 .

Search for more literature for 2.3.1.B41

Cloned(Commentary)

Cloned (Comment)	Organism
gene SIRT6, His-tagged full-length Sirt6 (residues 1-355) in pQE80L.1 vector is expressed in Escherichia coli strain M15[pREP4] and His-tagged Sirt6(13-308) in vector pET151-D-TOPO in Escherichia coli strain Rosetta2 (DE3) pLysS	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
Sirt6/ADP-ribose/trichostatin A complex, hanging drop vapor diffusion method, 10 mg/ml purified recombinant protein Sirt6 and 10 mM ADP-ribose in 50 mM Na-phosphate buffer, pH 7.5, 0.6 mM DTT, and 5% DMSO are mixed with an equal volume of reservoir solution containing 1.6 M (NH4)2SO4, 10% PEG 400, and Bis-Tris buffer, pH 5.7, at 20°C, X-ray diffraction structure determination and analysis at 1.70 A resolution, molecular replacement using a Sirt6/ADP-ribose structure (PDB ID 3K35) as search model, modeling	Homo sapiens

Crystallization (Comment)

Organism

Sirt6/ADP-ribose/trichostatin A complex, hanging drop vapor diffusion method, 10 mg/ml purified recombinant protein Sirt6 and 10 mM ADP-ribose in 50 mM Na-phosphate buffer, pH 7.5, 0.6 mM DTT, and 5% DMSO are mixed with an equal volume of reservoir solution containing 1.6 M (NH4)2SO4, 10% PEG 400, and Bis-Tris buffer, pH 5.7, at 20°C, X-ray diffraction structure determination and analysis at 1.70 A resolution, molecular replacement using a Sirt6/ADP-ribose structure (PDB ID 3K35) as search model, modeling

Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
trichostatin A	TSA, a potent, zinc-chelating hydroxamate inhibitors of zinc-dependent deacylases, which potently and isoform-specifically inhibits Sirt6. Sirtuin 6 inhibition mechanism, structural basis and interaction analysis, detailed overview. The binding site are nicotinamide pocket and acyl channel, binding kinetics	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
NAD+ + [protein]-N6-palmitoyl-L-lysine	Homo sapiens	-	nicotinamide + [protein]-L-lysine + 2'-O-palmitoyl-ADP ribose	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q8N6T7	-	-

Purification (Commentary)

Purification (Comment)	Organism
recombinant His-tagged enzyme from Escherichia coli by nickel affinity chromatography, tag cleavage by TEV protease, reverse affinity chromatography, action exchange chromatography, and gel filtration	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
NAD+ + [protein]-N6-palmitoyl-L-lysine	-	Homo sapiens	nicotinamide + [protein]-L-lysine + 2'-O-palmitoyl-ADP ribose	-	?

Synonyms

Synonyms	Comment	Organism
SIRT6	-	Homo sapiens
sirtuin-6	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
25	-	assay at	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.5	-	assay at	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
NAD+	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.45	-	trichostatin A	pH 7.5, 25°C	Homo sapiens