Literature summary for 2.6.1.1 extracted from

Holt, M.C.; Assar, Z.; Beheshti Zavareh, R.; Lin, L.; Anglin, J.; Mashadova, O.; Haldar, D.; Mullarky, E.; Kremer, D.M.; Cantley, L.C.; Kimmelman, A.C.; Stein, A.J.; Lairson, L.L.; Lyssiotis, C.A.
Biochemical characterization and structure-based mutational analysis provide insight into the binding and mechanism of action of novel aspartate aminotransferase inhibitors (2018), Biochemistry, 57, 6604-6614 .

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Cloned(Commentary)

Cloned (Comment)	Organism
expressed in Escherichia coli One Shot BL21 (DE3) cells	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
sitting drop vapor diffusion method, using 25% (w/v) polyethylene glycol 3350 5% (w/v) Cymal, and 0.1 M sodium acetate trihydrate (pH 4.5)	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
S256A	the mutant shows 3.51% activity compared to the wild type enzyme	Homo sapiens
T110A	the mutant shows 2.45% activity compared to the wild type enzyme	Homo sapiens
T110A/S256A	inactive	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
4-(1H-indol-4-yl)-N-phenylpiperazine-1-carboxamide	-	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
L-aspartate + 2-oxoglutarate	Homo sapiens	-	oxaloacetate + L-glutamate	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P17174	-	-

Purification (Commentary)

Purification (Comment)	Organism
HisTrap column chromatography and Sephacryl S-200 gel filtration	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
colonic cancer cell	-	Homo sapiens	-
DLD-1 cell	-	Homo sapiens	-
pancreatic cancer cell	-	Homo sapiens	-
PaTu-8902 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
L-aspartate + 2-oxoglutarate	-	Homo sapiens	oxaloacetate + L-glutamate	-	?

Synonyms

Synonyms	Comment	Organism
aspartate aminotransferase 1	-	Homo sapiens
glutamate oxaloacetate transaminase 1	-	Homo sapiens
GOT1	-	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
pyridoxal 5'-phosphate	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0113	-	at pH 7.4 and 37°C	Homo sapiens	4-(1H-indol-4-yl)-N-phenylpiperazine-1-carboxamide

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Release 2023.1 (January 2023)