Literature summary for 2.7.1.78 extracted from

Freschauf, G.K.; Mani, R.S.; Mereniuk, T.R.; Fanta, M.; Virgen, C.A.; Dianov, G.L.; Grassot, J.M.; Hall, D.G.; Weinfeld, M.
Mechanism of action of an imido-piperidine inhibitor of human polynucleotide kinase/phosphatase (2010), J. Biol. Chem., 285, 2351-2360.

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Cloned(Commentary)

Cloned (Comment)	Organism
the PNKP mutants are subcloned into the vector pET16b for expression in Escherichia coli BL21DE3 pLysS cells	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
W331F	single mutant, 90% phosphatase activity	Homo sapiens
W402F	single mutant, 85% phosphatase activity	Homo sapiens
WFX402	mutant, all tryptophans except 402 are replaced by phenylalanine, 85% phosphatase activity	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione	A12B4C3, noncompetitive inhibition	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + 5'-dephospho-DNA	Homo sapiens	-	ADP + 5'-phospho-DNA	-	r

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q96T60	-	-

Purification (Commentary)

Purification (Comment)	Organism
the mutant proteins are purified using ProBond resin	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
A-549 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + 5'-dephospho-DNA	-	Homo sapiens	ADP + 5'-phospho-DNA	-	r

Synonyms

Synonyms	Comment	Organism
PNKP	-	Homo sapiens
polynucleotide kinase/phosphatase	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	inhibition assay	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.4	-	inhibition assay	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
additional information	-	additional information	effect of A12B4C3 binding on the W331F mutant, 95% inhibition	Homo sapiens
additional information	-	additional information	effect of A12B4C3 binding on the W402F mutant, 6% inhibition	Homo sapiens
additional information	-	additional information	effect of A12B4C3 binding on the WFX402 mutant, 90% inhibition	Homo sapiens
additional information	-	additional information	effect of A12B4C3 binding on the wild-type PNKP, 100% inhibition	Homo sapiens

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Release 2023.1 (January 2023)