Literature summary for 5.6.1.1 extracted from

Luo, L.; Carson, J.D.; Molnar, K.S.; Tuske, S.J.; Coales, S.J.; Hamuro, Y.; Sung, C.M.; Sudakin, V.; Auger, K.R.; Dhanak, D.; Jackson, J.R.; Huang, P.S.; Tummino, P.J.; Copeland, R.A.
Conformation-dependent ligand regulation of ATP hydrolysis by human KSP - activation of basal hydrolysis and inhibition of microtubule-stimulated hydrolysis by a single, small molecule modulator (2008), J. Am. Chem. Soc., 130, 7584-7591.

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Activating Compound

Activating Compound	Comment	Organism	Structure
3-[[3-(methylsulfanyl)phenyl]amino]-4-[4-(trifluoromethyl)phenyl]-1H-pyrrole-2,5-dione	accelerates KSP-catalyzed ATP hydrolysis in the absence of microtubules circa 10fold	Homo sapiens

Application

Application	Comment	Organism
medicine	KSPA-1 inhibits the proliferation of tumor cells	Homo sapiens

Cloned(Commentary)

Cloned (Comment)	Organism
the motor domain of wild-type KSP monomer, aa 1-360, is expressed in Escherichia coli BL21DE3 cells	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
3-[[3-(methylsulfanyl)phenyl]amino]-4-[4-(trifluoromethyl)phenyl]-1H-pyrrole-2,5-dione	inhibits microtubule-stimulated ATP hydrolysis by KSP	Homo sapiens
ispinesib	SB-715992	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.014	-	ATP	KSP + microtubules	Homo sapiens
0.03	-	ATP	microtubule-free KSP	Homo sapiens
0.046	-	ATP	microtubule-free KSP + 50 microM KSPA-1	Homo sapiens
0.103	-	ATP	KSP + microtubules + 30 microM KSPA-1	Homo sapiens

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + H2O	Homo sapiens	-	ADP + phosphate	-	ir

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Purification (Commentary)

Purification (Comment)	Organism
using Ni-NTA agarose affinity chromatography	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + H2O	-	Homo sapiens	ADP + phosphate	-	ir

Synonyms

Synonyms	Comment	Organism
kinesin spindle protein	-	Homo sapiens
KSP	-	Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
0.2	-	ATP	microtubule-free KSP	Homo sapiens
1.4	-	ATP	microtubule-free KSP + 50 microM KSPA-1	Homo sapiens
4.4	-	ATP	KSP + microtubules + 30 microM KSPA-1	Homo sapiens
13	-	ATP	KSP + microtubules	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0012	-	3-[[3-(methylsulfanyl)phenyl]amino]-4-[4-(trifluoromethyl)phenyl]-1H-pyrrole-2,5-dione	inhibition of the microtubule-stimulated ATP activity of the ispinesib resistant mutant KHC-L5	Homo sapiens
0.006	-	3-[[3-(methylsulfanyl)phenyl]amino]-4-[4-(trifluoromethyl)phenyl]-1H-pyrrole-2,5-dione	inhibition of the microtubule-stimulated ATP activity	Homo sapiens

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Release 2023.1 (January 2023)