Literature summary for 5.6.1.3 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
kinesin spindle protein activator-1	accelerates the basal ATP turnover rate circa 10fold in the absence of microtubules	Homo sapiens

Cloned(Commentary)

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

Protein Variants

Protein Variants	Comment	Organism
A133D	ispinesib-resistant KSP mutant	Homo sapiens
D130V	ispinesib-resistant KSP mutant	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
ispinesib	SB-715992, a potent and selective inhibitor of kinesin spindle protein	Homo sapiens
kinesin spindle protein activator-1	inhibits kinesin spindle protein ATP turnover in the presence of microtubules	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.014	-	ATP	in the presence of microtubules	Homo sapiens
0.03	-	ATP	in the absence of microtubules	Homo sapiens
46	-	ATP	in the absence of microtubules with 0.05 mM kinesin spindle protein activator-1	Homo sapiens
103	-	ATP	in the presence of microtubules, with 0.03 mM kinesin spindle protein activator-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.
additional information	Homo sapiens	kinesin spindle protein is essential for mitotic spindle assembly in dividing human cells and is required for cell cycle progression through mitosis	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Purification (Commentary)

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

Source Tissue

Source Tissue	Comment	Organism	Textmining
HCT-116 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + H2O + a kinesin associated with a microtubule at position n	-	Homo sapiens	ADP + phosphate + a kinesin associated with a microtubule at position n+1 (toward the plus end)	-	?
additional information	kinesin spindle protein is essential for mitotic spindle assembly in dividing human cells and is required for cell cycle progression through mitosis	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
kinesin spindle protein	a member of the kinesin-5 family	Homo sapiens
sEg5	-	Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
0.2	-	ATP	in the absence of microtubules	Homo sapiens
1.4	-	ATP	in the absence of microtubules with 0.05 mM kinesin spindle protein activator-1	Homo sapiens
4.4	-	ATP	in the presence of microtubules, with 0.03 mM kinesin spindle protein activator-1	Homo sapiens
13	-	ATP	in the presence of microtubules	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0023	-	-	Homo sapiens	kinesin spindle protein activator-1

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Release 2023.1 (January 2023)