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Literature summary for 5.6.1.3 extracted from

  • Luo, L.; Parrish, C.A.; Nevins, N.; McNulty, D.E.; Chaudhari, A.M.; Carson, J.D.; Sudakin, V.; Shaw, A.N.; Lehr, R.; Zhao, H.; Sweitzer, S.; Lad, L.; Wood, K.W.; Sakowicz, R.; Annan, R.S.; Huang, P.S.; Jackson, J.R.; Dhanak, D.; Copeland, R.A.; Auger, K.R.
    ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism (2007), Nat. Chem. Biol., 3, 722-726.
    View publication on PubMed
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Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli as C-terminal His-tagged protein Homo sapiens

Protein Variants

Protein Variants Comment Organism
A133D substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors Homo sapiens
A356T substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors Homo sapiens
D130V substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors Homo sapiens
I299F substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors Homo sapiens
additional information mutant KHC-L5, loop L5 replaced by that of kinesin heavy chain. Substantially reduced sensitivity to ispinesib and other quinazoline Eg5 inhibitors Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one
-
 Homo sapiens
docetaxel
-
 Homo sapiens
SB-731489
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isoform Eg5
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000017
-
 6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one wild-type, pH 6.8 Homo sapiens
0.000066
-
 6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one mutant I299F, pH 6.8 Homo sapiens
0.000109
-
 6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one mutant A356T, pH 6.8 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000023
-
 mutant D130V, pH 6.8 Homo sapiens docetaxel
0.0000003
-
 wild-type, pH 6.8 Homo sapiens docetaxel
0.00000045
-
 mutant D130V, pH 6.8 Homo sapiens 6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one
0.00000046
-
 wild-type, pH 6.8 Homo sapiens SB-731489
0.000036
-
 wild-type, pH 6.8 Homo sapiens 6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinolin-2(1H)-one
0.000903
-
 mutant D130V, pH 6.8 Homo sapiens SB-731489