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Literature summary for 5.6.2.1 extracted from

  • Jensen, N.F.; Agama, K.; Roy, A.; Smith, D.H.; Pfister, T.D.; R?mer, M.U.; Zhang, H.L.; Doroshow, J.H.; Knudsen, B.R.; Stenvang, J.; Bruenner, N.; Pommier, Y.
    Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a new pair of resistance-associated mutations (2016), J. Exp. Clin. Cancer Res., 35, 56 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 5.6.2.1

Protein Variants

Protein Variants Comment Organism
R364K/G717R the mutations lead to resistance towards inhibitors SN-38 and NSC 743400 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
camptothecin
-
 Homo sapiens
epirubicin
-
 Homo sapiens
etoposide
-
 Homo sapiens
NSC 725776
-
 Homo sapiens
NSC 743400
-
 Homo sapiens
SN-38
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
colonic cancer cell
-
 Homo sapiens
-
HCT-116 cell
-
 Homo sapiens
-
HT-29 cell
-
 Homo sapiens
-
LoVo cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
DNA topoisomerase I
-
 Homo sapiens
Top1
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
 wild type enzyme from LoVo cells, pH and temperature not specified in the publication Homo sapiens SN-38
0.00002
-
 wild type enzyme from LoVo cells, pH and temperature not specified in the publication Homo sapiens NSC 725776
0.00003
-
 wild type enzyme from HT-29 cells, pH and temperature not specified in the publication Homo sapiens NSC 725776
0.00005
-
 wild type enzyme from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens SN-38
0.00006
-
 wild type enzyme from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens NSC 725776
0.00006
-
 wild type enzyme from LoVo cells, pH and temperature not specified in the publication Homo sapiens NSC 743400
0.00007
-
 wild type enzyme from HT-29 cells, pH and temperature not specified in the publication Homo sapiens NSC 743400
0.00009
-
 wild type enzyme from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens epirubicin
0.00011
-
 wild type enzyme from LoVo cells, pH and temperature not specified in the publication Homo sapiens epirubicin
0.00013
-
 wild type enzyme from HT-29 cells, pH and temperature not specified in the publication Homo sapiens SN-38
0.00017
-
 wild type enzyme from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens NSC 743400
0.00018
-
 wild type enzyme from HT-29 cells, pH and temperature not specified in the publication Homo sapiens epirubicin
0.0002
-
 mutant enzyme R364K/G717R from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens epirubicin
0.0018
-
 wild type enzyme from LoVo cells, pH and temperature not specified in the publication Homo sapiens etoposide
0.0034
-
 mutant enzyme R364K/G717R from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens SN-38
0.0044
-
 mutant enzyme R364K/G717R from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens etoposide
0.0063
-
 wild type enzyme from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens etoposide
0.0099
-
 wild type enzyme from HT-29 cells, pH and temperature not specified in the publication Homo sapiens etoposide
0.047
-
 mutant enzyme R364K/G717R from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens NSC 725776
0.047
-
 mutant enzyme R364K/G717R from HCT-116 cells, pH and temperature not specified in the publication Homo sapiens NSC 743400