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Literature summary for 5.6.2.1 extracted from

  • Cortopassi, W.A.; Penna-Coutinho, J.; Aguiar, A.C.; Pimentel, A.S.; Buarque, C.D.; Costa, P.R.; Alves, B.R.; Franca, T.C.; Krettli, A.U.
    Theoretical and experimental studies of new modified isoflavonoids as potential inhibitors of topoisomerase I from Plasmodium falciparum (2014), PLoS ONE, 9, e91191.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 5.6.2.1

Application

Application Comment Organism
drug development the enzyme is a potential selective target for chemotherapy and drug development against malaria Homo sapiens
drug development the enzyme is a potential selective target for chemotherapy and drug development against malaria Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
(6aR,11aS)-11-[(4-methylphenyl)sulfonyl]-6,6a,11,11a-tetrahydro-5H-benzo[a]carbazole binds selectively to PfTopoI Homo sapiens
(6aR,11aS)-11-[(4-methylphenyl)sulfonyl]-6,6a,11,11a-tetrahydro-5H-benzo[a]carbazole binds selectively to PfTopoI Plasmodium falciparum
(7aR,12aS)-5-methylidene-12-[(4-methylphenyl)sulfonyl]-7,7a,12,12a-tetrahydrobenzo[6,7]chromeno[4,3-b]indol-13(5H)-one
-
 Homo sapiens
(7aR,12aS)-5-methylidene-12-[(4-methylphenyl)sulfonyl]-7,7a,12,12a-tetrahydrobenzo[6,7]chromeno[4,3-b]indol-13(5H)-one
-
 Plasmodium falciparum
(7aS,12aS)-10-methoxy-5-methylidene-5,7,7a,12a-tetrahydro-13H-[1]benzofuro[3,2-c]benzo[g]chromen-13-one
-
 Homo sapiens
(7aS,12aS)-10-methoxy-5-methylidene-5,7,7a,12a-tetrahydro-13H-[1]benzofuro[3,2-c]benzo[g]chromen-13-one
-
 Plasmodium falciparum
(7aS,12aS)-11-methoxy-5-methylidene-13-oxo-5,7a,12a,13-tetrahydro-7H-[1]benzofuro[3,2-c]benzo[g]chromene-9-carbaldehyde
-
 Homo sapiens
(7aS,12aS)-11-methoxy-5-methylidene-13-oxo-5,7a,12a,13-tetrahydro-7H-[1]benzofuro[3,2-c]benzo[g]chromene-9-carbaldehyde
-
 Plasmodium falciparum
(7aS,12aS)-5-methylidene-5,7,7a,12a-tetrahydro-13H-[1]benzofuro[3,2-c]benzo[g]chromen-13-one
-
 Homo sapiens
(7aS,12aS)-5-methylidene-5,7,7a,12a-tetrahydro-13H-[1]benzofuro[3,2-c]benzo[g]chromen-13-one
-
 Plasmodium falciparum
camptothecin
-
 Homo sapiens
camptothecin
-
 Plasmodium falciparum
methyl (7aS,12aS)-5-methylidene-13-oxo-5,7a,12a,13-tetrahydro-7H-[1]benzofuro[3,2-c]benzo[g]chromene-9-carboxylate
-
 Homo sapiens
methyl (7aS,12aS)-5-methylidene-13-oxo-5,7a,12a,13-tetrahydro-7H-[1]benzofuro[3,2-c]benzo[g]chromene-9-carboxylate
-
 Plasmodium falciparum
additional information isolation of six synthetic isoflavonoid derivatives that dock in the binding site of inhibitors camptothecin and topotecan inside the enzyme, no inhibition by LQB223, docking and molecular dynamics simulations, overview Homo sapiens
additional information isolation of six synthetic isoflavonoid derivatives that dock in the binding site of inhibitors camptothecin and topotecan inside the enzyme, cytotoxicity in CQ-sensitive (3D7) or CQ-resistant (W2) parasites, overview Plasmodium falciparum
topotecan
-
 Homo sapiens
topotecan
-
 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-

Synonyms

Synonyms Comment Organism
DNA topoisomerase I
-
 Homo sapiens
DNA topoisomerase I
-
 Plasmodium falciparum
HssTopoI
-
 Homo sapiens
PfTopoI
-
 Plasmodium falciparum
Topoisomerase I
-
 Homo sapiens
Topoisomerase I
-
 Plasmodium falciparum