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Literature summary for 5.6.2.1 extracted from

  • Roy, A.; Das, B.B.; Ganguly, A.; Bosedasgupta, S.; Khalkho, N.V.; Pal, C.; Dey, S.; Giri, V.S.; Jaisankar, P.; Dey, S.; Majumder, H.K.
    An insight into the mechanism of inhibition of unusual bi-subunit topoisomerase I from Leishmania donovani by 3,3-diindolylmethane, a novel DNA topoisomerase I poison with a strong binding affinity to enzyme (2008), Biochem. J., 409, 611-622.
    View publication on PubMed

Application

Application Comment Organism
drug development 3,3’-diindolylmethane is a novel Leishmania donovani topoisomerase I poison which acts as a noncompetitive inhibitor. So this intriguing dietary component might be exploited for therapeutic development against leishmaniasis Leishmania donovani

Cloned(Commentary)

Cloned (Comment) Organism
Escherichia coli BL21 (DE3) Leishmania donovani

Inhibitors

Inhibitors Comment Organism Structure
3,3'-diindolylmethane (DIM) novel DNA topoisomerase I poison, which is a class I noncompetitive inhibitor, strongly inhibits Leishmania donovani topoisomerase I and stabilizes topoisomerase I-DNA cleavable complex Leishmania donovani
camptothecin most widely studied inhibitor of type IB topoisomerase Leishmania donovani
dihydrobetulinic acid catalytic inhibitor of topoisomerase I, inhibits the suicidal cleavage reaction Leishmania donovani

Organism

Organism UniProt Comment Textmining
Leishmania donovani
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Leishmania donovani

Subunits

Subunits Comment Organism
heterodimer DNA topoisomerase I of kinetoplastid protozoan parasite Leishmania donovani is an unusual bi-subunit enzyme. To find out the differential affinity of 3,3’-diindolylmethane towards the large subunit (LdTOP1L) and small subunit (LdTOP1S) of Leishmania donovani topoisomerase I, performed the binding of individual subunits with 3,3’-diindolylmethane by equilibrium dialysis experiment Leishmania donovani

Synonyms

Synonyms Comment Organism
bi-subunit topoisomerase I
-
Leishmania donovani
DNA topoisomerase
-
Leishmania donovani
LdTOP1LS
-
Leishmania donovani
Topoisomerase I
-
Leishmania donovani

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0012
-
potent inhibitor of Leishmania donovani topoisomerase I Leishmania donovani 3,3'-diindolylmethane