Literature summary for 5.6.2.2 extracted from

Sperry, J.; Lorenzo-Castrillejo, I.; Brimble, M.A.; Machin, F.
Pyranonaphthoquinone derivatives of eleutherin, ventiloquinone L, thysanone and nanaomycin A possessing a diverse topoisomerase II inhibition and cytotoxicity spectrum (2009), Bioorg. Med. Chem., 17, 7131-7137.

Inhibitors

Inhibitors	Comment	Organism
(+)-9-demethyleleutherin	-	Homo sapiens
(+)-9-demethyleleutherin	-	Saccharomyces cerevisiae
(+)-deoxyeleutherin	-	Homo sapiens
(+)-deoxyeleutherin	-	Saccharomyces cerevisiae
(-)-deoxyeleutherin	-	Homo sapiens
(-)-deoxyeleutherin	-	Saccharomyces cerevisiae
(1R,3R)-8-methoxy-1-methyl-5,10-dioxo-3,4,5,10-tetrahydro-1H-benzo[g]isochromene-3-carboxylic acid	-	Homo sapiens
(1R,3R)-8-methoxy-1-methyl-5,10-dioxo-3,4,5,10-tetrahydro-1H-benzo[g]isochromene-3-carboxylic acid	-	Saccharomyces cerevisiae
(1R,3S)-1,3,8-trimethyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Homo sapiens
(1R,3S)-1,3,8-trimethyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Saccharomyces cerevisiae
(1R,3S)-7,9-dimethoxy-1,3,6-trimethyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Homo sapiens
(1R,3S)-7,9-dimethoxy-1,3,6-trimethyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Saccharomyces cerevisiae
(3S)-3-methyl-7,9-bis(propan-2-yloxy)-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Homo sapiens
(3S)-3-methyl-7,9-bis(propan-2-yloxy)-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Saccharomyces cerevisiae
(3S)-7,9-dihydroxy-3-methyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Homo sapiens
(3S)-7,9-dihydroxy-3-methyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Saccharomyces cerevisiae
(3S)-7,9-dimethoxy-3-methyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Homo sapiens
(3S)-7,9-dimethoxy-3-methyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Saccharomyces cerevisiae
(3S)-9-hydroxy-7-methoxy-3-methyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Homo sapiens
(3S)-9-hydroxy-7-methoxy-3-methyl-3,4-dihydro-1H-benzo[g]isochromene-5,10-dione	-	Saccharomyces cerevisiae
7-methoxyeleutherin	-	Homo sapiens
7-methoxyeleutherin	-	Saccharomyces cerevisiae
deoxynanaomycin A	-	Homo sapiens
deoxynanaomycin A	-	Saccharomyces cerevisiae
eleutherin	-	Homo sapiens
eleutherin	-	Saccharomyces cerevisiae
additional information	the enzyme is inhibited by pyranonaphthoquinone derivatives of eleutherin possessing a diverse topoisomerase II inhibition and cytotoxicity spectrum, the natural products are generally weaker inhibitors than their synthetic counterparts, pyranonaphthoquinones do not unspecifically inactivate enzymatic activity, overview. The nature of the substituents at C1 on the pyran ring and oxygenated substituents on the aryl ring are critical for anti-topoII activity, structure-based mechanism, overview. Synthesis of the dimeric pyranonaphthoquinone core of the cardinalins using a palladium catalysed homocoupling of an aryl triflate as a key step	Homo sapiens
additional information	cytotoxicity of eleutherin and pyranonaphthoquinone derivatives, structure-activity study and mechanism, overview	Saccharomyces cerevisiae
nanaomycin A	-	Homo sapiens
nanaomycin A	-	Saccharomyces cerevisiae
thysanone	-	Homo sapiens
thysanone	-	Saccharomyces cerevisiae
ventiloquinone L	-	Homo sapiens
ventiloquinone L	-	Saccharomyces cerevisiae

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Saccharomyces cerevisiae	-	haploid strain BY4741	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	decatenation assay with substrate kinetoplast DNA from protozoa Crithidia fasciculata, and DNA relaxation assay using pRYG plasmid DNA as substrate	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
Top2alpha	-	Homo sapiens
Top2alpha	-	Saccharomyces cerevisiae
TOPOII	-	Homo sapiens
TOPOII	-	Saccharomyces cerevisiae
Topoisomerase II	-	Homo sapiens
Topoisomerase II	-	Saccharomyces cerevisiae

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Homo sapiens
37	-	assay at	Saccharomyces cerevisiae

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
8	-	assay at	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens