BRENDA - Enzyme Database show
show all sequences of 5.99.1.2

New tanshinone I derivatives S222 and S439 similarly inhibit topoisomerase I/II but reveal different p53-dependency in inducing G2/M arrest and apoptosis

Tian, Q.T.; Ding, C.Y.; Song, S.S.; Wang, Y.Q.; Zhang, A.; Miao, Z.H.; Biochem. Pharmacol. 154, 255-264 (2018)

Data extracted from this reference:

Inhibitors
Inhibitors
Commentary
Organism
Structure
4-[3-[ethyl(methyl)amino]propyl]furo[3,2-c]phenanthridine-5,10,11(4H)-trione
-
Homo sapiens
hydroxylcamptothecin
topoisomerase I inhibitor
Homo sapiens
N,N-dimethyl(6-methyl-10,11-dioxo-10,11-dihydrophenanthro[1,2-b]furan-1-yl)methanaminium (2E)-3-carboxyprop-2-enoate
-
Homo sapiens
tanshinone-1
less than 10% inhibition at 0.005 mM
Homo sapiens
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
P11387
-
-
Source Tissue
Source Tissue
Commentary
Organism
Textmining
A-549 cell
-
Homo sapiens
-
BEL-7402 cell
-
Homo sapiens
-
CAL-51 cell
-
Homo sapiens
-
HCT-116 cell
-
Homo sapiens
-
HCT-15 cell
-
Homo sapiens
-
HT-29 cell
-
Homo sapiens
-
KB cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-
MDA-MB-436 cell
-
Homo sapiens
-
MDA-MB-468 cell
-
Homo sapiens
-
MX-1 cell
-
Homo sapiens
-
SMMC-7721 cell
-
Homo sapiens
-
SPC-A4 cell
-
Homo sapiens
-
SW-620 cell
-
Homo sapiens
-
UWB1.289 cell
-
Homo sapiens
-
UWB1.289+BRCA1 cell
-
Homo sapiens
-
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
supercoiled plasmid DNA pBR322
-
747038
Homo sapiens
relaxed plasmid DNA pBR322
-
-
-
?
IC50 Value
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.02149
-
at pH 8.0 and 37°C
Homo sapiens
tanshinone-1
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.02149
-
at pH 8.0 and 37°C
Homo sapiens
tanshinone-1
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
4-[3-[ethyl(methyl)amino]propyl]furo[3,2-c]phenanthridine-5,10,11(4H)-trione
-
Homo sapiens
hydroxylcamptothecin
topoisomerase I inhibitor
Homo sapiens
N,N-dimethyl(6-methyl-10,11-dioxo-10,11-dihydrophenanthro[1,2-b]furan-1-yl)methanaminium (2E)-3-carboxyprop-2-enoate
-
Homo sapiens
tanshinone-1
less than 10% inhibition at 0.005 mM
Homo sapiens
Source Tissue (protein specific)
Source Tissue
Commentary
Organism
Textmining
A-549 cell
-
Homo sapiens
-
BEL-7402 cell
-
Homo sapiens
-
CAL-51 cell
-
Homo sapiens
-
HCT-116 cell
-
Homo sapiens
-
HCT-15 cell
-
Homo sapiens
-
HT-29 cell
-
Homo sapiens
-
KB cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-
MDA-MB-436 cell
-
Homo sapiens
-
MDA-MB-468 cell
-
Homo sapiens
-
MX-1 cell
-
Homo sapiens
-
SMMC-7721 cell
-
Homo sapiens
-
SPC-A4 cell
-
Homo sapiens
-
SW-620 cell
-
Homo sapiens
-
UWB1.289 cell
-
Homo sapiens
-
UWB1.289+BRCA1 cell
-
Homo sapiens
-
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
supercoiled plasmid DNA pBR322
-
747038
Homo sapiens
relaxed plasmid DNA pBR322
-
-
-
?
Other publictions for EC 5.99.1.2
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
747038
Tian
New tanshinone I derivatives ...
Homo sapiens
Biochem. Pharmacol.
154
255-264
2018
-
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4
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17
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1
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1
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1
4
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17
-
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1
-
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747698
Wu
Structure-based discovery of ...
Homo sapiens
Eur. J. Med. Chem.
148
268-278
2018
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7
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1
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8
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1
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7
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8
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1
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748358
Castelli
Comparative studies of oxindo ...
Homo sapiens
J. Inorg. Biochem.
186
85-94
2018
-
-
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-
4
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1
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1
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1
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1
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749223
Chan
Expression of stable and acti ...
Homo sapiens
Protein Expr. Purif.
141
52-62
2018
-
-
1
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-
1
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1
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1
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1
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1
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1
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1
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747226
Kupriyanova
Arabidopsis DNA topoisomerase ...
Arabidopsis thaliana
Biol. Open
6
832-843
2017
-
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1
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1
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1
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1
1
-
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748369
Ranjan
Selective inhibition of Esche ...
Escherichia coli, Homo sapiens
J. Med. Chem.
60
4904-4922
2017
-
-
-
-
-
-
48
-
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2
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1
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2
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23
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23
48
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1
-
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2
-
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748530
Xin
Discovery of DNA topoisomeras ...
Homo sapiens
Mar. Drugs
15
pii: E217
2017
-
-
-
-
-
-
36
-
-
-
-
-
-
1
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1
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36
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-
-
1
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-
-
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-
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747646
Ang
-
Comparing the expression of h ...
Homo sapiens
Electron. J. Biotechnol.
21
9-17
2016
-
-
1
-
-
-
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1
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1
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747775
Tiwari
Characterization of molecular ...
Escherichia coli
FEBS Lett.
590
2844-2851
2016
-
-
-
-
-
-
-
-
-
1
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1
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1
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1
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1
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748337
Jensen
Characterization of DNA topoi ...
Homo sapiens
J. Exp. Clin. Cancer Res.
35
56
2016
-
-
-
-
2
-
6
-
-
-
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-
-
1
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4
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5
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2
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5
6
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4
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748396
Tan
Insights from the structure o ...
Mycobacterium tuberculosis
J. Mol. Biol.
428
182-193
2016
-
-
1
1
-
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1
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1
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1
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1
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1
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1
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1
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748397
D'Alfonso
Molecular mechanism of DNA to ...
Homo sapiens, Saccharomyces cerevisiae, Saccharomyces cerevisiae W303-1A
J. Mol. Biol.
428
4905-4916
2016
-
-
-
-
2
-
2
-
-
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-
14
-
-
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-
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-
3
-
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2
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2
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3
-
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747474
Puc
Ligand-dependent enhancer act ...
Homo sapiens
Cell
160
367-380
2015
-
-
-
-
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-
-
-
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1
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2
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2
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-
1
1
-
-
-
747693
Yu
Synthesis and biological eval ...
Homo sapiens
Eur. J. Med. Chem.
101
525-533
2015
-
-
-
-
-
-
32
-
-
-
-
-
-
1
-
-
-
-
-
4
-
-
1
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1
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1
32
-
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4
-
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1
-
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-
-
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-
-
748187
Wright
DNA topoisomerase I domain in ...
Homo sapiens
J. Biol. Chem.
290
12068-12078
2015
-
-
1
-
1
-
1
-
-
-
-
-
-
1
-
-
1
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1
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1
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1
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1
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1
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748878
Sirikantaramas
Structural insight of DNA top ...
Camptotheca acuminata, Nothapodytes nimmoniana, Ophiorrhiza pumila
Phytochemistry
113
50-56
2015
-
-
3
-
2
-
12
-
-
-
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-
3
-
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-
2
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3
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2
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12
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2
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747263
de Oliveira Figueiredo
Further constituents of Galia ...
Homo sapiens
Bioorg. Med. Chem. Lett.
24
1358-1361
2014
-
-
-
-
-
-
2
-
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1
-
1
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4
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1
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747994
Kumar
Molecular docking studies of ...
Homo sapiens
Interdiscip. Sci. Comput. Life Sci.
6
285-291
2014
-
-
-
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-
5
-
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1
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748912
Liu
DNA topoisomerase I affects p ...
Arabidopsis thaliana
Plant Cell
26
2803-2817
2014
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1
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1
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1
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1
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1
1
-
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-
748151
Viard
Hyperthermophilic topoisomera ...
Thermotoga maritima, Thermotoga maritima DSM 3109
J. Biol. Chem.
276
46495-46503
2001
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-
1
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2
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1
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2
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1
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2
1
2
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1
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1
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1
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2
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1
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1
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2
1
2
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1
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1
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