DNA topoisomerase 1

A type 1B DNA topoisomerase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11387]

Synonyms

EC 5.6.2.1;
DNA topoisomerase I

Research

Bioassay Publications (51)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	1 (1.96)	18.7374
1990's	15 (29.41)	18.2507
2000's	14 (27.45)	29.6817
2010's	13 (25.49)	24.3611
2020's	8 (15.69)	2.80

Compounds (54)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
hoe 33342	Homo sapiens (human)	IC50	50.0000	1	1
bisbenzimidazole	Homo sapiens (human)	IC50	22.8600	1	1
LSM-1442	Homo sapiens (human)	IC50	1.5000	2	2
stallimycin	Homo sapiens (human)	IC50	2.7000	1	1
juglone	Homo sapiens (human)	IC50	8.2600	1	1
netropsin	Homo sapiens (human)	IC50	62.0000	1	1
reserpine	Homo sapiens (human)	IC50	160.0000	1	1
yohimbine	Homo sapiens (human)	IC50	30.0000	1	1
camptothecin	Homo sapiens (human)	IC50	33.2563	21	22
bisbenzimidazole trihydrochloride	Homo sapiens (human)	IC50	30.0000	1	1
etoposide	Homo sapiens (human)	IC50	460.0000	2	3
topotecan hydrochloride	Homo sapiens (human)	IC50	1.0800	1	1
topotecan	Homo sapiens (human)	IC50	3.3000	9	9
9-aminocamptothecin	Homo sapiens (human)	IC50	0.1100	1	1
10,11-methylenedioxy-20-camptothecin	Homo sapiens (human)	IC50	0.0525	2	2
alpha-amyrin	Homo sapiens (human)	IC50	250.0000	1	1
corilagin	Homo sapiens (human)	IC50	40.0000	1	1
gallanilide	Homo sapiens (human)	IC50	100.0000	1	1
10-hydroxycamptothecin	Homo sapiens (human)	IC50	0.1100	1	1
sn 38	Homo sapiens (human)	IC50	3.2500	2	2
7-ethyl-7-hydroxy-10h-1,3-dioxolo(4,5-g)pyrano(3',4':6,7)indolizino(1,2-b)quinoline-8,11(7h,12h)-dione	Homo sapiens (human)	IC50	0.0525	2	2
ginsenoside re	Homo sapiens (human)	IC50	250.0000	1	1
Chebulagic acid	Homo sapiens (human)	IC50	0.0750	2	2
oleic acid	Homo sapiens (human)	IC50	31.0000	1	1
ganoderiol f	Homo sapiens (human)	IC50	106.0000	1	1
beta, beta-dimethylacrylshikonin, (+)-isomer	Homo sapiens (human)	IC50	77.0000	1	1
shikonin	Homo sapiens (human)	IC50	208.0000	1	1
elaidic acid	Homo sapiens (human)	IC50	1,000.0000	1	1
ungeremine	Homo sapiens (human)	IC50	6.1000	1	1
ginsenoside rb1	Homo sapiens (human)	IC50	250.0000	1	1
ginsenoside f2	Homo sapiens (human)	IC50	250.0000	1	1
ginsenoside rg3	Homo sapiens (human)	IC50	250.0000	1	1
ginsenoside rd	Homo sapiens (human)	IC50	250.0000	1	1
ginsenoside rb3	Homo sapiens (human)	IC50	250.0000	1	1
nsc 100880	Homo sapiens (human)	IC50	12.0000	1	1
gypenoside XVII	Homo sapiens (human)	IC50	250.0000	1	1
(20R)-ginsenoside Rg3	Homo sapiens (human)	IC50	250.0000	1	1
nsc 158393	Homo sapiens (human)	IC50	10.0000	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
camptothecin	Homo sapiens (human)	EC50	0.3500	1	1
topotecan	Homo sapiens (human)	EC50	0.0626	2	2
topotecan	Homo sapiens (human)	Kd	0.0265	1	1
10,11-methylenedioxy-20-camptothecin	Homo sapiens (human)	EC50	0.0500	1	1
sn 38	Homo sapiens (human)	EC50	0.1950	1	2
edotecarin	Homo sapiens (human)	EC50	0.0673	3	3
tetracarboxyphenylporphine	Homo sapiens (human)	EC50	1.2890	2	2
tetraphenylporphine	Homo sapiens (human)	EC50	50.0000	2	2
5,10,15,20-tetra(4-pyridyl)porphyrin	Homo sapiens (human)	EC50	50.0000	2	2

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
juglone	Homo sapiens (human)	MIC	5.0000	1	1
1,4-naphthoquinone	Homo sapiens (human)	MIC	500.0000	1	1
naphthazarin	Homo sapiens (human)	MIC	50.0000	1	1
plumbagin	Homo sapiens (human)	MIC	50.0000	1	1
oleanolic acid	Homo sapiens (human)	Activity	265.0000	1	1
camptothecin	Homo sapiens (human)	CC50	0.8100	2	2
camptothecin	Homo sapiens (human)	IC10	0.0002	1	1
camptothecin	Homo sapiens (human)	Inhibition	100.0000	1	1
camptothecin	Homo sapiens (human)	MIC	0.0100	1	1
etoposide	Homo sapiens (human)	MIC	100.0000	1	1
amonafide	Homo sapiens (human)	UC50	8.0000	1	1
topotecan	Homo sapiens (human)	CC50	3.2000	1	1
irinotecan	Homo sapiens (human)	CC50	100.0000	1	1
9-aminocamptothecin	Homo sapiens (human)	CC50	0.9000	1	1
alkannin	Homo sapiens (human)	MIC	500.0000	1	1
rebeccamycin	Homo sapiens (human)	MIC	1.7500	4	4
10-hydroxycamptothecin	Homo sapiens (human)	CC50	1.0000	1	1
sn 38	Homo sapiens (human)	CC50	0.8000	1	1
nsc 314622	Homo sapiens (human)	Concentration	100.0000	1	1
shikonin	Homo sapiens (human)	MIC	50.0000	1	1
arc111	Homo sapiens (human)	IC10	0.0003	1	1
arc 31	Homo sapiens (human)	IC10	0.0003	1	1
genz-644282	Homo sapiens (human)	Activity	0.1000	1	1
nsc 100880	Homo sapiens (human)	CC50	0.9000	1	1

Enables

This protein enables 13 target(s):

Target	Category	Definition
RNA polymerase II cis-regulatory region sequence-specific DNA binding	molecular function	Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018]
DNA binding	molecular function	Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw]
chromatin binding	molecular function	Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130]
double-stranded DNA binding	molecular function	Binding to double-stranded DNA. [GOC:elh, GOC:vw]
single-stranded DNA binding	molecular function	Binding to single-stranded DNA. [GOC:elh, GOC:vw, PMID:22976174]
RNA binding	molecular function	Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah]
DNA topoisomerase type I (single strand cut, ATP-independent) activity	molecular function	Catalysis of a DNA topological transformation by transiently cleaving one DNA strand at a time to allow passage of another strand; changes the linking number by +1 per catalytic cycle. [PMID:8811192]
protein serine/threonine kinase activity	molecular function	Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
ATP binding	molecular function	Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
DNA binding, bending	molecular function	The activity of binding selectively and non-covalently to and distorting the original structure of DNA, typically a straight helix, into a bend, or increasing the bend if the original structure was intrinsically bent due to its sequence. [GOC:krc, GOC:vw, PMID:10710711, PMID:19037758]
protein domain specific binding	molecular function	Binding to a specific domain of a protein. [GOC:go_curators]
supercoiled DNA binding	molecular function	Binding to supercoiled DNA. For example, during replication and transcription, template DNA is negatively supercoiled in the receding downstream DNA and positively supercoiled in the approaching downstream DNA. [GOC:pr, GOC:rph, PMID:20723754, PMID:21345933, Wikipedia:DNA_supercoil]

Located In

This protein is located in 7 target(s):

Target	Category	Definition
P-body	cellular component	A focus in the cytoplasm where mRNAs may become inactivated by decapping or some other mechanism. Protein and RNA localized to these foci are involved in mRNA degradation, nonsense-mediated mRNA decay (NMD), translational repression, and RNA-mediated gene silencing. [GOC:clt, PMID:12730603]
fibrillar center	cellular component	A structure found most metazoan nucleoli, but not usually found in lower eukaryotes; surrounded by the dense fibrillar component; the zone of transcription from multiple copies of the pre-rRNA genes is in the border region between these two structures. [PMID:10754561]
male germ cell nucleus	cellular component	The nucleus of a male germ cell, a reproductive cell in males. [CL:0000015, GOC:hjd, GOC:mtg_sensu]
nucleus	cellular component	A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
nucleoplasm	cellular component	That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
nucleolus	cellular component	A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732]
perikaryon	cellular component	The portion of the cell soma (neuronal cell body) that excludes the nucleus. [GOC:jl]

Active In

This protein is active in 1 target(s):

Target	Category	Definition
nucleolus	cellular component	A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732]

Part Of

This protein is part of 1 target(s):

Target	Category	Definition
protein-DNA complex	cellular component	A macromolecular complex containing both protein and DNA molecules. [GOC:mah]

Involved In

This protein is involved in 11 target(s):

Target	Category	Definition
DNA topological change	biological process	The process in which a transformation is induced in the topological structure of a double-stranded DNA helix, resulting in a change in linking number. [ISBN:071673706X, ISBN:0935702490]
chromatin remodeling	biological process	A dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820]
circadian rhythm	biological process	Any biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:bf, GOC:go_curators]
response to xenobiotic stimulus	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc]
programmed cell death	biological process	A process which begins when a cell receives an internal or external signal and activates a series of biochemical events (signaling pathway). The process ends with the death of the cell. [GOC:lr, GOC:mtg_apoptosis]
phosphorylation	biological process	The process of introducing a phosphate group into a molecule, usually with the formation of a phosphoric ester, a phosphoric anhydride or a phosphoric amide. [ISBN:0198506732]
peptidyl-serine phosphorylation	biological process	The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037]
circadian regulation of gene expression	biological process	Any process that modulates the frequency, rate or extent of gene expression such that an expression pattern recurs with a regularity of approximately 24 hours. [GOC:mah]
embryonic cleavage	biological process	The first few specialized divisions of an activated animal egg. [GOC:clt, ISBN:0070524300]
chromosome segregation	biological process	The process in which genetic material, in the form of chromosomes, is organized into specific structures and then physically separated and apportioned to two or more sets. In eukaryotes, chromosome segregation begins with the condensation of chromosomes, includes chromosome separation, and ends when chromosomes have completed movement to the spindle poles. [GOC:jl, GOC:mah, GOC:mtg_cell_cycle, GOC:vw]
DNA replication	biological process	The cellular metabolic process in which a cell duplicates one or more molecules of DNA. DNA replication begins when specific sequences, known as origins of replication, are recognized and bound by the origin recognition complex, and ends when the original DNA molecule has been completely duplicated and the copies topologically separated. The unit of replication usually corresponds to the genome of the cell, an organelle, or a virus. The template for replication can either be an existing DNA molecule or RNA. [GOC:mah]