Page last updated: 2024-11-08

Telomestatin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

telomestatin: isolated from Spreptomyces anulatus; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID443590
CHEBI ID29689
SCHEMBL ID10025441
PubMed CID11954679
SCHEMBL ID61649
MeSH IDM0394772

Synonyms (15)

Synonym
chebi:29689 ,
SCHEMBL10025441
telomestatin (tms)
bdbm213233
gm95
4,8-dimethyl-3,7,11,15,19,23,27-heptaoxa-31-thia-33,34,35,36,37,38,39,40-octazanonacyclo[28.2.1.12,5.16,9.110,13.114,17.118,21.122,25.126,29]tetraconta-2(40),4,6(39),8,10(38),12,14(37),16,18(36),20,22(35),24,26(34),28,30(33)-pentadecaene
telomestatin
265114-54-3
SCHEMBL61649
DTXSID50474656
Q4391972
(1r)-4,8-dimethyl-3,7,11,15,19,23,27-heptaoxa-31-thia-33,34,35,36,37,38,39,40-octaazanonacyclo[28.2.1.12,5.16,9.110,13.114,17.118,21.122,25.126,29]tetraconta-2(40),4,6(39),8,10(38),12,14 (37),16,18(36),20,22(35),24,26(34),28,30(33)-pentadecaene
HY-15225
CS-0003820
AKOS040749628

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Sublethal dosage of NSC 19630 and the chemotherapy drug topotecan acted synergistically to inhibit cell proliferation and induce DNA damage."( Inhibition of helicase activity by a small molecule impairs Werner syndrome helicase (WRN) function in the cellular response to DNA damage or replication stress.
Aggarwal, M; Brosh, RM; Shoemaker, RH; Sommers, JA, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
1,3-oxazoles
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Telomerase reverse transcriptaseHomo sapiens (human)IC50 (µMol)0.35170.00062.69489.4000AID329708; AID329709; AID329710; AID329711; AID329712; AID587556
ATP-dependent DNA helicase DinGEscherichia coli K-12IC50 (µMol)0.00170.00100.00170.0022AID1802400
Fanconi anemia group J proteinHomo sapiens (human)IC50 (µMol)0.00170.00100.00170.0022AID1802400
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (53)

Processvia Protein(s)Taxonomy
telomere maintenanceTelomerase reverse transcriptaseHomo sapiens (human)
RNA-templated transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
RNA-templated DNA biosynthetic processTelomerase reverse transcriptaseHomo sapiens (human)
telomere maintenance via telomeraseTelomerase reverse transcriptaseHomo sapiens (human)
mitochondrion organizationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of gene expressionTelomerase reverse transcriptaseHomo sapiens (human)
DNA strand elongationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of Wnt signaling pathwayTelomerase reverse transcriptaseHomo sapiens (human)
siRNA processingTelomerase reverse transcriptaseHomo sapiens (human)
regulation of protein stabilityTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of hair cycleTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of neuron apoptotic processTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of angiogenesisTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of glucose importTelomerase reverse transcriptaseHomo sapiens (human)
response to cadmium ionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of nitric-oxide synthase activityTelomerase reverse transcriptaseHomo sapiens (human)
establishment of protein localization to telomereTelomerase reverse transcriptaseHomo sapiens (human)
cellular response to hypoxiaTelomerase reverse transcriptaseHomo sapiens (human)
DNA biosynthetic processTelomerase reverse transcriptaseHomo sapiens (human)
replicative senescenceTelomerase reverse transcriptaseHomo sapiens (human)
siRNA transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of miRNA transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of transdifferentiationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of protein localization to nucleolusTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell migrationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of endothelial cell apoptotic processTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of stem cell proliferationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of cellular senescenceTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandTelomerase reverse transcriptaseHomo sapiens (human)
DNA repairATP-dependent DNA helicase DinGEscherichia coli K-12
SOS responseATP-dependent DNA helicase DinGEscherichia coli K-12
DNA duplex unwindingATP-dependent DNA helicase DinGEscherichia coli K-12
nucleobase-containing compound metabolic processATP-dependent DNA helicase DinGEscherichia coli K-12
G-quadruplex DNA unwindingATP-dependent DNA helicase DinGEscherichia coli K-12
DNA duplex unwindingATP-dependent DNA helicase DinGEscherichia coli K-12
DNA repairATP-dependent DNA helicase DinGEscherichia coli K-12
SOS responseATP-dependent DNA helicase DinGEscherichia coli K-12
regulation of transcription by RNA polymerase IIFanconi anemia group J proteinHomo sapiens (human)
DNA damage checkpoint signalingFanconi anemia group J proteinHomo sapiens (human)
DNA repairFanconi anemia group J proteinHomo sapiens (human)
double-strand break repairFanconi anemia group J proteinHomo sapiens (human)
spermatogonial cell divisionFanconi anemia group J proteinHomo sapiens (human)
spermatid developmentFanconi anemia group J proteinHomo sapiens (human)
negative regulation of cell population proliferationFanconi anemia group J proteinHomo sapiens (human)
response to toxic substanceFanconi anemia group J proteinHomo sapiens (human)
negative regulation of gene expressionFanconi anemia group J proteinHomo sapiens (human)
meiotic DNA double-strand break processing involved in reciprocal meiotic recombinationFanconi anemia group J proteinHomo sapiens (human)
DNA duplex unwindingFanconi anemia group J proteinHomo sapiens (human)
homologous recombinationFanconi anemia group J proteinHomo sapiens (human)
chiasma assemblyFanconi anemia group J proteinHomo sapiens (human)
cellular response to vitaminFanconi anemia group J proteinHomo sapiens (human)
cellular response to hypoxiaFanconi anemia group J proteinHomo sapiens (human)
seminiferous tubule developmentFanconi anemia group J proteinHomo sapiens (human)
protein-DNA covalent cross-linking repairFanconi anemia group J proteinHomo sapiens (human)
cellular response to angiotensinFanconi anemia group J proteinHomo sapiens (human)
nucleotide-excision repairFanconi anemia group J proteinHomo sapiens (human)
double-strand break repair involved in meiotic recombinationFanconi anemia group J proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
tRNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
transcription coactivator bindingTelomerase reverse transcriptaseHomo sapiens (human)
DNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
telomerase activityTelomerase reverse transcriptaseHomo sapiens (human)
telomerase RNA reverse transcriptase activityTelomerase reverse transcriptaseHomo sapiens (human)
RNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
RNA-directed DNA polymerase activityTelomerase reverse transcriptaseHomo sapiens (human)
RNA-dependent RNA polymerase activityTelomerase reverse transcriptaseHomo sapiens (human)
protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
identical protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
protein homodimerization activityTelomerase reverse transcriptaseHomo sapiens (human)
metal ion bindingTelomerase reverse transcriptaseHomo sapiens (human)
protein-folding chaperone bindingTelomerase reverse transcriptaseHomo sapiens (human)
telomerase RNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
template-free RNA nucleotidyltransferaseTelomerase reverse transcriptaseHomo sapiens (human)
telomeric DNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
DNA bindingATP-dependent DNA helicase DinGEscherichia coli K-12
DNA helicase activityATP-dependent DNA helicase DinGEscherichia coli K-12
helicase activityATP-dependent DNA helicase DinGEscherichia coli K-12
protein bindingATP-dependent DNA helicase DinGEscherichia coli K-12
ATP bindingATP-dependent DNA helicase DinGEscherichia coli K-12
hydrolase activityATP-dependent DNA helicase DinGEscherichia coli K-12
hydrolase activity, acting on acid anhydrides, in phosphorus-containing anhydridesATP-dependent DNA helicase DinGEscherichia coli K-12
isomerase activityATP-dependent DNA helicase DinGEscherichia coli K-12
ATP hydrolysis activityATP-dependent DNA helicase DinGEscherichia coli K-12
DNA/RNA helicase activityATP-dependent DNA helicase DinGEscherichia coli K-12
5'-3' DNA helicase activityATP-dependent DNA helicase DinGEscherichia coli K-12
metal ion bindingATP-dependent DNA helicase DinGEscherichia coli K-12
4 iron, 4 sulfur cluster bindingATP-dependent DNA helicase DinGEscherichia coli K-12
DNA bindingFanconi anemia group J proteinHomo sapiens (human)
DNA helicase activityFanconi anemia group J proteinHomo sapiens (human)
chromatin bindingFanconi anemia group J proteinHomo sapiens (human)
RNA helicase activityFanconi anemia group J proteinHomo sapiens (human)
protein bindingFanconi anemia group J proteinHomo sapiens (human)
ATP bindingFanconi anemia group J proteinHomo sapiens (human)
ATP hydrolysis activityFanconi anemia group J proteinHomo sapiens (human)
5'-3' DNA helicase activityFanconi anemia group J proteinHomo sapiens (human)
metal ion bindingFanconi anemia group J proteinHomo sapiens (human)
4 iron, 4 sulfur cluster bindingFanconi anemia group J proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

Processvia Protein(s)Taxonomy
PML bodyTelomerase reverse transcriptaseHomo sapiens (human)
chromosome, telomeric regionTelomerase reverse transcriptaseHomo sapiens (human)
nucleusTelomerase reverse transcriptaseHomo sapiens (human)
nucleoplasmTelomerase reverse transcriptaseHomo sapiens (human)
telomerase holoenzyme complexTelomerase reverse transcriptaseHomo sapiens (human)
nucleolusTelomerase reverse transcriptaseHomo sapiens (human)
cytosolTelomerase reverse transcriptaseHomo sapiens (human)
plasma membraneTelomerase reverse transcriptaseHomo sapiens (human)
nuclear speckTelomerase reverse transcriptaseHomo sapiens (human)
mitochondrial nucleoidTelomerase reverse transcriptaseHomo sapiens (human)
TERT-RMRP complexTelomerase reverse transcriptaseHomo sapiens (human)
telomerase catalytic core complexTelomerase reverse transcriptaseHomo sapiens (human)
nuclear telomere cap complexTelomerase reverse transcriptaseHomo sapiens (human)
RNA-directed RNA polymerase complexTelomerase reverse transcriptaseHomo sapiens (human)
replication forkFanconi anemia group J proteinHomo sapiens (human)
nucleusFanconi anemia group J proteinHomo sapiens (human)
nucleoplasmFanconi anemia group J proteinHomo sapiens (human)
cytoplasmFanconi anemia group J proteinHomo sapiens (human)
nuclear membraneFanconi anemia group J proteinHomo sapiens (human)
BRCA1-B complexFanconi anemia group J proteinHomo sapiens (human)
nucleusFanconi anemia group J proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID329714Inhibition of human telomerase elongation activity expressed in HEK293T cells in presence of primer Telo4R by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID329709Inhibition of human telomerase expressed in HEK293T cells treated after telomerase elongation by telomeric repeat amplification protocol assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID329708Inhibition of human telomerase expressed in HEK293T cells treated before telomerase elongation by telomeric repeat amplification protocol assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID375566Binding affinity to G-quadruplex F21T DNA assessed as change in melting temperature at 0.6 uM under K+ ionic conditions by FRET assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers.
AID375567Binding affinity to G-quadruplex F21T DNA assessed as change in melting temperature at 0.8 uM under K+ ionic conditions by FRET assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers.
AID329710Inhibition of human telomerase expressed in HEK293T cells in presence of primer (T2AG3)3 by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID587556Inhibition of human Telomerase activity in cell free system by TRAP assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
N-cyclic bay-substituted perylene G-quadruplex ligands have selective antiproliferative effects on cancer cells and induce telomere damage.
AID329711Inhibition of human telomerase expressed in HEK293T cells in presence of primer TS by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID329712Inhibition of human telomerase expressed in in HEK293T cells in presence of primer (T2AG3)4 by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID1180157Growth inhibition of human U2OS cells after 3 days in presence of werner syndrome helicase inhibitor NSC 196302014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
DNA binders in clinical trials and chemotherapy.
AID329713Decrease in telomerase processivity assessed as decrease in telomerase elongation in presence of Telo3R primer by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID1802400Helicase Assays from Article 10.1074/jbc.M113.496463: \\Specialization among iron-sulfur cluster helicases to resolve G-quadruplex DNA structures that threaten genomic stability.\\2013The Journal of biological chemistry, Sep-27, Volume: 288, Issue:39
Specialization among iron-sulfur cluster helicases to resolve G-quadruplex DNA structures that threaten genomic stability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (69)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's38 (55.07)29.6817
2010's29 (42.03)24.3611
2020's2 (2.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.06

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index33.06 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index37.30 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (33.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Reviews8 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
Other56 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]