Page last updated: 2024-10-15

9-beta-d-arabinofuranosylguanosine 5'-triphosphate

Cross-References

ID SourceID
PubMed CID135544356
CHEMBL ID1201369
SCHEMBL ID5809658
MeSH IDM0077965

Synonyms (12)

Synonym
72490-81-4
CHEMBL1201369
9beta-d-arabinofuranosylguanosine 5'-triphosphate
unii-q5en532ne7
9-beta-d-arabinofuranosylguanosine 5'-triphosphate
ara-gtp
6h-purin-6-one, 2-amino-1,9-dihydro-9-(5-o-(hydroxy((hydroxy(phosphonooxy)phosphinyl)oxy)phosphinyl)-beta-d-arabinofuranosyl)-
q5en532ne7 ,
SCHEMBL5809658
9-.beta.-d-arabinofuranosylguanosine 5'-triphosphate
6h-purin-6-one, 2-amino-1,9-dihydro-9-(5-o-(hydroxy((hydroxy(phosphonooxy)phosphinyl)oxy)phosphinyl)-.beta.-d-arabinofuranosyl)-
2-amino-1,9-dihydro-9-(5-o-(hydroxy((hydroxy(phosphonooxy)phosphinyl)oxy)phosphinyl)-.beta.-d-arabinofuranosyl)-6h-purin-6-one

Pharmacokinetics

ExcerptReference
" Parallel plasma and cellular pharmacokinetic studies were conducted."( Compound GW506U78 in refractory hematologic malignancies: relationship between cellular pharmacokinetics and clinical response.
Ayres, M; Du, M; Gandhi, V; Keating, MJ; Kisor, DF; Kurtzberg, J; Mitchell, BS; Nowak, BJ; Plunkett, W; Rodriguez, CO, 1998
)
" Plasma and cellular pharmacokinetic measurements were conducted during the first 5 days."( Evaluation of the combination of nelarabine and fludarabine in leukemias: clinical response, pharmacokinetics, and pharmacodynamics in leukemia cells.
Ayres, M; Du, M; Gandhi, V; Hodge, JP; Keating, MJ; O'Brien, S; Plunkett, W; Ramakrishna, P; Rodriguez, CO; Rosner, GL; Weller, S, 2001
)

Dosage Studied

ExcerptReference
" Hence, dosing regimens that achieve high plasma levels of ara-G during therapy may increase cellular levels of ara-GTP."( Pharmacological and biochemical strategies to increase the accumulation of arabinofuranosylguanine triphosphatein primary human leukemia cells.
Estey, E; Gandhi, V; Keating, MJ; Legha, JK; Rodriguez, CO, 1997
)
" Investigation of other dosing schedules may limit neurotoxicity."( Complete hematologic and cytogenetic response to 2-amino-9-beta-D-arabinosyl-6-methoxy-9H-guanine in a patient with chronic myelogenous leukemia in T-cell blastic phase: a case report and review of the literature.
Aguayo, A; Beran, M; Cortes, JE; Gandhi, V; Kantarjian, HM; Keating, MJ; Kurtzberg, J; Plunkett, W, 1999
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID523071Ratio of Kcat to Km for Aminoglycoside 2'-phosphotransferase 2a N196D/D268N mutant using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID613863Activation of Escherichia coli CTPS assessed as Gln-dependent CTP formation at < 0.15 mM by continuous spectrophotometric assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Activation and inhibition of CTP synthase from Trypanosoma brucei, the causative agent of African sleeping sickness.
AID523069Activity of Aminoglycoside 2'-phosphotransferase 2a R92H/D268N mutant using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID523072Ratio of Kcat to Km for Aminoglycoside 2'-phosphotransferase 2a R92H/D268N mutant using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID613867Inhibition of N-terminal His6-tagged Trypanosoma brucei CTPS assessed as NH3-dependent CTP formation by continuous spectrophotometric assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Activation and inhibition of CTP synthase from Trypanosoma brucei, the causative agent of African sleeping sickness.
AID613868Activation of N-terminal His6-tagged Trypanosoma brucei CTPS assessed as Gln-dependent CTP formation at <0.2 mM by continuous spectrophotometric assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Activation and inhibition of CTP synthase from Trypanosoma brucei, the causative agent of African sleeping sickness.
AID523067Activity of Aminoglycoside 2'-phosphotransferase 2a using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID613864Inhibition of Escherichia coli CTPS assessed as Gln-dependent CTP formation at > 0.15 mM by continuous spectrophotometric assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Activation and inhibition of CTP synthase from Trypanosoma brucei, the causative agent of African sleeping sickness.
AID1137666Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes at 100 uM after 60 mins by liquid scintillation counting2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.
AID706074Binding affinity to Staphylococcus aureus FtsZ expressed in Escherichia coli BL21 (DE3) by fluorescence anisotropy BoGTPgammaS competition assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
A bactericidal guanidinomethyl biaryl that alters the dynamics of bacterial FtsZ polymerization.
AID613865Activation of N-terminal His6-tagged Trypanosoma brucei CTPS assessed as Gln-dependent CTP formation by continuous spectrophotometric assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Activation and inhibition of CTP synthase from Trypanosoma brucei, the causative agent of African sleeping sickness.
AID1124515Effect on thymidine kinase in BHK21 (C13) cells using [14C]thymidine at 5 mM after 10 mins by liquid scintillation spectrometer analysis relative to control in presence of Mg2+1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Design of species- or isozyme-specific enzyme inhibitors. 1. Effect of thymidine substituents on affinity for the thymidine site of hamster cytoplasmic thymidine kinase.
AID706073Binding affinity to Escherichia coli FtsZ by fluorescence anisotropy BoGTPgammaS competition assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
A bactericidal guanidinomethyl biaryl that alters the dynamics of bacterial FtsZ polymerization.
AID613866Inhibition of N-terminal His6-tagged Trypanosoma brucei CTPS assessed as Gln-dependent CTP formation at by continuous spectrophotometric assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Activation and inhibition of CTP synthase from Trypanosoma brucei, the causative agent of African sleeping sickness.
AID706072Binding affinity to Enterococcus faecalis FtsZ by fluorescence anisotropy BoGTPgammaS competition assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
A bactericidal guanidinomethyl biaryl that alters the dynamics of bacterial FtsZ polymerization.
AID523068Activity of Aminoglycoside 2'-phosphotransferase 2a N196D/D268N mutant using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID1124518Effect on human mitochondrial thymidine kinase using [14C]thymidine at 5 mM after 10 mins by liquid scintillation spectrometer analysis relative to control in presence of Mg2+1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Design of species- or isozyme-specific enzyme inhibitors. 1. Effect of thymidine substituents on affinity for the thymidine site of hamster cytoplasmic thymidine kinase.
AID1124517Effect on human cytoplasmic thymidine kinase using [14C]thymidine at 5 mM after 10 mins by liquid scintillation spectrometer analysis relative to control in presence of Mg2+1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Design of species- or isozyme-specific enzyme inhibitors. 1. Effect of thymidine substituents on affinity for the thymidine site of hamster cytoplasmic thymidine kinase.
AID523070Ratio of Kcat to Km for Aminoglycoside 2'-phosphotransferase 2a using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID613869Inhibition of N-terminal His6-tagged Trypanosoma brucei CTPS assessed as Gln-dependent CTP formation at > 0.2 mM by continuous spectrophotometric assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Activation and inhibition of CTP synthase from Trypanosoma brucei, the causative agent of African sleeping sickness.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (26)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (26.92)18.7374
1990's7 (26.92)18.2507
2000's4 (15.38)29.6817
2010's8 (30.77)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (15.38%)5.53%
Reviews1 (3.85%)6.00%
Case Studies1 (3.85%)4.05%
Observational0 (0.00%)0.25%
Other20 (76.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]