DGIdb - THIOGUANINE Drug Record

THIOGUANINE chembl:CHEMBL727 ApprovedAntineoplasticImmunotherapy

Alternate Names:

LANVIS
TIOGUANINE HEMIHYDRATE
TABLOID
NSC-76504
THIOGUANINE
TIOGUANINE
NSC-752
TG
2-AMINO-1,7-DIHYDRO-6H-PURINE-6-THIONE
2-AMINO-6-MERCAPTOPURINE
6-TG
2-AMINOPURINE-6-THIOL
2-AMINOPURINE-6(1H)-THIONE
THG
2-AMINOPURIN-6-THIOL
6-MERCAPTOGUANINE
THIOGUANINE ANHYDROUS
2-AMINO-6-PURINETHIOL
6-MERCAPTO-2-AMINOPURINE
2-AMINO-1,9-DIHYDROPURINE-6-THIONE
TIOGUANIN
2-AMINO 6MP
chemidplus:154-42-7
chembl:CHEMBL727
rxcui:1546005
pubchem.compound:2723601
drugbank:00352

Drug Info:

Drug Categories	thiopurine analogs
Drug Categories	immunosuppressive agents
Drug Categories	heterocyclic compounds, fused-ring

(9 More Sources)

Publications:

Ciesielski-Treska et al., 1975, Morphological, histochemical and chromosomal patterns of neuroblastoma parental and purine resistant lines., Neurobiology
Meyer JA et al., 2013, Relapse-specific mutations in NT5C2 in childhood acute lymphoblastic leukemia., Nat Genet
Tzoneva et al., 2013, Activating mutations in the NT5C2 nucleotidase gene drive chemotherapy resistance in relapsed ALL., Nat. Med.
Li B et al., 2015, Negative feedback-defective PRPS1 mutants drive thiopurine resistance in relapsed childhood ALL., Nat Med
Perez-Andreu V et al., 2013, Inherited GATA3 variants are associated with Ph-like childhood acute lymphoblastic leukemia and risk of relapse., Nat Genet
French et al., 1991, Queuine, a tRNA anticodon wobble base, maintains the proliferative and pluripotent potential of HL-60 cells in the presence of the differentiating agent 6-thioguanine., Proc. Natl. Acad. Sci. U.S.A.
Valerie NC et al., 2016, NUDT15 Hydrolyzes 6-Thio-DeoxyGTP to Mediate the Anticancer Efficacy of 6-Thioguanine., Cancer Res
Moriyama T et al., 2016, NUDT15 polymorphisms alter thiopurine metabolism and hematopoietic toxicity., Nat Genet
Mirzayans et al., 1992, Cytotoxic and mutagenic effects of methylnitrosourea in two human fetal fibroblast strains differing in O6-methylguanine-DNA methyltransferase activity., Carcinogenesis
Karol SE et al., 2016, Genetic risk factors for the development of osteonecrosis in children under age 10 treated for acute lymphoblastic leukemia., Blood
Cheng et al., 2005, Karyotypic abnormalities create discordance of germline genotype and cancer cell phenotypes., Nat. Genet.
Bai et al., 2004, Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione., Int. J. Biochem. Cell Biol.
Volonté et al., 1993, A purine analog-sensitive protein kinase activity associates with Trk nerve growth factor receptors., J. Neurochem.
Saxena et al., 1980, New imidazolylthiocarbamides as guanine deaminase inhibitors., Pharmazie

THIOGUANINE NUDT15

Interaction Score: 3.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27530327 26878724

Sources:
FDA PharmGKB CIViC
THIOGUANINE GDA

Interaction Score: 1.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7384171

Sources:
NCI
THIOGUANINE PRPS1

Interaction Score: 1.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25962120

Sources:
CIViC
THIOGUANINE NT5C2

Interaction Score: 0.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23377183 23377281

Sources:
CIViC
THIOGUANINE GGH

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16041371

Sources:
NCI
THIOGUANINE TPM3

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7687657

Sources:
NCI
THIOGUANINE DOK5

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26590194

Sources:
PharmGKB
THIOGUANINE LINC00251

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26590194

Sources:
PharmGKB
THIOGUANINE BMP7

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26590194

Sources:
PharmGKB
THIOGUANINE TPMT

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Guanine analog

Alteration TPMT:.

Alteration TPMT:A80P,Y240C,A154T,A167G

PMIDs:
None found

Sources:
FDA CGI
THIOGUANINE IMPDH1

Interaction Score: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
THIOGUANINE IMPDH2

Interaction Score: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
THIOGUANINE GATA3

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24141364

Sources:
PharmGKB
THIOGUANINE MGMT

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1638685

Sources:
NCI
THIOGUANINE ABCC4

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14643890

Sources:
NCI
THIOGUANINE MYC

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1988936

Sources:
NCI
THIOGUANINE ACHE

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1207869

Sources:
NCI
THIOGUANINE HBB

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIOGUANINE NAT1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
THIOGUANINE PAX8

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIOGUANINE HPGD

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIOGUANINE IDH1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIOGUANINE KDM4A

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIOGUANINE NFE2L2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIOGUANINE EHMT2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIOGUANINE AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB00352

Version: 5.1.7

Alternate Names:

TIOGUANINE DrugBank Drug Name

154-42-7 CAS Number

Lanvis Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories antimetabolites

Publications:

Schwartz et al., 1983, Induction of leukemia cell differentiation by chemotherapeutic agents., Adv. Enzyme Regul.

Coulthard et al., 2005, The thiopurines: an update., Invest New Drugs

Riscoe et al., 1989, Purine metabolism as a target for leukemia chemotherapy., Blood Rev.

NCI: THIOGUANINE

Version: 14-September-2017

Alternate Names:

C876 NCI drug code

Drug Info:

Publications:

Saxena et al., 1980, New imidazolylthiocarbamides as guanine deaminase inhibitors., Pharmazie

Cheng et al., 2005, Karyotypic abnormalities create discordance of germline genotype and cancer cell phenotypes., Nat. Genet.

NCI: 6-TG

Version: 14-September-2017

Alternate Names:

C876 NCI drug code

Drug Info:

Publications:

French et al., 1991, Queuine, a tRNA anticodon wobble base, maintains the proliferative and pluripotent potential of HL-60 cells in the presence of the differentiating agent 6-thioguanine., Proc. Natl. Acad. Sci. U.S.A.

NCI: 6-THIOGUANINE

Version: 14-September-2017

Alternate Names:

C876 NCI drug code

Drug Info:

Publications:

Ciesielski-Treska et al., 1975, Morphological, histochemical and chromosomal patterns of neuroblastoma parental and purine resistant lines., Neurobiology

Mirzayans et al., 1992, Cytotoxic and mutagenic effects of methylnitrosourea in two human fetal fibroblast strains differing in O6-methylguanine-DNA methyltransferase activity., Carcinogenesis

Bai et al., 2004, Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione., Int. J. Biochem. Cell Biol.

PharmGKB: thioguanine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Perez-Andreu V et al., 2013, Inherited GATA3 variants are associated with Ph-like childhood acute lymphoblastic leukemia and risk of relapse., Nat Genet

Karol SE et al., 2016, Genetic risk factors for the development of osteonecrosis in children under age 10 treated for acute lymphoblastic leukemia., Blood

Valerie NC et al., 2016, NUDT15 Hydrolyzes 6-Thio-DeoxyGTP to Mediate the Anticancer Efficacy of 6-Thioguanine., Cancer Res

CIViC: THIOGUANINE

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Meyer JA et al., 2013, Relapse-specific mutations in NT5C2 in childhood acute lymphoblastic leukemia., Nat Genet

Tzoneva et al., 2013, Activating mutations in the NT5C2 nucleotidase gene drive chemotherapy resistance in relapsed ALL., Nat. Med.

Moriyama T et al., 2016, NUDT15 polymorphisms alter thiopurine metabolism and hematopoietic toxicity., Nat Genet

TTD: Thioguanine
- Version: 2020.06.01
Alternate Names:

D02ZXM TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103451
- Version: 29-September-2020
Alternate Names:

THIOGUANINE GuideToPharmacology Ligand Name

Drug Info:

Publications:
DTC: THIOGUANINE
- Version: 02-September-2020
Alternate Names:

CHEMBL727 ChEMBL Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL727
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
CGI: Thioguanine
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL727
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
FDA: Thioguanine
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Drug family	Guanine analog
Alteration	TPMT:.
Alteration	TPMT:A80P,Y240C,A154T,A167G

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	True

Mechanism of Interaction	Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor
Direct Interaction	yes
Specific Action of the Ligand	Inhibition

TIOGUANINE	DrugBank Drug Name
154-42-7	CAS Number
Lanvis	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	antimetabolites

THIOGUANINE Drug Record

THIOGUANINE chembl:CHEMBL727 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27530327 26878724

Sources: FDA PharmGKB CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7384171

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25962120

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23377183 23377281

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16041371

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7687657

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26590194

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26590194

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26590194

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Drug family Guanine analog Alteration TPMT:. Alteration TPMT:A80P,Y240C,A154T,A167G

PMIDs: None found

Sources: FDA CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24141364

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 1638685

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14643890

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 1988936

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 1207869

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

n/a

PMIDs:
27530327 26878724

Sources:
FDA PharmGKB CIViC

Interaction Types & Directionality:

n/a

PMIDs:
7384171

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
25962120

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
23377183 23377281

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
16041371

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
7687657

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
26590194

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26590194

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26590194

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Guanine analog

Alteration TPMT:.

Alteration TPMT:A80P,Y240C,A154T,A167G

PMIDs:
None found

Sources:
FDA CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
24141364

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
1638685

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
14643890

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
1988936

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
1207869

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found