DGIdb - DHFR Gene Record

DHFR 1719 Druggable Genome

Alternate Names:

1719
DIHYDROFOLATE REDUCTASE
DHFR
DHFRP1
DYR
126060
2861
ENSG00000228716
OTTHUMG00000162529
P00374
DYR_HUMAN
ENSG00000188985
DIHYDROFOLATE REDUCTASE (EC 1.5.1.3). [SOURCE:UNIPROT/SWISSPROT;ACC:P00374]
ENSG00000168129
PA143
T17345

Gene Info:

Uniprot Evidence	1: Evidence at protein level
Interpro Short Name	DHFR_dom
Human Readable Name	DRUGGABLE GENOME
Interpro Type	Domain
Interpro Acc	IPR001796
Interpro Name	Dihydrofolate reductase domain
Uniprot Status	Swiss-Prot
Target Subclass	1.5.1.3
Target Main Class	Enzymes
Target Class	Enzymes
Target Subclass	EC:1.5.1.3
Gene Biotype	PROTEIN_CODING

(10 More Sources)

Gene Categories: Category Details

DRUGGABLE GENOME
ENZYME

Publications:

Shimanovsky et al., 2013, Pralatrexate : evaluation of clinical efficacy and toxicity in T-cell lymphoma., Expert Opin Pharmacother
Fidock et al., 1997, Transformation with human dihydrofolate reductase renders malaria parasites insensitive to WR99210 but does not affect the intrinsic activity of proguanil., Proc. Natl. Acad. Sci. U.S.A.
Wooden et al., 1997, Analysis in yeast of antimalaria drugs that target the dihydrofolate reductase of Plasmodium falciparum., Mol. Biochem. Parasitol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Rastelli et al., 2003, Structure of Plasmodium vivax dihydrofolate reductase determined by homology modeling and molecular dynamics refinement., Bioorg. Med. Chem. Lett.
Tropak MB et al., 2015, Pyrimethamine Derivatives: Insight into Binding Mechanism and Improved Enhancement of Mutant β-N-acetylhexosaminidase Activity., J Med Chem
Pivot et al., 2001, Pemetrexed disodium in recurrent locally advanced or metastatic squamous cell carcinoma of the head and neck., Br. J. Cancer
Kindler, 2002, Pemetrexed in pancreatic cancer., Semin. Oncol.
Hanauske et al., 2001, Pemetrexed disodium: a novel antifolate clinically active against multiple solid tumors., Oncologist
Mauritz et al., 2002, Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis., Biochem. Pharmacol.
Adjei, 2001, Gemcitabine and Pemetrexed disodium in treating breast cancer., Oncology (Williston Park, N.Y.)
Adjei, 2002, Pemetrexed in the treatment of selected solid tumors., Semin. Oncol.
Giovannetti et al., 2005, Cellular and pharmacogenetics foundation of synergistic interaction of pemetrexed and gemcitabine in human non-small-cell lung cancer cells., Mol. Pharmacol.
Norman, 2001, Pemetrexed disodium (Eli Lilly)., Curr Opin Investig Drugs
Schultz et al., Sequence dependence of Alimta (LY231514, MTA) combined with doxorubicin in ZR-75-1 human breast carcinoma cells., Anticancer Res.
Molina et al., 2003, The role of Pemetrexed (Alimta , LY231514) in lung cancer therapy., Clin Lung Cancer
Adjei, 2001, Gemcitabine and pemetrexed disodium combinations in vitro and in vivo., Lung Cancer
Corrigan A et al., 2014, Pharmacogenetics of pemetrexed combination therapy in lung cancer: pathway analysis reveals novel toxicity associations., Pharmacogenomics J
Jung M et al., 2013, Pharmacogenomic assessment of outcomes of pemetrexed-treated patients with adenocarcinoma of the lung., Yonsei Med J
Kodidela S et al., 2015, Influence of dihydrofolate reductase gene polymorphisms rs408626 (-317A>G) and rs442767 (-680C>A) on the outcome of methotrexate-based maintenance therapy in South Indian patients with acute lymphoblastic leukemia., Eur J Clin Pharmacol
Jabeen S et al., 2015, Impact of genetic variants of RFC1, DHFR and MTHFR in osteosarcoma patients treated with high-dose methotrexate., Pharmacogenomics J
Salazar J et al., 2014, Polymorphisms in genes involved in the mechanism of action of methotrexate: are they associated with outcome in rheumatoid arthritis patients?, Pharmacogenomics
Salazar J et al., 2012, Methotrexate consolidation treatment according to pharmacogenetics of MTHFR ameliorates event-free survival in childhood acute lymphoblastic leukaemia., Pharmacogenomics J
Sharma S et al., 2009, Purine biosynthetic pathway genes and methotrexate response in rheumatoid arthritis patients among north Indians., Pharmacogenet Genomics
Al-Shakfa F et al., 2009, DNA variants in region for noncoding interfering transcript of dihydrofolate reductase gene and outcome in childhood acute lymphoblastic leukemia., Clin Cancer Res
Ongaro A et al., 2009, Gene polymorphisms in folate metabolizing enzymes in adult acute lymphoblastic leukemia: effects on methotrexate-related toxicity and survival., Haematologica
Neef et al., 1976, Interaction of 1,N6-ethenoadenine derivatives of triphosphopyridine and reduced triphosphopyridine nucleotides with dihydrofolate reductase from amethopterin-resistant L1210 cells., Biochemistry
Hänggi et al., 1976, Altered regulation of the rate of synthesis of dihydrofolate reductase in methotrexate-resistant hamster cells., J. Biol. Chem.
Wani et al., 1994, Increased methotrexate resistance and dhfr gene amplification as a consequence of induced Ha-ras expression in NIH 3T3 cells., Cancer Res.
Kaufman et al., 1981, Amplification and loss of dihydrofolate reductase genes in a Chinese hamster ovary cell line., Mol. Cell. Biol.
Domin et al., 1983, Establishment of dihydrofolate reductase-increased human cell lines and relationship between dihydrofolate reductase levels and gene copy., Cancer Res.
Thompson et al., 1992, Assay for expression of methotrexate-resistant dihydrofolate reductase activity in the presence of drug-sensitive enzyme., J Pharmacol Toxicol Methods
Selassie et al., 1982, A comparison of the inhibition of growth of methotrexate-resistant and -sensitive leukemia cells in culture by triazines. Evidence for a new mechanism of cell resistance to methotrexate., J. Med. Chem.
Cavalcanti et al., 1992, Simultaneous changes in various mechanisms that mediate the cell incorporation of folate compounds account for low levels of resistance to methotrexate., Cell Biochem. Funct.
Serra et al., 2004, Analysis of dihydrofolate reductase and reduced folate carrier gene status in relation to methotrexate resistance in osteosarcoma cells., Ann. Oncol.
Bennett et al., 2006, Neutron diffraction studies of Escherichia coli dihydrofolate reductase complexed with methotrexate., Proc. Natl. Acad. Sci. U.S.A.
Uga et al., 2006, A new mechanism of methotrexate action revealed by target screening with affinity beads., Mol. Pharmacol.
Al-Rashood et al., 2006, Synthesis, dihydrofolate reductase inhibition, antitumor testing, and molecular modeling study of some new 4(3H)-quinazolinone analogs., Bioorg. Med. Chem.
Totani et al., 2006, High-mannose-type glycan modifications of dihydrofolate reductase using glycan-methotrexate conjugates., Bioorg. Med. Chem.
Assaraf, 2007, Molecular basis of antifolate resistance., Cancer Metastasis Rev.
Inoue K et al., 2014, Molecular basis for pharmacokinetics and pharmacodynamics of methotrexate in rheumatoid arthritis therapy., Drug Metab Pharmacokinet
Nahimana et al., 2004, Mutations of Pneumocystis jirovecii dihydrofolate reductase associated with failure of prophylaxis., Antimicrob. Agents Chemother.
Floris-Moore et al., 2003, Adverse reactions to trimethoprim/sulfamethoxazole in AIDS., Ann Pharmacother
Rosowsky et al., 2004, Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase., J. Med. Chem.
Barrow et al., 2004, Functional cloning of Bacillus anthracis dihydrofolate reductase and confirmation of natural resistance to trimethoprim., Antimicrob. Agents Chemother.
Laskowska et al., 2003, Trimethoprim induces heat shock proteins and protein aggregation in E. coli cells., Curr. Microbiol.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Selhub et al., 1978, Inhibition of folate enzymes by sulfasalazine., J. Clin. Invest.
Takebe et al., 2001, Generation of dual resistance to 4-hydroperoxycyclophosphamide and methotrexate by retroviral transfer of the human aldehyde dehydrogenase class 1 gene and a mutated dihydrofolate reductase gene., Mol. Ther.
Levine et al., 1985, Effects of estrogen and tamoxifen on the regulation of dihydrofolate reductase gene expression in a human breast cancer cell line., Cancer Res.
Takemura et al., 1996, Biological activity and intracellular metabolism of ZD1694 in human leukemia cell lines with different resistance mechanisms to antifolate drugs., Jpn. J. Cancer Res.
Li et al., 1995, Antitumor activity of antifolate inhibitors of thymidylate and purine synthesis in human soft tissue sarcoma cell lines with intrinsic resistance to methotrexate., Clin. Cancer Res.
Polshakov et al., 1999, Structure and dynamics in solution of the complex of Lactobacillus casei dihydrofolate reductase with the new lipophilic antifolate drug trimetrexate., Protein Sci.
Warlick et al., 2002, In vivo selection of antifolate-resistant transgenic hematopoietic stem cells in a murine bone marrow transplant model., J. Pharmacol. Exp. Ther.
Bertino et al., 1999, Use of variants of dihydrofolate reductase in gene transfer to produce resistance to methotrexate and trimetrexate., Prog Exp Tumor Res
Graffner-Nordberg et al., 2001, Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii., J. Med. Chem.
Zhu et al., Severe folate restriction results in depletion of and alteration in the composition of the intracellular folate pool, moderate sensitization to methotrexate and trimetrexate, upregulation of endogenous DHFR activity, and overexpression of metallothionein II and folate receptor alpha that, upon folate repletion, confer drug resistance to CHL cells., J. Exp. Ther. Oncol.
Sweeney et al., 2003, Trimetrexate inhibits progression of the murine 32Dp210 model of chronic myeloid leukemia in animals expressing drug-resistant dihydrofolate reductase., Cancer Res.
Sowers R et al., 2011, Impairment of methotrexate transport is common in osteosarcoma tumor samples., Sarcoma

PIRITREXIM DHFR

Interaction Score: 16.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17139284 17016423 10592235

Sources:
TTD
PRALATREXATE DHFR

Interaction Score: 6.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name PDX

Novel drug target Established target

Mechanism of Interaction Dihydrofolate reductase inhibitor

PMIDs:
23409799

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions TEND
PEMETREXED DHFR

Interaction Score: 5.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Alimta

Novel drug target Established target

Trial Name -

PMIDs:
11531245 12571811 11524555 11841783 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712 24732178 23709418

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial TEND PharmGKB
TRIMETREXATE DHFR

Interaction Score: 4.58

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10091649 11752096 10386066 11448221 12416030 12649191 11752352 21234348

Sources:
TdgClinicalTrial TEND
ICLAPRIM DHFR

Interaction Score: 4.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL22148 DHFR

Interaction Score: 4.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25984755

Sources:
DTC
METHOTREXATE SODIUM DHFR

Interaction Score: 4.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dihydrofolate reductase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRIMETHOPRIM DHFR

Interaction Score: 2.62

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
15504856 14632594 15115391 11752352 15561838 14629008

Sources:
TTD
PYRIMETHAMINE DHFR

Interaction Score: 2.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
9380737 9108546 11752352 12951104 25984755

Sources:
DTC
RALTITREXED DHFR

Interaction Score: 1.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8698629 9816025

Sources:
NCI
TALOTREXIN DHFR

Interaction Score: 1.37

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name talotrexin, PT-523,Talvesta

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
PERFOSFAMIDE DHFR

Interaction Score: 1.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11162315

Sources:
NCI
METHOTREXATE DHFR

Interaction Score: 1.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name VIBEX MTX

Mechanism of Interaction Dihydrofolate reductase inhibitor

PMIDs:
26335211 25778468 25084201 21747412 19902562 19861437 19648163 9129 944698 8162600 7346712 6831441 1489988 7057421 1533575 14679136 17130456 16936229 16971132 16647263 11752352 17333344 24284432

Sources:
TdgClinicalTrial ChemblInteractions NCI PharmGKB
SULFASALAZINE DHFR

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22555

Sources:
NCI
TAMOXIFEN DHFR

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
3978632

Sources:
NCI

Ensembl: ENSG00000228716
- Version: 101_38
Alternate Names:

DHFR Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P00374
- Version: 11-September-2012
Alternate Names:

DHFR Uniprot Gene Name

ENSG00000228716 Ensembl Gene Id

DYR_HUMAN Uniprot Id

Gene Info:

Uniprot Evidence 1: Evidence at protein level

Interpro Short Name DHFR_dom

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: P00374
- Version: 01-August-2011
Alternate Names:

ENSG00000228716 Ensembl Gene Id

P00374 Uniprot Accession

DHFR Gene Symbol

Gene Info:

Target Subclass 1.5.1.3

Target Main Class Enzymes

Publications:
RussLampel: ENSG00000188985
- Version: 26-July-2011
Alternate Names:

DHFR Display Id

ENSG00000188985 Ensembl Gene Id

DIHYDROFOLATE REDUCTASE (EC 1.5.1.3). [SOURCE:UNIPROT/SWISSPROT;ACC:P00374] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P00374
- Version: January-2014
Alternate Names:

DHFR Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:1.5.1.3

Publications:
RussLampel: ENSG00000168129
- Version: 26-July-2011
Alternate Names:

DHFR Display Id

DIHYDROFOLATE REDUCTASE (EC 1.5.1.3). [SOURCE:UNIPROT/SWISSPROT;ACC:P00374] Description

ENSG00000168129 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

PharmGKB: DHFR

Version: 18-August-2020

Alternate Names:

PA143 PharmGKB ID

Gene Info:

Publications:

Corrigan A et al., 2014, Pharmacogenetics of pemetrexed combination therapy in lung cancer: pathway analysis reveals novel toxicity associations., Pharmacogenomics J

Jung M et al., 2013, Pharmacogenomic assessment of outcomes of pemetrexed-treated patients with adenocarcinoma of the lung., Yonsei Med J

Salazar J et al., 2014, Polymorphisms in genes involved in the mechanism of action of methotrexate: are they associated with outcome in rheumatoid arthritis patients?, Pharmacogenomics

NCI: DHFR

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Li et al., 1995, Antitumor activity of antifolate inhibitors of thymidylate and purine synthesis in human soft tissue sarcoma cell lines with intrinsic resistance to methotrexate., Clin. Cancer Res.

Schornagel et al., 1984, Synthesis and evaluation of 2,4-diaminoquinazoline antifolates with activity against methotrexate-resistant human tumor cells., Biochem. Pharmacol.

Tang et al., 1994, Formation and repair of antitumor antibiotic CC-1065-induced DNA adducts in the adenine phosphoribosyltransferase and amplified dihydrofolate reductase genes of Chinese hamster ovary cells., Biochemistry

DTC: DHFR
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Tropak MB et al., 2015, Pyrimethamine Derivatives: Insight into Binding Mechanism and Improved Enhancement of Mutant β-N-acetylhexosaminidase Activity., J Med Chem
ChemblInteractions: DHFR
- Version: chembl_23
Alternate Names:

DHFR GENE_SYMBOL

Dihydrofolate reductase UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000228716
- Version: 31-May-2017
Alternate Names:

ENSG00000228716 Gene Symbol

DHFR Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TTD: Dihydrofolate reductase
- Version: 2020.06.01
Alternate Names:

DHFR TTD Gene Abbreviation

T17345 TTD Target ID

Gene Info:

Publications:
Pharos: DHFR
- Version: 01-February-2022
Alternate Names:

Dihydrofolate reductase Gene Name

P00374 UniProt ID

Gene Info:

Gene Categories:

ENZYME

Publications:
ClearityFoundationClinicalTrial: DHFR
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:

Trial Name	PDX
Novel drug target	Established target
Mechanism of Interaction	Dihydrofolate reductase inhibitor

Trial Name	Alimta
Novel drug target	Established target
Trial Name	-

Mechanism of Interaction	Dihydrofolate reductase inhibitor
Direct Interaction	yes

Trial Name	talotrexin, PT-523,Talvesta
Novel drug target	Established target

DHFR	Uniprot Gene Name
ENSG00000228716	Ensembl Gene Id
DYR_HUMAN	Uniprot Id

DHFR	Display Id
ENSG00000188985	Ensembl Gene Id
DIHYDROFOLATE REDUCTASE (EC 1.5.1.3). [SOURCE:UNIPROT/SWISSPROT;ACC:P00374]	Description

DHFR Gene Record

DHFR 1719 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17139284 17016423 10592235

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name PDX Novel drug target Established target Mechanism of Interaction Dihydrofolate reductase inhibitor

PMIDs: 23409799

Sources: TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Alimta Novel drug target Established target Trial Name -

PMIDs: 11531245 12571811 11524555 11841783 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712 24732178 23709418

Sources: TdgClinicalTrial ClearityFoundationClinicalTrial TEND PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10091649 11752096 10386066 11448221 12416030 12649191 11752352 21234348

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25984755

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Dihydrofolate reductase inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 15504856 14632594 15115391 11752352 15561838 14629008

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 9380737 9108546 11752352 12951104 25984755

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8698629 9816025

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info: Trial Name talotrexin, PT-523,Talvesta Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11162315

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name VIBEX MTX Mechanism of Interaction Dihydrofolate reductase inhibitor

PMIDs: 26335211 25778468 25084201 21747412 19902562 19861437 19648163 9129 944698 8162600 7346712 6831441 1489988 7057421 1533575 14679136 17130456 16936229 16971132 16647263 11752352 17333344 24284432

Sources: TdgClinicalTrial ChemblInteractions NCI PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22555

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 3978632

Sources: NCI

Ensembl: ENSG00000228716

Alternate Names: DHFR Ensembl Gene Name

Gene Info: Gene Biotype PROTEIN_CODING

Publications:

HopkinsGroom: P00374

Alternate Names: DHFR Uniprot Gene Name ENSG00000228716 Ensembl Gene Id DYR_HUMAN Uniprot Id

Gene Info: Uniprot Evidence 1: Evidence at protein level Interpro Short Name DHFR_dom Human Readable Name DRUGGABLE GENOME

Gene Categories: DRUGGABLE GENOME

Publications:

TEND: P00374

Alternate Names: ENSG00000228716 Ensembl Gene Id P00374 Uniprot Accession DHFR Gene Symbol

Gene Info: Target Subclass 1.5.1.3 Target Main Class Enzymes

Publications:

RussLampel: ENSG00000188985

Interaction Types & Directionality:

n/a

PMIDs:
17139284 17016423 10592235

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name PDX

Novel drug target Established target

Mechanism of Interaction Dihydrofolate reductase inhibitor

PMIDs:
23409799

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Alimta

Novel drug target Established target

Trial Name -

PMIDs:
11531245 12571811 11524555 11841783 11252887 12023793 15795320 11752352 11763166 11848474 14596699 11742712 24732178 23709418

Sources:
TdgClinicalTrial ClearityFoundationClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10091649 11752096 10386066 11448221 12416030 12649191 11752352 21234348

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
25984755

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dihydrofolate reductase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
15504856 14632594 15115391 11752352 15561838 14629008

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
9380737 9108546 11752352 12951104 25984755

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
8698629 9816025

Sources:
NCI

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name talotrexin, PT-523,Talvesta

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
11162315

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name VIBEX MTX

Mechanism of Interaction Dihydrofolate reductase inhibitor

PMIDs:
26335211 25778468 25084201 21747412 19902562 19861437 19648163 9129 944698 8162600 7346712 6831441 1489988 7057421 1533575 14679136 17130456 16936229 16971132 16647263 11752352 17333344 24284432

Sources:
TdgClinicalTrial ChemblInteractions NCI PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22555

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
3978632

Sources:
NCI

Alternate Names:

DHFR Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Alternate Names:

DHFR Uniprot Gene Name

ENSG00000228716 Ensembl Gene Id

DYR_HUMAN Uniprot Id

Gene Info:

Uniprot Evidence 1: Evidence at protein level

Interpro Short Name DHFR_dom

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

ENSG00000228716 Ensembl Gene Id

P00374 Uniprot Accession

DHFR Gene Symbol

Gene Info:

Target Subclass 1.5.1.3

Target Main Class Enzymes

Alternate Names:

DHFR Display Id

ENSG00000188985 Ensembl Gene Id

DIHYDROFOLATE REDUCTASE (EC 1.5.1.3). [SOURCE:UNIPROT/SWISSPROT;ACC:P00374] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

DHFR Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:1.5.1.3

Alternate Names:

DHFR Display Id

DIHYDROFOLATE REDUCTASE (EC 1.5.1.3). [SOURCE:UNIPROT/SWISSPROT;ACC:P00374] Description

ENSG00000168129 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

PA143 PharmGKB ID

Publications:

Tropak MB et al., 2015, Pyrimethamine Derivatives: Insight into Binding Mechanism and Improved Enhancement of Mutant β-N-acetylhexosaminidase Activity., J Med Chem

Alternate Names:

DHFR GENE_SYMBOL

Dihydrofolate reductase UNIPROT

Alternate Names:

ENSG00000228716 Gene Symbol

DHFR Ensembl Id

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

DHFR TTD Gene Abbreviation

T17345 TTD Target ID

Alternate Names:

Dihydrofolate reductase Gene Name

P00374 UniProt ID

Gene Categories:

ENZYME