Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

DHFR (P00374) - Overview - Molecular Target Synopsis


DHFR, Dihydrofolate reductase
Enzyme Classification
UniProt P00374

Also Known as DYR_HUMAN, DHFR

Key enzyme in folate metabolism. Contributes to the de novo mitochondrial thymidylate biosynthesis pathway. Catalyzes an essential reaction for de novo glycine and purine synthesis, and for DNA precursor synthesis. Binds its own mRNA and that of DHFR2. Homodimer.

Isoforms / Transcripts (Protein Coding)


DHFR is targeted by Approved Drugs Raltitrexed, Pralatrexate, Pemetrexed, Methotrexate. (see details)

Sub-cellular localization

UniProt: DHFR is active in the following subcellular-locations: cytoplasm, mitochondrion.
GO terms: DHFR is active in the following subcellular-locations: cytosol, mitochondrion.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project DHFR has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: RPMI_8226, CCRF_CEM, COLO205

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: TK, COLO 206F, SK-N-DZ

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HeLa-S3, HSMM, A549

(see details)

3D Structures

For DHFR there are:
79 structures (93 chains) solved
78 are solved in complex with at least one small molecule ligand

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

DHFR has been screened with 1468 compounds (2692 bioactivities), 447 compounds have bioactivities that show binding affinity of <= 500nM (728 bioactivities). (see details)