Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

Dhfr (P00375) - Overview - Molecular Target Synopsis

Protein


Dhfr, Dihydrofolate reductase
Enzyme Classification 1.5.1.3
UniProt P00375

Also Known as DYR_MOUSE, Dhfr

Key enzyme in folate metabolism. Contributes to the de novo mitochondrial thymidylate biosynthesis pathway (PubMed:25980602). Catalyzes an essential reaction for de novo glycine and purine synthesis, and for DNA precursor synthesis (PubMed:25980602). Binds its own mRNA. Homodimer.

3K45
ALTERNATE BINDING MODES OBSERVED FOR THE E- AND Z-ISOMERS OF 2,4- DIAMINOFURO[2,3D]PYRIMIDINES AS TERNARY COMPLEXES WITH NADPH AND MOUSE DIHYDROFOLATE REDUCTASE
RCSB/PDB
Inspect Structure
See all 3D Structures for Dhfr

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
187P00375-1

Sub-cellular localization


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



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project Dhfr has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

3D Structures


For Dhfr there are:
6 structures (6 chains) solved
6 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

Dhfr is solved in complex with the approved drug(s):

MTX/METHOTREXATE (1U70_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


Dhfr has been screened with 472 compounds (725 bioactivities), 134 compounds have bioactivities that show binding affinity of <= 500nM (195 bioactivities). (see details)