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

FOLH1 (Q04609) - Overview - Molecular Target Synopsis

Protein


FOLH1, Glutamate carboxypeptidase 2
Enzyme Classification 3.4.17.21
UniProt Q04609

Also Known as FOLH1_HUMAN, FOLH1, FOLH, NAALAD1, PSM, PSMA

Has both folate hydrolase and N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) activity. Has a preference for tri-alpha-glutamate peptides. In the intestine, required for the uptake of folate. In the brain, modulates excitatory neurotransmission through the hydrolysis of the neuropeptide, N-aceylaspartylglutamate (NAAG), thereby releasing glutamate. Involved in prostate tumor progression., Also exhibits a dipeptidyl-peptidase IV type activity. In vitro, cleaves Gly-Pro-AMC. Homodimer.

6FE5
X-RAY STRUCTURE OF HUMAN GLUTAMATE CARBOXYPEPTIDASE II (GCPII) - THE E424M INACTIVE MUTANT, IN COMPLEX WITH A INHIBITOR JHU 2249
RCSB/PDB
Inspect Structure
See all 3D Structures for FOLH1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: FOLH1 is active in the following subcellular-locations: cell membrane, cytoplasm.
GO terms: FOLH1 is active in the following subcellular-locations: cell surface, cytoplasm, extracellular exosome, integral component of plasma membrane, membrane, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project FOLH1 has gain in 4 cell-lines, loss in 1 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_2, UACC_62, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: LNCAP, HCC1482, SK-MEL-24

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: SK-N-SH, NHLF, HSMM

(see details)

3D Structures


For FOLH1 there are:
75 structures (78 chains) solved
75 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

FOLH1 is solved in complex with the approved drug(s):

MET/METHIONINE (2CIJ_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


FOLH1 has been screened with 320 compounds (491 bioactivities), 178 compounds have bioactivities that show binding affinity of <= 500nM (251 bioactivities). (see details)