Tchem FOLR1 Folate receptor alpha

Protein Summary

Description

Binds to folate and reduced folic acid derivatives and mediates delivery of 5-methyltetrahydrofolate and folate analogs into the interior of cells. Has high affinity for folate and folic acid analogs at neutral pH. Exposure to slightly acidic pH after receptor endocytosis triggers a conformation change that strongly reduces its affinity for folates and mediates their release. Required for normal embryonic development and normal cell proliferation. The protein encoded by this gene is a member of the folate receptor family. Members of this gene family bind folic acid and its reduced derivatives, and transport 5-methyltetrahydrofolate into cells. This gene product is a secreted protein that either anchors to membranes via a glycosyl-phosphatidylinositol linkage or exists in a soluble form. Mutations in this gene have been associated with neurodegeneration due to cerebral folate transport deficiency. Due to the presence of two promoters, multiple transcription start sites, and alternative splicing, multiple transcript variants encoding the same protein have been found for this gene. [provided by RefSeq, Oct 2009]

Uniprot Accession IDs

• P15328
• Q53EW2
• Q6FGT8
• Q6LC90
• Q9UCT2
• FR-alpha

Gene Name

• FOLR1

Ensembl ID

• ENST00000312293
• ENSP00000308137
• ENSG00000110195
• ENST00000393676
• ENSP00000377281
• ENST00000393679
• ENSP00000377284
• ENST00000393681
• ENSP00000377286

Symbol

• FOLR
• FBP
• FOLR

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
PubMedID	0.82
transcription factor perturbation	0.8
disease perturbation	0.79
gene perturbation	0.77
small molecule perturbation	0.77

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 231.99   (req: < 5)

Gene RIFs: 90   (req: <= 3)

Antibodies: 432   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 231.99   (req: >= 5)

Gene RIFs: 90   (req: > 3)

Antibodies: 432   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 20

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 22

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 3

Approved Drugs (3)

Explore Approved Drugs

1 – 3 of 3

methotrexate

FOLR1Tchem

IC50: 6.94000006

pemetrexed

FOLR1Tchem

IC50: 7.38000011

raltitrexed

FOLR1Tchem

IC50: 7.82000017

Active Ligands (22)

Explore Active Ligands

1 – 10 of 22

CHEMBL1834488

FOLR1Tchem

IC50: 9.51

CHEMBL3628344

FOLR1Tchem

IC50: 9.48

CHEMBL3628346

FOLR1Tchem

IC50: 9.21

CHEMBL590740

FOLR1Tchem

IC50: 8.74

CHEMBL3409335

FOLR1Tchem

IC50: 7.31

CHEMBL3628345

FOLR1Tchem

IC50: 6.81

CHEMBL3407519

FOLR1Tchem

IC50: 6.26

CHEMBL3335605

FOLR1Tchem

IC50: 8.02

CHEMBL3628347

FOLR1Tchem

IC50: 6.83

CHEMBL3409334

FOLR1Tchem

IC50: 6.96

Protein Data Bank (5)

1 – 5 of 5

PDB Structure Id	Ligand	Method	Resolution (Å)	M.W. (kDa)	Pub Year	Title

PDB Structure Id	M.W.	Resolution	Pub Year

Pathways (89)

Reactome (10)

KEGG (2)

WikiPathways (77)

Asparagine N-linked glycosylation (R-HSA-446203)

Click on a row in the table to change the structure displayed.

Items per page:

5

1 – 5 of 10

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Asparagine N-linked glycosylation	286 targets	R-HSA-446203
Reactome	COPI-mediated anterograde transport	83 targets	R-HSA-6807878
Reactome	COPII-mediated vesicle transport	68 targets	R-HSA-204005
Reactome	Cargo concentration in the ER	33 targets	R-HSA-5694530
Reactome	ER to Golgi Anterograde Transport	136 targets	R-HSA-199977

Name	Explore in Pharos	Explore in Source
Asparagine N-linked glycosylation	286 targets	R-HSA-446203
COPI-mediated anterograde transport	83 targets	R-HSA-6807878
COPII-mediated vesicle transport	68 targets	R-HSA-204005
Cargo concentration in the ER	33 targets	R-HSA-5694530
ER to Golgi Anterograde Transport	136 targets	R-HSA-199977

Gene Ontology Terms (36)

Functions (5)

Components (16)

Processes (15)

Items per page:

10

1 – 5 of 5

GO Term	Evidence	Assigned by
folic acid binding	Inferred from Direct Assay (IDA)	UniProtKB
methotrexate binding	Inferred from Direct Assay (IDA)	BHF-UCL
drug binding	Inferred from Physical Interaction (IPI)	BHF-UCL
folic acid receptor activity	Inferred from Mutant Phenotype (IMP)	UniProtKB
signaling receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central

Protein-Protein Interactions (168)

Explore Interacting Targets

1 – 10 of 168

• See Interactions on String-DB

ACTR10

Tbio

Novelty: 0.17285319

Score: 0.926

Data Source: STRINGDB

LMAN1

Tbio

Novelty: 0.00340578

Score: 0.921

Data Source: STRINGDB

SPTB

Tbio

Novelty: 0.0031907

Score: 0.918

Data Source: STRINGDB

TMED10

Tbio

Novelty: 0.0307377

Score: 0.913

Data Source: Reactome,STRINGDB

DCTN6

Tdark

Novelty: 0.93301435

Score: 0.913

Data Source: STRINGDB

ARFGAP2

Tbio

Family: Enzyme

Novelty: 0.07850068

Score: 0.91

Data Source: STRINGDB

CNIH1

Tbio

Novelty: 0.13636364

Score: 0.909

Data Source: STRINGDB

CAPZA1

Tbio

Novelty: 0.04371834

Score: 0.908

Data Source: STRINGDB

INS

Tbio

Novelty: 0.00000614

Score: 0.908

Data Source: STRINGDB

SPTBN4

Tbio

Novelty: 0.02643805

Score: 0.907

Data Source: STRINGDB

Publication Statistics

PubMed Score  231.99

PubMed score by year

Reset Zoom

PubTator Score  287.84

PubTator score by year

Reset Zoom

Amino Acid Sequence

Residue Counts

Sequence

MAQRMTTQLLLLLVWVAVVGEAQTRIAWARTELLNVCMNAKHHKEKPGPEDKLHEQCRPWRKNACCSTNT

1-70

SQEAHKDVSYLYRFNWNHCGEMAPACKRHFIQDTCLYECSPNLGPWIQQVDQSWRKERVLNVPLCKEDCE

70-140

QWWEDCRTSYTCKSNWHKGWNWTSGFNKCAVGAACQPFHFYFPTPTVLCNEIWTHSYKVSNYSRGSGRCI

140-210

QMWFDPAQGNPNEEVARFYAAAMSGAGPWAAWPFLLSLALMLLWLLS

210-257

MAQRMTTQLLLLLVWVAVVGEAQTRIAWARTELLNVCMNAKHHKEKPGPEDKLHEQCRPWRKNACCSTNTSQEAHKDVSYLYRFNWNHCGEMAPACKRHFIQDTCLYECSPNLGPWIQQVDQSWRKERVLNVPLCKEDCEQWWEDCRTSYTCKSNWHKGWNWTSGFNKCAVGAACQPFHFYFPTPTVLCNEIWTHSYKVSNYSRGSGRCIQMWFDPAQGNPNEEVARFYAAAMSGAGPWAAWPFLLSLALMLLWLLS

Find similar targets by:

Uniprot Keyword

3D-structure
Cell membrane
Complete proteome
Cytoplasmic vesicle
Direct protein sequencing
Disulfide bond
Endosome
Folate-binding
Glycoprotein
GPI-anchor