General Information of Target

Target ID LDTP02781
Target Name Folate receptor alpha (FOLR1)
Gene Name FOLR1
Gene ID 2348
Synonyms
FOLR; Folate receptor alpha; FR-alpha; Adult folate-binding protein; FBP; Folate receptor 1; Folate receptor, adult; KB cells FBP; Ovarian tumor-associated antigen MOv18
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAQRMTTQLLLLLVWVAVVGEAQTRIAWARTELLNVCMNAKHHKEKPGPEDKLHEQCRPW
RKNACCSTNTSQEAHKDVSYLYRFNWNHCGEMAPACKRHFIQDTCLYECSPNLGPWIQQV
DQSWRKERVLNVPLCKEDCEQWWEDCRTSYTCKSNWHKGWNWTSGFNKCAVGAACQPFHF
YFPTPTVLCNEIWTHSYKVSNYSRGSGRCIQMWFDPAQGNPNEEVARFYAAAMSGAGPWA
AWPFLLSLALMLLWLLS
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Folate receptor family
Subcellular location
Cell membrane
Function
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.
TTD ID
T83386
Uniprot ID
P15328
DrugMap ID
TTVC37M
Ensemble ID
ENST00000312293.9
HGNC ID
HGNC:3791
ChEMBL ID
CHEMBL2121

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
OPA-S-S-alkyne
 Probe Info 
K41(1.41); K44(1.80); K76(3.42); K97(4.12)  LDD3494  [1]
DBIA
 Probe Info 
C135(1.01)  LDD3313  [2]
TFBX
 Probe Info 
N.A.  LDD0027  [3]
Acrolein
 Probe Info 
N.A.  LDD0217  [4]
Crotonaldehyde
 Probe Info 
N.A.  LDD0219  [4]
Methacrolein
 Probe Info 
C37(0.00); C139(0.00); C146(0.00)  LDD0218  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa C37(0.00); C135(0.00); C209(0.00); C152(0.00)  LDD0222  [4]
 LDCM0107  IAA HeLa C135(0.00); C139(0.00); C146(0.00); C96(0.00)  LDD0221  [4]
 LDCM0022  KB02 A2780 C135(0.99)  LDD2254  [2]
 LDCM0023  KB03 ABC-1 C135(3.14)  LDD2679  [2]
 LDCM0024  KB05 Hs 936.T C135(1.01)  LDD3313  [2]
 LDCM0109  NEM HeLa N.A.  LDD0226  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Solute carrier family 35 member F6 (SLC35F6) SLC35F solute transporter family Q8N357

The Drug(s) Related To This Target

Approved
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Folic Acid Small molecular drug DB00158
Methotrexate Small molecular drug DB00563
Pyrimethamine Small molecular drug D0C0SK
Pafolacianine . DB15413
Phase 3
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Farletuzumab Monoclonal antibody D06XVN
Ec20 Small molecular drug D00BHL
Mirvetuximab Soravtansine . D0RP2W
Mk-8109 . D02TJT
Phase 2
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bms-753493 Small molecular drug D0N2GC
Folateimmune Small molecular drug D0N8JG
Talotrexin Small molecular drug D0GL7H
Ec-145 . D09JGH
Phase 1
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Stro-002 Antibody drug conjugate D10GPJ
Ec0489 Small molecular drug D06CVN
Imgn-853 . D07DPC
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Vintafolide . DB05168

References

1 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
4 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.