Details of the Target

General Information of Target

Target ID LDTP05420
Target Name Glutamate carboxypeptidase 2 (FOLH1)
Gene Name FOLH1
Gene ID 2346
Synonyms
FOLH; NAALAD1; PSM; PSMA; Glutamate carboxypeptidase 2; EC 3.4.17.21; Cell growth-inhibiting gene 27 protein; Folate hydrolase 1; Folylpoly-gamma-glutamate carboxypeptidase; FGCP; Glutamate carboxypeptidase II; GCPII; Membrane glutamate carboxypeptidase; mGCP; N-acetylated-alpha-linked acidic dipeptidase I; NAALADase I; Prostate-specific membrane antigen; PSM; PSMA; Pteroylpoly-gamma-glutamate carboxypeptidase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MWNLLHETDSAVATARRPRWLCAGALVLAGGFFLLGFLFGWFIKSSNEATNITPKHNMKA
FLDELKAENIKKFLYNFTQIPHLAGTEQNFQLAKQIQSQWKEFGLDSVELAHYDVLLSYP
NKTHPNYISIINEDGNEIFNTSLFEPPPPGYENVSDIVPPFSAFSPQGMPEGDLVYVNYA
RTEDFFKLERDMKINCSGKIVIARYGKVFRGNKVKNAQLAGAKGVILYSDPADYFAPGVK
SYPDGWNLPGGGVQRGNILNLNGAGDPLTPGYPANEYAYRRGIAEAVGLPSIPVHPIGYY
DAQKLLEKMGGSAPPDSSWRGSLKVPYNVGPGFTGNFSTQKVKMHIHSTNEVTRIYNVIG
TLRGAVEPDRYVILGGHRDSWVFGGIDPQSGAAVVHEIVRSFGTLKKEGWRPRRTILFAS
WDAEEFGLLGSTEWAEENSRLLQERGVAYINADSSIEGNYTLRVDCTPLMYSLVHNLTKE
LKSPDEGFEGKSLYESWTKKSPSPEFSGMPRISKLGSGNDFEVFFQRLGIASGRARYTKN
WETNKFSGYPLYHSVYETYELVEKFYDPMFKYHLTVAQVRGGMVFELANSIVLPFDCRDY
AVVLRKYADKIYSISMKHPQEMKTYSVSFDSLFSAVKNFTEIASKFSERLQDFDKSNPIV
LRMMNDQLMFLERAFIDPLGLPDRPFYRHVIYAPSSHNKYAGESFPGIYDALFDIESKVD
PSKAWGEVKRQIYVAAFTVQAAAETLSEVA
Target Type
Successful
Target Bioclass
Enzyme
Family
Peptidase M28 family, M28B subfamily
Subcellular location
Cytoplasm; Cell membrane
Function
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.
TTD ID
T97071
Uniprot ID
Q04609
DrugMap ID
TT9G4N0
Ensemble ID
ENST00000256999.7
HGNC ID
HGNC:3788
ChEMBL ID
CHEMBL1892

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A549 SNV: p.M616R .
AU565 SNV: p.N51K .
FTC133 SNV: p.Y625C .
HCT15 Deletion: p.V239Ter
SNV: p.D244Y		 .
HEC1 SNV: p.G168R .
HEC1B SNV: p.G168R .
HT115 SNV: p.E727K .
JURKAT SNV: p.K407R .
KYSE150 SNV: p.N438D .
MDST8 SNV: p.G263D .
MEWO SNV: p.G221E .
NCIH1793 SNV: p.D599V .
NCIH1993 SNV: p.V253F .
NCIH2172 SNV: p.Q167K .
PF382 SNV: p.Y179H .
SNGM SNV: p.A701T .
SW1116 SNV: p.I708M .
SW480 SNV: p.N350D .
TE4 SNV: p.P166S .

Probe(s) Labeling This Target

PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-2
 Probe Info  		N.A.  LDD0139  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
TPA-induced transmembrane protein (TTMP) . Q5BVD1

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Capromab Antibody D09PGL
Capromab Pendetide BiotechDrug DB00089
Psma-11 Ga-68 Radioactive diagnostic agent DBG46D
Glutamic Acid Small molecular drug DB00142
Piflufolastat F 18 . DB14805
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
177lu-labelled Psma-617 Radiopharmaceutical therapy DGQW52
177-lu-psma-617 Small molecular drug DSM5X9
Phase 2
Click To Hide/Show 11 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mln-2704 Antibody D0W7FC
Mln-591rl Antibody D0H5ER
Regn5678 Antibody D8UZM7
4scar-psma CAR T Cell Therapy D0VI8T
Car-t Cells Targeting Psma CAR T Cell Therapy D0RO2L
177lu-labelled Psma-r2 Radiopharmaceutical therapy DP6J5K
177-lu-psma-r2 Small molecular drug D1CZ8K
99mtc-mip-1404 . D08FTP
Atl101 . D06URI
G-202 . D05MOZ
J 591 Lu-177 . D02EEK
Phase 1
Click To Hide/Show 18 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amg 160 Antibody DOY4E6
Autologous T-cell Therapy Antibody D04UWG
Ccw702 Antibody DY4X5W
Jnj-63898081 Antibody D2Y9IG
Mt-112 Antibody D0N6QB
Psma Car-t Cell Therapy CAR T Cell Therapy DAS4D6
177lu-labelled Ctt-1403 Radiopharmaceutical therapy DM6CE2
227th-labelled Psma-ttc Radiopharmaceutical therapy DXV67Q
Ctt1403 Small molecular drug DH5S6Z
Gpi-16072 Small molecular drug D0H4IU
Iofolastat I-124 Small molecular drug D04KRV
Psma Subunit Vaccine Vaccine D08JYV
Psma-vrp Vaccine D07KHR
99mtc-mip-1405 . D0F5KN
Apvo414 . D03JTL
Bay-1075553 . D0TN7S
Hpn424 . D48MDS
Psma-targeted Tubulysin B Conjugates . D0O0JB
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Irx-4 . D0M8PM
Investigative
Click To Hide/Show 42 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
J591-ac-225 Antibody D05UAO
2-(2-carboxy-5-mercaptopentyl)Benzoic Acid Small molecular drug D0QA5U
2-(2-carboxy-7-mercaptoheptyl)Benzoic Acid Small molecular drug D03JFL
2-(2-hydroxycarbamoyl-ethyl)-pentanedioic Acid Small molecular drug D05SNS
2-(2-mercapto-ethyl)-pentanedioic Acid Small molecular drug D0C2FS
2-(2-phosphonooxy-ethyl)-pentanedioic Acid Small molecular drug D0Z5VI
2-(3-carbamoylbenzyl)-5-mercaptopentanoic Acid Small molecular drug D0D8NM
2-(3-carboxybenzyl)Succinic Acid Small molecular drug D05VWZ
2-(3-cyanobenzyl)-5-mercaptopentanoic Acid Small molecular drug D0E3OH
2-(3-hydroxycarbamoyl-propyl)-pentanedioic Acid Small molecular drug D0ZJ9S
2-(3-mercapto-propyl)-pentanedioic Acid Small molecular drug D0Y7AN
2-(3-methylsulfanyl-propyl)-pentanedioic Acid Small molecular drug D0Q2OH
2-(4-mercapto-butyl)-pentanedioic Acid Small molecular drug D08TDE
2-(5-mercapto-pentyl)-pentanedioic Acid Small molecular drug D0Q3KD
2-benzyl-5-mercaptopentanoic Acid Small molecular drug D0B9YO
2-hydroxycarbamoyl-pentanedioic Acid Small molecular drug D02CYQ
2-hydroxycarbamoylmethyl-pentanedioic Acid Small molecular drug D0FU7Y
2-mercapto-pentanedioic Acid Small molecular drug D08CYU
2-mercaptomethyl-pentanedioic Acid Small molecular drug D0E0HK
2-phosphonooxy-pentanedioic Acid Small molecular drug D0A1FL
2-pmpa Small molecular drug D0Y6UB
3-(1-carboxy-4-mercaptobutoxy)Benzoic Acid Small molecular drug D0ND1C
3-(2-carbamoyl-5-mercaptopentyl)Benzoic Acid Small molecular drug D0JX2S
3-(2-carboxy-3-mercaptopropyl)Benzoic Acid Small molecular drug D0T8ZL
3-(2-carboxy-3-phosphonopropyl)Benzoic Acid Small molecular drug D0C5JP
3-(2-carboxy-4-mercaptobutyl)Benzoic Acid Small molecular drug D04VFS
3-(2-carboxy-5-mercaptopentyl)Benzoic Acid Small molecular drug D0F8TZ
3-(2-carboxy-6-mercaptohexyl)Benzoic Acid Small molecular drug D03RMT
3-[(1-carboxy-4-mercaptobutyl)Thio]Benzoic Acid Small molecular drug D0X1DO
4-(2-carboxy-5-mercaptopentyl)Benzoic Acid Small molecular drug D04SZR
5-mercapto-pentanoic Acid Small molecular drug D0Z0UQ
Pmid15027864c8d Small molecular drug D06JOJ
[3h]Quisqualate Small molecular drug D06DUE
(2s)-2-{[Hydroxy(4-iodobenzyl)Phosphoryl]Methyl}Pentanedioic Acid . DB06928
99mtc-ec-0652 . D0Z9BU
99mtc-mip-1340 . D0K3GB
Ctt-54 . D0M1NS
Dcfbc . DB07754
Mdx-1147 . D0IW9Q
Mip-1375 . D0Z5UD
Pgi-02749 . D06LAX
Spaglumic Acid . DB08835
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mdx-070 Antibody D03ZHE

References

1 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.