General Information of Drug-Metabolizing Enzyme (DME) (ID: DEN8V7Z)

DME Name Glutamate carboxypeptidase II (FOLH1)
Synonyms
Glutamate carboxypeptidase 2; Membrane glutamate carboxypeptidase; N-acetylated-alpha-linked acidic dipeptidase I; Prostate-specific membrane antigen; Cell growth-inhibiting gene 27 protein; Folate hydrolase 1; Folylpoly-gamma-glutamate carboxypeptidase; Pteroylpoly-gamma-glutamate carboxypeptidase; mGCP; FGCP; FOLH; FOLH1; NAALAD1; NAALADase I; PSM; PSMA; GCPII; GIG27
Gene Name FOLH1
UniProt ID
FOLH1_HUMAN
INTEDE ID
DME0579
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Gene ID
2346
EC Number EC: 3.4.17.21
Hydrolases
Peptidase
Metallocarboxypeptidase
EC: 3.4.17.21
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MWNLLHETDSAVATARRPRWLCAGALVLAGGFFLLGFLFGWFIKSSNEATNITPKHNMKA
FLDELKAENIKKFLYNFTQIPHLAGTEQNFQLAKQIQSQWKEFGLDSVELAHYDVLLSYP
NKTHPNYISIINEDGNEIFNTSLFEPPPPGYENVSDIVPPFSAFSPQGMPEGDLVYVNYA
RTEDFFKLERDMKINCSGKIVIARYGKVFRGNKVKNAQLAGAKGVILYSDPADYFAPGVK
SYPDGWNLPGGGVQRGNILNLNGAGDPLTPGYPANEYAYRRGIAEAVGLPSIPVHPIGYY
DAQKLLEKMGGSAPPDSSWRGSLKVPYNVGPGFTGNFSTQKVKMHIHSTNEVTRIYNVIG
TLRGAVEPDRYVILGGHRDSWVFGGIDPQSGAAVVHEIVRSFGTLKKEGWRPRRTILFAS
WDAEEFGLLGSTEWAEENSRLLQERGVAYINADSSIEGNYTLRVDCTPLMYSLVHNLTKE
LKSPDEGFEGKSLYESWTKKSPSPEFSGMPRISKLGSGNDFEVFFQRLGIASGRARYTKN
WETNKFSGYPLYHSVYETYELVEKFYDPMFKYHLTVAQVRGGMVFELANSIVLPFDCRDY
AVVLRKYADKIYSISMKHPQEMKTYSVSFDSLFSAVKNFTEIASKFSERLQDFDKSNPIV
LRMMNDQLMFLERAFIDPLGLPDRPFYRHVIYAPSSHNKYAGESFPGIYDALFDIESKVD
PSKAWGEVKRQIYVAAFTVQAAAETLSEVA
Function
This enzyme has both folate hydrolase and N-acetylated-alpha-linked- acidic dipeptidase (NAALADase) activity. It has a preference for tri- alpha-glutamate peptides. It also exhibits a dipeptidyl-peptidase IV type activity. In vitro, it cleaves Gly-Pro-AMC.
KEGG Pathway
Alanine, aspartate and glutamate metabolism (hsa00250 )
Metabolic pathways (hsa01100 )
Vitamin digestion and absorption (hsa04977 )
Reactome Pathway
Aspartate and asparagine metabolism (R-HSA-8963693 )

Molecular Interaction Atlas (MIA) of This DME

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DME
1 Approved Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [49]

Molecular Expression Atlas (MEA) of This DME

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DME
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 2.60E-02 6.03E-02 2.87E-01
Alopecia ED70 Skin from scalp 1.79E-01 1.17E-01 2.59E-01
Alzheimer's disease 8A20 Entorhinal cortex 5.03E-01 -3.63E-02 -5.38E-02
Ankylosing spondylitis FA92.0 Pheripheral blood 4.79E-01 -7.34E-02 -3.35E-01
Aortic stenosis BB70 Calcified aortic valve 7.45E-01 2.16E-01 3.09E-01
Apnea 7A40 Hyperplastic tonsil 9.77E-01 -1.83E-01 -5.01E-01
Arthropathy FA00-FA5Z Peripheral blood 1.56E-01 6.86E-02 4.00E-01
Asthma CA23 Nasal and bronchial airway 7.32E-04 -1.92E-01 -1.94E-01
Atopic dermatitis EA80 Skin 1.12E-01 7.47E-02 3.26E-01
Autism 6A02 Whole blood 3.07E-01 -1.23E-01 -4.98E-01
Autoimmune uveitis 9A96 Peripheral monocyte 7.55E-01 8.04E-02 2.40E-01
Autosomal dominant monocytopenia 4B04 Whole blood 4.56E-01 2.01E-01 9.06E-01
Bacterial infection of gingival 1C1H Gingival tissue 2.50E-01 -8.78E-03 -2.19E-02
Batten disease 5C56.1 Whole blood 2.17E-01 1.29E-01 1.21E+00
Behcet's disease 4A62 Peripheral blood 3.39E-01 1.92E-01 9.95E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 2.18E-01 -1.17E-01 -4.11E-01
Bladder cancer 2C94 Bladder tissue 9.97E-09 1.15E+00 7.22E+00
Breast cancer 2C60-2C6Z Breast tissue 6.62E-19 -2.29E-01 -4.91E-01
Cardioembolic stroke 8B11.20 Whole blood 1.34E-04 -3.11E-01 -1.14E+00
Cervical cancer 2C77 Cervical tissue 1.96E-01 -1.50E-01 -4.92E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 5.18E-01 -6.17E-02 -3.35E-01
Chronic hepatitis C 1E51.1 Whole blood 6.92E-02 1.44E-01 8.34E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 1.46E-02 1.58E-01 6.45E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 9.30E-01 -2.07E-02 -6.64E-02
Chronic rhinosinusitis CA0A Sinus mucosa tissue 1.60E-01 1.33E-01 7.35E-01
Colon cancer 2B90 Colon tissue 1.31E-08 1.10E-01 4.41E-01
Coronary artery disease BA80-BA8Z Peripheral blood 6.34E-01 -3.68E-02 -1.75E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 9.92E-01 4.58E-02 3.15E-01
Endometriosis GA10 Endometrium tissue 9.98E-01 -6.07E-02 -1.79E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 7.58E-01 -2.95E-02 -2.40E-01
Familial hypercholesterolemia 5C80.00 Whole blood 3.68E-01 -1.74E-01 -8.11E-01
Gastric cancer 2B72 Gastric tissue 9.79E-01 -1.17E-01 -3.14E-01
Glioblastopma 2A00.00 Nervous tissue 1.70E-33 -6.12E-01 -7.99E-01
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 9.68E-02 -3.11E-01 -3.22E+00
Glioma 2A00.0Y-2A00.0Z White matter tissue 3.10E-05 -2.98E+00 -2.55E+00
Head and neck cancer 2D42 Head and neck tissue 4.15E-03 -6.13E-02 -2.47E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 8.86E-01 -1.01E-01 -3.08E-01
Huntington's disease 8A01.10 Whole blood 4.84E-01 1.20E-02 1.24E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 3.46E-01 -1.00E-01 -3.40E-01
Immunodeficiency 4A00-4A20 Peripheral blood 6.87E-01 2.04E-02 2.01E-01
Influenza 1E30 Whole blood 4.99E-01 1.16E-01 4.50E-01
Interstitial cystitis GC00.3 Bladder tissue 4.18E-01 -3.69E-02 -3.13E-01
Intracranial aneurysm 8B01.0 Intracranial artery 4.00E-01 8.95E-02 2.88E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 7.91E-01 8.22E-02 1.70E-01
Ischemic stroke 8B11 Peripheral blood 2.89E-01 2.63E-02 1.55E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 6.62E-01 -3.26E-02 -1.22E-01
Lateral sclerosis 8B60.4 Skin 4.82E-02 2.19E-01 1.70E+00
Lateral sclerosis 8B60.4 Cervical spinal cord 4.50E-01 -6.62E-03 -3.59E-02
Liver cancer 2C12.0 Liver tissue 1.05E-05 -4.03E-01 -6.61E-01
Liver failure DB99.7-DB99.8 Liver tissue 2.66E-03 2.75E-01 2.07E+00
Lung cancer 2C25 Lung tissue 1.58E-02 2.84E-02 1.03E-01
Lupus erythematosus 4A40 Whole blood 3.73E-02 7.01E-02 1.45E-01
Major depressive disorder 6A70-6A7Z Hippocampus 3.79E-01 -9.42E-02 -3.52E-01
Major depressive disorder 6A70-6A7Z Whole blood 8.23E-02 6.97E-02 3.28E-01
Melanoma 2C30 Skin 2.74E-02 8.62E-01 8.82E-01
Multiple myeloma 2A83.1 Peripheral blood 4.61E-01 1.47E-01 1.05E+00
Multiple myeloma 2A83.1 Bone marrow 1.46E-03 -5.94E-01 -1.66E+00
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 5.69E-01 -2.99E-02 -1.47E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 5.70E-01 -1.85E-02 -5.95E-02
Myelofibrosis 2A20.2 Whole blood 2.09E-06 1.52E-01 9.51E-01
Myocardial infarction BA41-BA50 Peripheral blood 3.33E-01 1.77E-01 2.09E-01
Myopathy 8C70.6 Muscle tissue 2.16E-01 -1.31E-01 -8.86E-01
Neonatal sepsis KA60 Whole blood 1.10E-01 6.79E-02 2.56E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 7.86E-09 -1.66E+00 -5.93E+00
Non-alcoholic fatty liver disease DB92 Liver tissue 5.90E-01 1.60E-01 5.34E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 3.85E-02 1.55E-01 1.67E+00
Olive pollen allergy CA08.00 Peripheral blood 2.95E-01 4.12E-02 1.47E-01
Oral cancer 2B6E Oral tissue 2.69E-04 -5.61E-01 -1.20E+00
Osteoarthritis FA00-FA0Z Synovial tissue 9.78E-01 -1.13E-02 -6.46E-02
Osteoporosis FB83.1 Bone marrow 8.96E-01 -5.79E-02 -4.01E-01
Ovarian cancer 2C73 Ovarian tissue 1.14E-01 -1.87E-01 -8.33E-01
Pancreatic cancer 2C10 Pancreas 6.75E-03 -3.09E-01 -8.13E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 6.16E-01 2.51E-02 9.47E-02
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 6.30E-01 -1.96E-02 -1.18E-01
Pituitary cancer 2D12 Pituitary tissue 4.80E-01 9.59E-02 2.89E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 4.48E-01 -1.65E-01 -5.30E-01
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 9.85E-01 4.44E-02 2.39E-01
Polycythemia vera 2A20.4 Whole blood 1.01E-03 5.10E-02 3.70E-01
Pompe disease 5C51.3 Biceps muscle 9.14E-01 1.28E-02 1.07E-01
Preterm birth KA21.4Z Myometrium 6.09E-01 -1.38E-01 -4.74E-01
Prostate cancer 2C82 Prostate 1.40E-09 2.08E+00 2.21E+00
Psoriasis EA90 Skin 9.87E-07 2.22E-01 7.07E-01
Rectal cancer 2B92 Rectal colon tissue 1.39E-01 1.78E-01 7.88E-01
Renal cancer 2C90-2C91 Kidney 5.20E-01 -2.64E-01 -6.67E-01
Retinoblastoma 2D02.2 Uvea 1.10E-07 -4.56E-01 -3.17E+00
Rheumatoid arthritis FA20 Synovial tissue 7.84E-01 1.09E-01 2.63E-01
Rhinovirus infection CA42.1 Nasal epithelium tissue 3.65E-01 6.63E-02 3.16E-01
Schizophrenia 6A20 Prefrontal cortex 8.11E-01 -4.86E-02 -1.02E-01
Schizophrenia 6A20 Superior temporal cortex 6.86E-01 -2.24E-02 -1.24E-01
Scleroderma 4A42.Z Whole blood 2.67E-01 5.97E-02 3.42E-01
Seizure 8A60-8A6Z Whole blood 5.67E-01 -1.59E-02 -8.89E-02
Sensitive skin EK0Z Skin 9.48E-01 -1.00E-01 -7.11E-01
Sepsis with septic shock 1G41 Whole blood 4.34E-06 1.93E-01 5.88E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 2.57E-01 4.66E-01 1.09E+00
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 4.82E-01 5.06E-03 2.41E-02
Simpson golabi behmel syndrome LD2C Adipose tissue 5.83E-01 -5.96E-02 -7.71E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 6.12E-01 8.32E-02 1.79E-01
Skin cancer 2C30-2C3Z Skin 4.11E-03 -2.06E-02 -4.57E-02
Thrombocythemia 3B63 Whole blood 1.12E-01 1.02E-01 6.34E-01
Thrombocytopenia 3B64 Whole blood 1.29E-01 5.27E-02 4.52E-01
Thyroid cancer 2D10 Thyroid 2.96E-08 2.19E-01 7.68E-01
Tibial muscular dystrophy 8C75 Muscle tissue 1.85E-01 5.36E-02 4.47E-01
Tuberous sclerosis complex LD2D.2 Perituberal tissue 7.93E-01 -1.99E-01 -1.54E+00
Type 2 diabetes 5A11 Liver tissue 7.79E-01 6.06E-02 1.58E-01
Ureter cancer 2C92 Urothelium 8.38E-01 -1.20E-01 -2.98E-01
Uterine cancer 2C78 Endometrium tissue 6.39E-08 -3.49E-01 -8.40E-01
Vitiligo ED63.0 Skin 6.18E-01 3.03E-02 5.93E-02
------------------------------------------------------------------------------------
⏷ Show the Full List of DME Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DME

DME DTT Name Glutamate carboxypeptidase II (GCPII) DTT Info
DME DTT Type Successful
3 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capromab DMHERIJ Prostate cancer 2C82.0 Approved [1]
Lutetium Lu-177 vipivotide tetraxetan DMQ0IZ6 Prostate cancer 2C82.0 Approved [2]
PSMA-11 Ga-68 DMWLTU2 Diagnostic imaging N.A. Approved [3]
40 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
177-Lu-PSMA-617 DMX178V Prostate cancer 2C82.0 Phase 3 [4]
BAY 2315497 DMUHH2G Prostate cancer 2C82.0 Phase 3 [5]
99mTc-MIP-1404 DML4GU1 Prostate cancer 2C82.0 Phase 2 [6]
ATL101 DMYAQV2 Influenza virus infection 1E30-1E32 Phase 2 [7]
G-202 DMQR9I8 Adenocarcinoma 2D40 Phase 2 [8]
J 591 Lu-177 DM9XKJU Prostate cancer 2C82.0 Phase 2 [9]
MLN-591RL DMJHVZC Prostate cancer 2C82.0 Phase 2 [10]
177-Lu-PSMA-R2 DMF4AOE Prostate cancer 2C82.0 Phase 1/2 [11]
177Lu-labelled PSMA-R2 DMWPD7N Prostate cancer 2C82.0 Phase 1/2 [12]
4SCAR-PSMA DMM8J5W Bladder cancer 2C94 Phase 1/2 [13]
64Cu-SAR-bisPSMA DMGUHFN Prostate cancer 2C82.0 Phase 1/2 [14]
67Cu-SAR-bisPSMA DMMYR39 Prostate cancer 2C82.0 Phase 1/2 [14]
Acapatamab DMTAI2F Prostate cancer 2C82.0 Phase 1/2 [15]
CAR-T cells targeting PSMA DMW340V Cervical cancer 2C77.0 Phase 1/2 [16]
LAVA-1207 DMQIZ8V Prostate cancer 2C82.0 Phase 1/2 [17]
MLN-2704 DMGC96P Prostate cancer 2C82.0 Phase 1/2 [18]
REGN4336 DMAKSZW Prostate cancer 2C82.0 Phase 1/2 [19]
REGN5678 DM0Y6WU Prostate cancer 2C82.0 Phase 1/2 [20]
177Lu-labelled CTT-1403 DMM2V74 Prostate cancer 2C82.0 Phase 1 [21]
225Ac-J591 DMVHFE1 Prostate cancer 2C82.0 Phase 1 [22]
225Ac-PSMA-617 DMG77MF Aggressive cancer 2A00-2F9Z Phase 1 [23]
227Th-labelled PSMA-TTC DM7L45S Prostate cancer 2C82.0 Phase 1 [24]
99mTc-MIP-1405 DMJB6E2 Prostate cancer 2C82.0 Phase 1 [6]
AMG 160 DMM0HNF Non-small-cell lung cancer 2C25 Phase 1 [25]
AMG 340 DM3VRX6 Prostate cancer 2C82.0 Phase 1 [26]
APVO414 DMXDMH5 Prostate cancer 2C82.0 Phase 1 [27]
Autologous T-cell therapy DMOAET3 Prostate cancer 2C82.0 Phase 1 [28]
BAY-1075553 DM8U3Q2 Prostate cancer 2C82.0 Phase 1 [29]
CCW702 DMPTYE6 Prostate cancer 2C82.0 Phase 1 [30]
CTT1403 DMAV86R Prostate cancer 2C82.0 Phase 1 [31]
GPI-16072 DM0ZQ48 Neuropathic pain 8E43.0 Phase 1 [32]
HPN424 DMLZDVR Prostate cancer 2C82.0 Phase 1 [33]
Iofolastat I-124 DMNBPKS Prostate cancer 2C82.0 Phase 1 [34]
JNJ-63898081 DMJFK6X Solid tumour/cancer 2A00-2F9Z Phase 1 [35]
MIP-1095 DMELSIU Prostate cancer 2C82.0 Phase 1 [36]
MT-112 DMT0EBU Solid tumour/cancer 2A00-2F9Z Phase 1 [37]
PSMA CAR-T cell therapy DM8Y1M9 Prostate cancer 2C82.0 Phase 1 [38]
PSMA subunit vaccine DMRHQTU Prostate cancer 2C82.0 Phase 1 [37]
PSMA-targeted tubulysin B conjugates DMOYX6W Prostate cancer 2C82.0 Phase 1 [39]
PSMA-VRP DM03O8T Prostate cancer 2C82.0 Phase 1 [40]
⏷ Show the Full List of 40 Clinical Trial Drug(s)
1 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
MDX-070 DM9ZEGT Prostate cancer 2C82.0 Discontinued in Phase 2 [41]
1 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
IRX-4 DMMUVAF Prostate cancer 2C82.0 Preclinical [42]
39 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
2-(2-carboxy-5-mercaptopentyl)benzoic acid DMEGY0T Discovery agent N.A. Investigative [43]
2-(2-carboxy-7-mercaptoheptyl)benzoic acid DMR98ML Discovery agent N.A. Investigative [43]
2-(2-Hydroxycarbamoyl-ethyl)-pentanedioic acid DMMEL39 Discovery agent N.A. Investigative [44]
2-(2-Mercapto-ethyl)-pentanedioic acid DMGELY0 Discovery agent N.A. Investigative [45]
2-(2-Phosphonooxy-ethyl)-pentanedioic acid DMQM6IA Discovery agent N.A. Investigative [45]
2-(3-carbamoylbenzyl)-5-mercaptopentanoic acid DMHXVNZ Discovery agent N.A. Investigative [43]
2-(3-carboxybenzyl)succinic acid DMI6AZ5 Discovery agent N.A. Investigative [43]
2-(3-cyanobenzyl)-5-mercaptopentanoic acid DMVB5U0 Discovery agent N.A. Investigative [43]
2-(3-Hydroxycarbamoyl-propyl)-pentanedioic acid DMFVITM Discovery agent N.A. Investigative [44]
2-(3-Mercapto-propyl)-pentanedioic acid DMMDNA8 Discovery agent N.A. Investigative [45]
2-(3-Methylsulfanyl-propyl)-pentanedioic acid DM4D1UT Discovery agent N.A. Investigative [45]
2-(4-Mercapto-butyl)-pentanedioic acid DMXPJF3 Discovery agent N.A. Investigative [45]
2-(5-Mercapto-pentyl)-pentanedioic acid DM0P6A3 Discovery agent N.A. Investigative [45]
2-benzyl-5-mercaptopentanoic acid DM3I7EL Discovery agent N.A. Investigative [43]
2-Hydroxycarbamoyl-pentanedioic acid DM412RI Discovery agent N.A. Investigative [44]
2-Hydroxycarbamoylmethyl-pentanedioic acid DMA8DZT Discovery agent N.A. Investigative [44]
2-Mercapto-pentanedioic acid DMRVBCI Discovery agent N.A. Investigative [45]
2-Mercaptomethyl-pentanedioic acid DMHK25N Discovery agent N.A. Investigative [45]
2-Phosphonooxy-pentanedioic acid DMM05AO Discovery agent N.A. Investigative [45]
2-PMPA DM27GZC Discovery agent N.A. Investigative [46]
3-(1-carboxy-4-mercaptobutoxy)benzoic acid DMHPYWM Discovery agent N.A. Investigative [43]
3-(2-carbamoyl-5-mercaptopentyl)benzoic acid DMNOKR3 Discovery agent N.A. Investigative [43]
3-(2-carboxy-3-mercaptopropyl)benzoic acid DM67B8S Discovery agent N.A. Investigative [43]
3-(2-carboxy-3-phosphonopropyl)benzoic acid DMG5R0N Discovery agent N.A. Investigative [43]
3-(2-carboxy-4-mercaptobutyl)benzoic acid DM6HPYN Discovery agent N.A. Investigative [43]
3-(2-carboxy-5-mercaptopentyl)benzoic acid DM6H52B Discovery agent N.A. Investigative [43]
3-(2-carboxy-6-mercaptohexyl)benzoic acid DM870W1 Discovery agent N.A. Investigative [43]
3-[(1-carboxy-4-mercaptobutyl)thio]benzoic acid DMLSET4 Discovery agent N.A. Investigative [43]
4-(2-carboxy-5-mercaptopentyl)benzoic acid DM5L4WP Discovery agent N.A. Investigative [43]
5-Mercapto-pentanoic acid DM7YGJO Discovery agent N.A. Investigative [45]
99mTc-EC-0652 DMAGTL1 Prostate cancer 2C82.0 Investigative [37]
99mTc-MIP-1340 DMQOFX2 Prostate cancer 2C82.0 Investigative [37]
CTT-54 DMQ5JX8 Solid tumour/cancer 2A00-2F9Z Investigative [37]
J591-Ac-225 DMXC319 Prostate cancer 2C82.0 Investigative [37]
MDX-1147 DM9ZTX4 Prostate cancer 2C82.0 Investigative [37]
MIP-1375 DM0J38I Prostate cancer 2C82.0 Investigative [37]
PGI-02749 DMTVY6K Brain injury NA07.Z Investigative [37]
PMID15027864C8d DMOQ8PF Discovery agent N.A. Investigative [47]
[3H]quisqualate DMDQBTX Discovery agent N.A. Investigative [48]
⏷ Show the Full List of 39 Investigative Drug(s)

References

1 Synergistic value of single-photon emission computed tomography/computed tomography fusion to radioimmunoscintigraphic imaging of prostate cancer. Semin Nucl Med. 2007 Jan;37(1):17-28.
2 [177Lu-PSMA-617 therapy, dosimetry and follow-up in patients with metastatic castration-resistant prostate cancer]. Nuklearmedizin. 2016 Jun 28;55(3):123-8.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
4 Review of 177Lu-PSMA-617 in Patients With Metastatic Castration-Resistant Prostate Cancer. Cureus. 2020 Jun 30;12(6):e8921.
5 ClinicalTrials.gov (NCT03724747) Study to Evaluate the Safety, Tolerability,Pharmacokinetics, and Antitumor Activity of a Thorium-227 Labeled Antibody-chelator Conjugate Alone and in Combination With Darolutamide, in Patients With Metastatic Castration Resistant Prostate Cancer. U.S. National Institutes of Health.
6 99mTc-labeled small-molecule inhibitors of prostate-specific membrane antigen for molecular imaging of prostate cancer. J Nucl Med. 2013 Aug;54(8):1369-76.
7 Clinical pipeline report, company report or official report of Atlab pharma.
8 National Cancer Institute Drug Dictionary (drug id 666090).
9 Phase II study of Lutetium-177-labeled anti-prostate-specific membrane antigen monoclonal antibody J591 for metastatic castration-resistant prostate cancer. Clin Cancer Res. 2013 Sep 15;19(18):5182-91.
10 Indium 111-labeled J591 anti-PSMA antibody for vascular targeted imaging in progressive solid tumors. EJNMMI Res. 2015 Apr 29;5:28.
11 National Cancer Institute Drug Dictionary (drug name Lu-177-PSMA-R2).
12 Radiopharmaceutical therapy in cancer: clinical advances and challenges. Nat Rev Drug Discov. 2020 Sep;19(9):589-608.
13 ClinicalTrials.gov (NCT03185468) Intervention of Bladder Cancer by CAR-T
14 Clinical pipeline report, company report or official report of Clarity Pharmaceuticals
15 The PSMA-targeting Half-life Extended BiTE Therapy AMG 160 has Potent Antitumor Activity in Preclinical Models of Metastatic Castration-resistant Prostate Cancer. Clin Cancer Res. 2021 May 15;27(10):2928-2937.
16 ClinicalTrials.gov (NCT03356795) Intervention of CAR-T Against Cervical Cancer
17 Clinical pipeline report, company report or official report of Lava Therapeutics
18 Phase I trial of the prostate-specific membrane antigen-directed immunoconjugate MLN2704 in patients with progressive metastatic castration-resistant prostate cancer. J Clin Oncol. 2008 May 1;26(13):2147-54.
19 ClinicalTrials.gov (NCT05125016) Phase 1/2 Study of REGN4336 (a PSMAXCD3 Bispecific Antibody) Administered Alone or in Combination With Cemiplimab in Patients With Metastatic Castration-Resistant Prostate Cancer. U.S.National Institutes of Health.
20 Clinical pipeline report, company report or official report of Regeneron Pharmaceuticals.
21 Clinical pipeline report, company report or official report of Cancer Targeted Technologies.
22 Novel agents and clinical trials in castration-resistant prostate cancer: latest updates from 2023 ASCO-GU Cancers Symposium. Exp Hematol Oncol. 2023 Aug 1;12(1):68.
23 (225)Ac-PSMA-617 for Therapy of Prostate Cancer. Semin Nucl Med. 2020 Mar;50(2):133-140.
24 Darolutamide Potentiates the Antitumor Efficacy of a PSMA-targeted Thorium-227 Conjugate by a Dual Mode of Action in Prostate Cancer Models. Clin Cancer Res. 2021 May 25.
25 Clinical pipeline report, company report or official report of Amgen.
26 ClinicalTrials.gov (NCT04740034) A Multicenter, Phase 1, Open-label, Dose-escalation and Expansion Study of AMG 340, a Bispecific Antibody Targeting PSMA in Subjects With Metastatic Castrate-Resistant Prostate Carcinoma. U.S.National Institutes of Health.
27 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
28 Antitumor activities of PSMA CD3 diabodies by redirected T-cell lysis of prostate cancer cells. Immunotherapy. 2013 Jan;5(1):27-38.
29 Preclinical evaluation of BAY 1075553, a novel (18)F-labelled inhibitor of prostate-specific membrane antigen for PET imaging of prostate cancer. Eur J Nucl Med Mol Imaging. 2014 Jan;41(1):89-101.
30 Clinical pipeline report, company report or official report of AbbVie.
31 177 Lu-Labeled Phosphoramidate-Based PSMA Inhibitors: The Effect of an Albumin Binder on Biodistribution and Therapeutic Efficacy in Prostate Tumor-Bearing Mice. Theranostics. 2017 Apr 27;7(7):1928-1939.
32 Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
33 Clinical pipeline report, company report or official report of Harpoon Therapeutics.
34 123I-MIP-1072, a small-molecule inhibitor of prostate-specific membrane antigen, is effective at monitoring tumor response to taxane therapy. J Nucl Med. 2011 Jul;52(7):1087-93.
35 Clinical pipeline report, company report or official report of Genmab.
36 Radiation dosimetry and first therapy results with a (124)I/ (131)I-labeled small molecule (MIP-1095) targeting PSMA for prostate cancer therapy. Eur J Nucl Med Mol Imaging. 2014 Jul;41(7):1280-92.
37 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1606).
38 Clinical pipeline report, company report or official report of Tmunity.
39 Prostate-specific membrane antigen targeted imaging and therapy of prostate cancer using a PSMA inhibitor as a homing ligand. Mol Pharm. 2009 May-Jun;6(3):780-9.
40 A phase I dose escalation trial of vaccine replicon particles (VRP) expressing prostate-specific membrane antigen (PSMA) in subjects with prostate cancer. Vaccine. 2013 Jan 30;31(6):943-9.
41 Nanoparticles for Improving Cancer Diagnosis. Mater Sci Eng R Rep. 2013 March; 74(3): 35-69.
42 Irx4 identifies a chamber-specific cell population that contributes to ventricular myocardium development. Dev Dyn. 2014 Mar;243(3):381-92.
43 Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain. J Med Chem. 2006 May 18;49(10):2876-85.
44 Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II. Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.
45 Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor. J Med Chem. 2003 May 8;46(10):1989-96.
46 Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury. Nat Med. 1999 Dec;5(12):1396-402.
47 Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents. J Med Chem. 2004 Mar 25;47(7):1729-38.
48 Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II. J Med Chem. 2007 Jul 12;50(14):3267-73.
49 Understanding and managing methotrexate nephrotoxicity. Oncologist. 2006 Jun;11(6):694-703.