Details of Drug-Metabolizing Enzyme (DME)

General Information of Drug-Metabolizing Enzyme (DME) (ID: DE7WS3H)

DME Name Aldo-keto reductase 1B1 (AKR1B1)
Synonyms Aldo-keto reductase family 1 member B1; Aldose reductase; AKR1B1; ALR2; AR
Gene Name AKR1B1
UniProt ID
ALDR_HUMAN
INTEDE ID
DME0087
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Gene ID
231
EC Number EC: 1.1.1.21
Oxidoreductase
CH-OH donor oxidoreductase
NAD/NADP oxidoreductase
EC: 1.1.1.21
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MASRLLLNNGAKMPILGLGTWKSPPGQVTEAVKVAIDVGYRHIDCAHVYQNENEVGVAIQ
EKLREQVVKREELFIVSKLWCTYHEKGLVKGACQKTLSDLKLDYLDLYLIHWPTGFKPGK
EFFPLDESGNVVPSDTNILDTWAAMEELVDEGLVKAIGISNFNHLQVEMILNKPGLKYKP
AVNQIECHPYLTQEKLIQYCQSKGIVVTAYSPLGSPDRPWAKPEDPSLLEDPRIKAIAAK
HNKTTAQVLIRFPMQRNLVVIPKSVTPERIAENFKVFDFELSSQDMTTLLSYNRNWRVCA
LLSCTSHKDYPFHEEF
Function
This enzyme catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols. It displays enzymatic activity towards endogenous metabolites such as aromatic and aliphatic aldehydes, ketones, monosacharides, bile acids and xenobiotics substrates. It displays low enzymatic activity toward all-trans-retinal, 9-cis-retinal, and 13-cis- retinal. It can also catalyzes the reduction of diverse phospholipid aldehydes such as 1-palmitoyl-2- (5-oxovaleroyl)-sn -glycero-3-phosphoethanolamin (POVPC) and related phospholipid aldehydes that are generated from the oxydation of phosphotidylcholine and phosphatdyleethanolamides. Besides, it plays a role in detoxifying dietary and lipid-derived unsaturated carbonyls, such as crotonaldehyde, 4-hydroxynonenal, trans-2-hexenal, trans-2,4-hexadienal and their glutathione-conjugates carbonyls (GS-carbonyls).
KEGG Pathway
Folate biosynthesis (hsa00790 )
Fructose and mannose metabolism (hsa00051 )
Galactose metabolism (hsa00052 )
Glycerolipid metabolism (hsa00561 )
Metabolic pathways (hsa01100 )
Pentose and glucuronate interconversions (hsa00040 )
Reactome Pathway
Pregnenolone biosynthesis (R-HSA-196108 )
Fructose biosynthesis (R-HSA-5652227 )

Molecular Interaction Atlas (MIA) of This DME

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DME
2 Approved Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Allopregnanolone DMNLHAC Depression 6A70-6A7Z approved [43]
FENOFIBRIC ACID DMGO2MC Cardiovascular disease BA00-BE2Z Approved [44]

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 4.05E-11 4.65E-01 8.38E-01
Alopecia ED70 Skin from scalp 7.96E-02 1.94E-02 6.03E-02
Alzheimer's disease 8A20 Entorhinal cortex 9.95E-01 8.94E-03 3.33E-02
Ankylosing spondylitis FA92.0 Pheripheral blood 1.38E-01 3.10E-01 5.53E-01
Aortic stenosis BB70 Calcified aortic valve 5.50E-01 -2.35E-01 -2.19E-01
Apnea 7A40 Hyperplastic tonsil 2.77E-01 4.66E-01 6.09E-01
Arthropathy FA00-FA5Z Peripheral blood 2.69E-02 -3.27E-01 -1.50E+00
Asthma CA23 Nasal and bronchial airway 1.28E-05 3.44E-01 4.31E-01
Atopic dermatitis EA80 Skin 7.72E-08 -4.20E-01 -1.70E+00
Autism 6A02 Whole blood 3.18E-02 -2.08E-01 -7.04E-01
Autoimmune uveitis 9A96 Peripheral monocyte 8.55E-02 -4.58E-01 -7.58E-01
Autosomal dominant monocytopenia 4B04 Whole blood 2.28E-01 -7.57E-01 -1.43E+00
Bacterial infection of gingival 1C1H Gingival tissue 4.37E-23 7.72E-01 1.92E+00
Batten disease 5C56.1 Whole blood 5.88E-01 3.03E-01 1.55E+00
Behcet's disease 4A62 Peripheral blood 7.28E-02 -3.51E-02 -2.29E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 1.34E-01 -2.45E-02 -1.12E-01
Bladder cancer 2C94 Bladder tissue 8.11E-01 -8.46E-02 -2.45E-01
Breast cancer 2C60-2C6Z Breast tissue 2.60E-44 -4.97E-01 -1.10E+00
Cardioembolic stroke 8B11.20 Whole blood 1.47E-08 -3.15E-01 -2.25E+00
Cervical cancer 2C77 Cervical tissue 1.95E-08 8.44E-01 1.86E+00
Childhood onset rheumatic disease FA20.Z Peripheral blood 6.18E-01 9.01E-02 6.75E-02
Chronic hepatitis C 1E51.1 Whole blood 2.77E-01 -2.28E-02 -7.65E-02
Chronic obstructive pulmonary disease CA22 Lung tissue 5.68E-01 -1.55E-02 -4.07E-02
Chronic obstructive pulmonary disease CA22 Small airway epithelium 1.19E-06 6.45E-01 1.01E+00
Chronic rhinosinusitis CA0A Sinus mucosa tissue 1.05E-02 -6.01E-01 -1.03E+00
Colon cancer 2B90 Colon tissue 6.27E-10 -3.15E-01 -5.40E-01
Coronary artery disease BA80-BA8Z Peripheral blood 5.65E-02 8.64E-01 1.57E+00
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 8.17E-01 -6.77E-02 -2.03E-01
Endometriosis GA10 Endometrium tissue 6.68E-01 3.66E-01 1.94E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 4.29E-01 5.86E-02 4.77E-01
Familial hypercholesterolemia 5C80.00 Whole blood 1.54E-03 3.20E-01 1.13E+00
Gastric cancer 2B72 Gastric tissue 9.99E-01 7.29E-02 4.70E-01
Glioblastopma 2A00.00 Nervous tissue 2.53E-18 2.17E-01 5.40E-01
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 7.43E-14 -7.43E-01 -1.54E+02
Glioma 2A00.0Y-2A00.0Z White matter tissue 7.01E-04 1.30E+00 1.59E+00
Head and neck cancer 2D42 Head and neck tissue 1.08E-20 9.36E-01 1.58E+00
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 4.98E-01 1.52E-01 3.85E-01
Huntington's disease 8A01.10 Whole blood 9.94E-01 -2.78E-02 -6.39E-02
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 3.00E-01 3.15E-01 9.73E-01
Immunodeficiency 4A00-4A20 Peripheral blood 1.98E-01 -5.51E-02 -7.84E-01
Influenza 1E30 Whole blood 1.18E-01 -6.97E-01 -1.48E+00
Interstitial cystitis GC00.3 Bladder tissue 4.14E-01 9.80E-02 3.47E-01
Intracranial aneurysm 8B01.0 Intracranial artery 3.28E-03 9.57E-01 2.26E+00
Irritable bowel syndrome DD91.0 Rectal colon tissue 7.82E-02 -9.39E-02 -2.59E-01
Ischemic stroke 8B11 Peripheral blood 5.72E-01 -5.72E-02 -2.00E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 1.30E-11 -4.96E-01 -1.14E+00
Lateral sclerosis 8B60.4 Skin 4.71E-01 1.04E-01 5.17E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 6.28E-01 -1.53E-01 -2.00E-01
Liver cancer 2C12.0 Liver tissue 4.98E-04 4.73E-02 1.18E-01
Liver failure DB99.7-DB99.8 Liver tissue 4.92E-08 2.74E+00 8.55E+00
Lung cancer 2C25 Lung tissue 6.33E-06 -1.87E-01 -4.93E-01
Lupus erythematosus 4A40 Whole blood 1.89E-02 8.42E-02 1.27E-01
Major depressive disorder 6A70-6A7Z Hippocampus 8.67E-01 1.40E-02 7.77E-02
Major depressive disorder 6A70-6A7Z Whole blood 3.47E-02 -1.30E-01 -5.18E-01
Melanoma 2C30 Skin 3.50E-03 1.03E+00 1.04E+00
Multiple myeloma 2A83.1 Peripheral blood 9.56E-01 -8.87E-02 -2.10E-01
Multiple myeloma 2A83.1 Bone marrow 4.82E-01 2.90E-01 6.12E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 5.02E-02 -1.23E-01 -4.97E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 6.12E-02 5.08E-02 1.13E-01
Myelofibrosis 2A20.2 Whole blood 3.73E-03 -7.16E-01 -2.71E+00
Myocardial infarction BA41-BA50 Peripheral blood 1.54E-02 -5.16E-01 -6.52E-01
Myopathy 8C70.6 Muscle tissue 7.02E-01 2.24E-02 1.23E-01
Neonatal sepsis KA60 Whole blood 3.22E-33 -1.09E+00 -3.08E+00
Neuroectodermal tumour 2A00.11 Brain stem tissue 4.25E-01 1.26E-01 3.90E-01
Non-alcoholic fatty liver disease DB92 Liver tissue 8.49E-02 5.31E-02 1.82E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 2.87E-01 -4.35E-02 -2.06E-01
Olive pollen allergy CA08.00 Peripheral blood 8.72E-01 -1.78E-01 -2.26E-01
Oral cancer 2B6E Oral tissue 6.99E-02 3.27E-01 3.07E-01
Osteoarthritis FA00-FA0Z Synovial tissue 2.68E-01 4.58E-01 4.39E-01
Osteoporosis FB83.1 Bone marrow 3.91E-01 -1.00E-01 -1.82E-01
Ovarian cancer 2C73 Ovarian tissue 2.91E-01 -4.77E-01 -7.92E-01
Pancreatic cancer 2C10 Pancreas 6.84E-03 9.32E-01 1.48E+00
Parkinson's disease 8A00.0 Substantia nigra tissue 7.81E-01 1.03E-02 2.33E-02
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 1.23E-03 -2.21E-01 -1.19E+00
Pituitary cancer 2D12 Pituitary tissue 1.82E-06 6.27E-01 2.95E+00
Pituitary gonadotrope tumour 2D12 Pituitary tissue 1.04E-05 6.22E-01 2.55E+00
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 1.54E-02 1.22E-01 1.22E+00
Polycythemia vera 2A20.4 Whole blood 7.39E-19 -6.59E-01 -2.79E+00
Pompe disease 5C51.3 Biceps muscle 9.11E-01 3.02E-02 4.23E-01
Preterm birth KA21.4Z Myometrium 7.57E-01 -9.79E-02 -2.49E-01
Prostate cancer 2C82 Prostate 8.82E-04 -1.70E-01 -2.57E-01
Psoriasis EA90 Skin 3.21E-01 -1.03E-01 -2.67E-01
Rectal cancer 2B92 Rectal colon tissue 6.47E-04 -8.71E-01 -2.69E+00
Renal cancer 2C90-2C91 Kidney 9.70E-01 -2.94E-01 -3.12E-01
Retinoblastoma 2D02.2 Uvea 3.97E-03 5.35E-01 2.91E+00
Rheumatoid arthritis FA20 Synovial tissue 3.36E-03 1.16E+00 2.04E+00
Rhinovirus infection CA42.1 Nasal epithelium tissue 4.04E-01 4.21E-02 1.09E-01
Schizophrenia 6A20 Prefrontal cortex 2.09E-03 -7.10E-02 -3.06E-01
Schizophrenia 6A20 Superior temporal cortex 2.47E-01 -1.39E-01 -5.29E-01
Scleroderma 4A42.Z Whole blood 6.01E-05 -2.60E-01 -1.63E+00
Seizure 8A60-8A6Z Whole blood 6.40E-01 4.65E-01 5.71E-01
Sensitive skin EK0Z Skin 8.84E-01 9.70E-02 7.71E-01
Sepsis with septic shock 1G41 Whole blood 5.96E-86 -8.74E-01 -2.73E+00
Shwachman-Diamond syndrome 3A70.0 Bone marrow 7.74E-03 -3.78E-01 -1.22E+00
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 5.90E-01 -8.08E-02 -1.77E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 8.90E-01 6.13E-03 8.56E-03
Sjogren's syndrome 4A43.2 Salivary gland tissue 2.72E-02 6.06E-01 2.71E+00
Skin cancer 2C30-2C3Z Skin 7.51E-59 1.06E+00 2.30E+00
Thrombocythemia 3B63 Whole blood 6.28E-06 -5.00E-01 -1.99E+00
Thrombocytopenia 3B64 Whole blood 3.91E-01 2.28E-01 4.16E-01
Thyroid cancer 2D10 Thyroid 5.14E-06 2.13E-01 7.65E-01
Tibial muscular dystrophy 8C75 Muscle tissue 2.94E-02 -2.34E-01 -9.51E-01
Tuberous sclerosis complex LD2D.2 Perituberal tissue 8.25E-01 -1.69E-01 -1.72E+00
Type 2 diabetes 5A11 Liver tissue 5.59E-01 4.27E-01 9.70E-01
Ureter cancer 2C92 Urothelium 8.41E-02 9.11E-02 3.04E-01
Uterine cancer 2C78 Endometrium tissue 7.72E-01 9.44E-02 1.54E-01
Vitiligo ED63.0 Skin 4.37E-01 -4.10E-02 -1.00E-01
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⏷ Show the Full List of DME Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DME

DME DTT Name Aldose reductase (AKR1B1) DTT Info
DME DTT Type Successful
2 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Epalrestat DM5OGK0 Diabetic neuropathy 8C0Z Approved [1]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [2]
11 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fidarestat DMZL1I8 Diabetic complication 5A2Y Phase 3 [3]
Ranirestat DMD5QRS Diabetic neuropathy 8C0Z Phase 3 [4]
BNV-222 DMYFQJL Diabetic neuropathy 8C0Z Phase 2/3 [4]
CONTIGOSIDE B DMX9V8K Thrombosis DB61-GB90 Phase 2/3 [5]
ADMVA DM819CO Diabetic complication 5A2Y Phase 2 [4]
LIDORESTAT DMA0RI9 Diabetic complication 5A2Y Phase 2 [6]
M-16209 DMZ7YX3 Diabetic complication 5A2Y Phase 2 [7]
QR-333 DMKVIWM Diabetic neuropathy 8C0Z Phase 2 [8]
T2c-003 DMWIH59 Diabetic neuropathy 8C0Z Phase 1/2 [4]
ALO-1567 DMGFVYL Glaucoma/ocular hypertension 9C61 Phase 1 [9]
SSR-125047 DMSUFW6 Schizophrenia 6A20 Phase 1 [10]
⏷ Show the Full List of 11 Clinical Trial Drug(s)
14 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
IMIRESTAT DM8KSMX Diabetic complication 5A2Y Discontinued in Phase 3 [11]
MINALRESTAT DM86XJG Diabetic complication 5A2Y Discontinued in Phase 3 [12]
Ponalrestat DM04ZUW Gout FA25 Discontinued in Phase 3 [13]
AD-5467 DMM02XV Diabetic complication 5A2Y Discontinued in Phase 2 [14]
Alrestatin DMIAXCZ N. A. N. A. Discontinued in Phase 2 [15]
CTL-102-GDEPT DM09CUO Head and neck cancer 2D42 Discontinued in Phase 2 [16]
JTT-811 DMJ1ZTB Diabetic complication 5A2Y Discontinued in Phase 2 [4]
ZOPOLRESTAT DMWOT92 Diabetic complication 5A2Y Discontinued in Phase 2 [17]
E-0722 DM2PVMZ Diabetic cataract 9B10.21 Terminated [19]
FR-62765 DMJS9YB Diabetic complication 5A2Y Terminated [20]
Sorbinil DM31VE4 Diabetic cataract 9B10.21 Terminated [21]
SPR-210 DMTGIUV Diabetic complication 5A2Y Terminated [22]
WF-2421 DMBMOI6 Diabetic complication 5A2Y Terminated [23]
Zenarestat DMQUSG9 Diabetic neuropathy 8C0Z Terminated [24]
⏷ Show the Full List of 14 Discontinued Drug(s)
1 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ARI-809 DM61TDB Diabetic complication 5A2Y Preclinical [18]
73 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(4-Methyl-2-oxo-2H-quinolin-1-yl)-acetic acid DMPU7KE Discovery agent N.A. Investigative [25]
(6-Hydroxy-2-oxo-2H-quinolin-1-yl)-acetic acid DMQJ5RU Discovery agent N.A. Investigative [25]
(6-Methoxy-2-oxo-2H-quinolin-1-yl)-acetic acid DMTYXFU Discovery agent N.A. Investigative [25]
(8-Hydroxy-2-oxo-2H-quinolin-1-yl)-acetic acid DMRU0IB Discovery agent N.A. Investigative [25]
2'-Monophosphoadenosine 5'-Diphosphoribose DME9S8M Discovery agent N.A. Investigative [15]
2,3-dihydroxypropanal DMOWNB4 Discovery agent N.A. Investigative [26]
2-(3,4-Dihydroxy-benzyl)-7-hydroxy-chromen-4-one DMAOD0K Discovery agent N.A. Investigative [27]
2-(3,4-Dihydroxy-phenyl)-7-hydroxy-chromen-4-one DM5MKEI Discovery agent N.A. Investigative [27]
2-(3-benzoyl-1H-pyrrol-1-yl)acetic acid DMDB4LZ Discovery agent N.A. Investigative [28]
2-(4-aminophenylsulfonamido)acetic acid DMMU2BZ Discovery agent N.A. Investigative [29]
2-(Phenylsulfonamido)acetic Acid DMMSI67 Discovery agent N.A. Investigative [30]
2-Benzhydryl-7-hydroxy-chromen-4-one DMXZ1HL Discovery agent N.A. Investigative [27]
2-Benzyl-7-hydroxy-chromen-4-one DMAX5TC Discovery agent N.A. Investigative [27]
3,5-dichlorosalicylic acid DMQ45WH Discovery agent N.A. Investigative [31]
3-(3-Benzoyl-1H-pyrrol-1-yl)propanoic acid DMXKL75 Discovery agent N.A. Investigative [28]
3-[5-(3-nitrophenyl)thiophen-2-yl]propanoic acid DM1QKNU Discovery agent N.A. Investigative [32]
4-(3-Benzoyl-1H-pyrrol-1-yl)butanoic acid DMT0EK8 Discovery agent N.A. Investigative [28]
4-(3-Methoxy-phenyl)-isoxazolidine-3,5-dione DMSUFJZ Discovery agent N.A. Investigative [33]
6,7-Dihydroxy-2-phenyl-chromen-4-one DMF08UT Discovery agent N.A. Investigative [27]
6-(1H-Indole-2-sulfonyl)-2H-pyridazin-3-one DM1TOFD Discovery agent N.A. Investigative [34]
6-(2-Bromo-benzenesulfonyl)-2H-pyridazin-3-one DMYDHLN Discovery agent N.A. Investigative [34]
6-(2-Chloro-benzenesulfonyl)-2H-pyridazin-3-one DM2Y9O4 Discovery agent N.A. Investigative [34]
6-(2-Fluoro-benzenesulfonyl)-2H-pyridazin-3-one DMQKR2W Discovery agent N.A. Investigative [34]
6-(3-Chloro-benzenesulfonyl)-2H-pyridazin-3-one DMJO4I7 Discovery agent N.A. Investigative [34]
6-(4-Bromo-benzenesulfonyl)-2H-pyridazin-3-one DM9K8DY Discovery agent N.A. Investigative [34]
6-(4-Chloro-benzenesulfonyl)-2H-pyridazin-3-one DMNAHVB Discovery agent N.A. Investigative [34]
6-(4-Fluoro-benzenesulfonyl)-2H-pyridazin-3-one DM7WYNT Discovery agent N.A. Investigative [34]
6-(4-Methoxy-benzenesulfonyl)-2H-pyridazin-3-one DM5LBCH Discovery agent N.A. Investigative [34]
6-(Benzofuran-2-sulfonyl)-2H-pyridazin-3-one DM2GFI3 Discovery agent N.A. Investigative [34]
6-(Benzothiazole-2-sulfonyl)-2H-pyridazin-3-one DMXLDHR Discovery agent N.A. Investigative [34]
6-(Biphenyl-2-sulfonyl)-2H-pyridazin-3-one DM4KMDB Discovery agent N.A. Investigative [34]
6-(Naphthalene-1-sulfonyl)-2H-pyridazin-3-one DMXSCQE Discovery agent N.A. Investigative [34]
6-(Naphthalene-2-sulfonyl)-2H-pyridazin-3-one DMCIA63 Discovery agent N.A. Investigative [34]
6-(Toluene-4-sulfonyl)-2H-pyridazin-3-one DMV3MF4 Discovery agent N.A. Investigative [34]
6-Benzenesulfonyl-2H-pyridazin-3-one DM81DTC Discovery agent N.A. Investigative [34]
6-Hydroxy-2-(4-hydroxy-benzyl)-chromen-4-one DMU1CGD Discovery agent N.A. Investigative [27]
6-methoxykaempferol 3-O-beta-D-robinobioside DM5JB9D Discovery agent N.A. Investigative [35]
6-Phenylmethanesulfonyl-2H-pyridazin-3-one DMPA534 Discovery agent N.A. Investigative [34]
7-Hydroxy-2-(4-hydroxy-benzyl)-chromen-4-one DMCB2IM Discovery agent N.A. Investigative [27]
7-Hydroxy-2-(4-methoxy-benzyl)-chromen-4-one DM2BV6P Discovery agent N.A. Investigative [27]
7-Hydroxy-4-phenylcoumarin DM3T612 Discovery agent N.A. Investigative [36]
7-Hydroxy-6-nitro-2-phenyl-chromen-4-one DM49RWY Discovery agent N.A. Investigative [27]
AK198 DMWKPJH Discovery agent N.A. Investigative [37]
Alpha-D-Glucose-6-Phosphate DMR0EVN Discovery agent N.A. Investigative [15]
APIGENIN DMI3491 Discovery agent N.A. Investigative [38]
Apigenin-7-O-beta-D-glucuronide DMIQOXH Discovery agent N.A. Investigative [38]
Apigenin-7-O-beta-D-glucuronide methyl ester DMP7J0I Discovery agent N.A. Investigative [38]
ASTRAGALIN DMZHWPG Discovery agent N.A. Investigative [38]
Chrysin DM7V2LG Discovery agent N.A. Investigative [39]
daidzein DMRFTJX Discovery agent N.A. Investigative [27]
EPALRESTATE DM01MW7 Discovery agent N.A. Investigative [38]
Fidarestat(Stereoisomer) DMETVLB Discovery agent N.A. Investigative [15]
Hydroxydimethylarsine Oxide DMPS2B1 Discovery agent N.A. Investigative [15]
IDD552 DM3P7W5 Discovery agent N.A. Investigative [15]
IDD594 DMDHLG3 Discovery agent N.A. Investigative [32]
Inhibitor Idd 384 DMBQY3C Discovery agent N.A. Investigative [15]
Isorhamnetin 3,7-disulfate DMFKQ0B Discovery agent N.A. Investigative [5]
Isorhamnetin 3-O-rhamnoside DMZQUY4 Discovery agent N.A. Investigative [40]
KAEMPFEROL DMHEMUB Discovery agent N.A. Investigative [38]
MANGIFERIN DMWAF5Z Discovery agent N.A. Investigative [41]
N-Acetylalanine DMZW9AC Discovery agent N.A. Investigative [15]
NSC-94258 DM6VY3P Discovery agent N.A. Investigative [27]
O5-Acetyl-O7-nitrooxyethyl chrysin DMKMH2X Discovery agent N.A. Investigative [39]
O7-Nitrooxyethyl chrysin DMAUDCW Discovery agent N.A. Investigative [39]
PALBINONE DMN97BF Discovery agent N.A. Investigative [42]
Patuletin 3-O-beta-D-galactoside DMOXNYQ Discovery agent N.A. Investigative [35]
Patuletin 3-O-beta-D-robinobioside DMZ5Q7J Discovery agent N.A. Investigative [35]
Quercetin 3-O-neohesperidoside DMXIU6W Discovery agent N.A. Investigative [40]
QUERCITRIN DM1DH96 Discovery agent N.A. Investigative [38]
Tamarixetin 3-glucoside-7-sulfate DM17JFO Discovery agent N.A. Investigative [5]
TINGENIN B DMEV7FY Discovery agent N.A. Investigative [41]
TINGENONE DMH3NTP Discovery agent N.A. Investigative [41]
TRIPTOCALLINE A DMBYV3M Discovery agent N.A. Investigative [41]
⏷ Show the Full List of 73 Investigative Drug(s)

References

1 Long-term effect of epalrestat, an aldose reductase inhibitor, on the development of incipient diabetic nephropathy in Type 2 diabetic patients. J Diabetes Complications. 2001 Sep-Oct;15(5):241-4.
2 Inhibition of human lens aldose reductase by flavonoids, sulindac and indomethacin. Biochem Pharmacol. 1983 Jul 1;32(13):1995-8.
3 Clinical efficacy of fidarestat, a novel aldose reductase inhibitor, for diabetic peripheral neuropathy: a 52-week multicenter placebo-controlled double-blind parallel group study. Diabetes Care. 2001 Oct;24(10):1776-82.
4 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: 2768).
5 Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes. J Nat Prod. 1996 Apr;59(4):443-5.
6 Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors ... J Med Chem. 2005 May 5;48(9):3141-52.
7 Effects of novel aldose reductase inhibitors, M16209 and M16287, on streptozotocin-induced diabetic neuropathy in rats. Eur J Pharmacol. 1991 Feb 7;193(2):185-91.
8 A multicenter, double-blind, safety study of QR-333 for the treatment of symptomatic diabetic peripheral neuropathy. A preliminary report. J Diabetes Complications. 2005 Sep-Oct;19(5):247-53.
9 Metabolism of the aldose reductase inhibitor ALO1567 in man. Br J Clin Pharmacol. 1991 Aug;32(2):221-7.
10 Aldose reductase inhibitors: an update. Ann Pharmacother. 1993 Jun;27(6):751-4.
11 Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors. J Med Chem. 1991 Nov;34(11):3229-34.
12 Minalrestat, an aldose reductase inhibitor, corrects the impaired microvascular reactivity in diabetes. J Pharmacol Exp Ther. 2003 Mar;304(3):1236-42.
13 Ponalrestat, an aldose reductase inhibitor, inhibits cachexia syndrome induced by colon26 adenocarcinoma in mice. Anticancer Res. 1999 Sep-Oct;19(5B):4105-11.
14 Studies on antidiabetic agents. IX. A new aldose reductase inhibitor, AD-5467, and related 1,4-benzoxazine and 1,4-benzothiazine derivatives: synthesis and biological activity. Chem Pharm Bull (Tokyo). 1990 May;38(5):1238-45.
15 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
16 Genes in the Service of Therapeutic Index: Progress for Virus-Directed Enzyme Prodrug Therapy. JCO May 1, 2004 vol. 22 no. 9 1535-1537c.
17 Comparison of the effects of Zopolrestat and Sorbinil on lens myo-inositol influx. Pharmacology. 1997 Feb;54(2):76-83.
18 A selective aldose reductase inhibitor of a new structural class prevents or reverses early retinal abnormalities in experimental diabetic retinopathy. Diabetes. 2006 Oct;55(10):2757-62.
19 Aldose reductase inhibitors and prevention of galactose cataracts in rats. Invest Ophthalmol Vis Sci. 1989 Jul;30(7):1623-32.
20 Studies on WF-3681, a novel aldose reductase inhibitor. IV. Effect of FR-62765, a derivative of WF-3681, on the diabetic neuropathy in rats. J Antibiot (Tokyo). 1991 Apr;44(4):441-4.
21 A controlled trial of sorbinil, an aldose reductase inhibitor, in chronic painful diabetic neuropathy. Diabetes. 1983 Oct;32(10):938-42.
22 Pharmacological profiles of a novel aldose reductase inhibitor, SPR-210, and its effects on streptozotocin-induced diabetic rats. Jpn J Pharmacol. 1994 Feb;64(2):115-24.
23 WF-2421, a new aldose reductase inhibitor produced from a fungus, Humicola grisea. J Antibiot (Tokyo). 1991 Feb;44(2):130-5.
24 The effects of zenarestat, an aldose reductase inhibitor, on minimal F-wave latency and nerve blood flow in streptozotocin-induced diabetic rats. Life Sci. 2001 Feb 9;68(12):1439-48.
25 Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives. J Med Chem. 1986 Oct;29(10):2024-8.
26 Structural basis for the high all-trans-retinaldehyde reductase activity of the tumor marker AKR1B10. Proc Natl Acad Sci U S A. 2007 Dec 26;104(52):20764-9.
27 1-Benzopyran-4-one antioxidants as aldose reductase inhibitors. J Med Chem. 1999 Jun 3;42(11):1881-93.
28 Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisoste... Bioorg Med Chem. 2010 Mar 15;18(6):2107-2114.
29 Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors. Bioorg Med Chem. 2008 Apr 1;16(7):3926-32.
30 A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activ... J Med Chem. 2010 Nov 11;53(21):7756-66.
31 Correlation of binding constants and molecular modelling of inhibitors in the active sites of aldose reductase and aldehyde reductase. Bioorg Med Chem. 2009 Feb 1;17(3):1244-50.
32 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
33 Isoxazolidine-3,5-diones as lens aldose reductase inhibitors. J Med Chem. 1982 Jun;25(6):745-7.
34 A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3... J Med Chem. 2005 Oct 6;48(20):6326-39.
35 Flavonoids with anti-cataract activity from Brickellia arguta. J Nat Prod. 1984 Mar-Apr;47(2):316-9.
36 6,7-Dihydroxy-4-phenylcoumarin as inhibitor of aldose reductase 2. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5630-3.
37 The Effect of Halogen-to-Hydrogen Bond Substitution on Human Aldose Reductase Inhibition. ACS Chem Biol. 2015 Jul 17;10(7):1637-42.
38 Erigeroflavanone, a flavanone derivative from the flowers of Erigeron annuus with protein glycation and aldose reductase inhibitory activity. J Nat Prod. 2008 Apr;71(4):713-5.
39 Synthesis, characterization and vasculoprotective effects of nitric oxide-donating derivatives of chrysin. Bioorg Med Chem. 2010 May 1;18(9):3020-5.
40 New flavonol oligoglycosides and polyacylated sucroses with inhibitory effects on aldose reductase and platelet aggregation from the flowers of Pru... J Nat Prod. 2002 Aug;65(8):1151-5.
41 Structures of new friedelane-type triterpenes and eudesmane-type sesquiterpene and aldose reductase inhibitors from Salacia chinensis. J Nat Prod. 2003 Sep;66(9):1191-6.
42 Inhibitors of aldose reductase and formation of advanced glycation end-products in moutan cortex (Paeonia suffruticosa). J Nat Prod. 2009 Aug;72(8):1465-70.
43 FDA Label of Brexanolone. The 2020 official website of the U.S. Food and Drug Administration.
44 In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016 Oct 25;258:153-8.