Details of Drug-Metabolizing Enzyme (DME)

General Information of Drug-Metabolizing Enzyme (DME) (ID: DEOG15F)

DME Name Steroid 5-alpha-reductase 1 (SRD5A1)
Synonyms Alpha-reductase steroid 1; 3-oxo-5-alpha-steroid 4-dehydrogenase 1; S5AR 1; SR type 1; SRD5A1
Gene Name SRD5A1
UniProt ID
S5A1_HUMAN
INTEDE ID
DME0204
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Gene ID
6715
EC Number EC: 1.3.1.22
Oxidoreductase
CH-CH donor oxidoreductase
NAD/NADP acceptor oxidoreductase
EC: 1.3.1.22
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MATATGVAEERLLAALAYLQCAVGCAVFARNRQTNSVYGRHALPSHRLRVPARAAWVVQE
LPSLALPLYQYASESAPRLRSAPNCILLAMFLVHYGHRCLIYPFLMRGGKPMPLLACTMA
IMFCTCNGYLQSRYLSHCAVYADDWVTDPRFLIGFGLWLTGMLINIHSDHILRNLRKPGD
TGYKIPRGGLFEYVTAANYFGEIMEWCGYALASWSVQGAAFAFFTFCFLSGRAKEHHEWY
LRKFEEYPKFRKIIIPFLF
Function This enzyme converts testosterone into 5-alpha-dihydrotestosterone and progesterone or corticosterone into their corresponding 5-alpha-3- oxosteroids.
KEGG Pathway
( )
Reactome Pathway
Androgen biosynthesis (R-HSA-193048 )

Molecular Interaction Atlas (MIA) of This DME

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DME
3 Approved Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Oxymetholone DMFXUT8 Aplastic anemia 3A70 Approved [9]
Testosterone cypionate DMC1TEV Testosterone deficiency 5A81.1 Approved [10]
Testosterone enanthate DMB6871 Testosterone deficiency 5A81.1 Approved [10]

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 3.49E-02 -2.65E-01 -5.44E-01
Alopecia ED70 Skin from scalp 8.62E-01 1.11E-01 3.06E-01
Alzheimer's disease 8A20 Entorhinal cortex 1.79E-09 -6.51E-01 -9.39E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 5.44E-01 1.82E-01 4.52E-01
Aortic stenosis BB70 Calcified aortic valve 1.23E-01 5.18E-01 9.47E-01
Apnea 7A40 Hyperplastic tonsil 3.94E-01 -1.27E-01 -3.02E-01
Arthropathy FA00-FA5Z Peripheral blood 8.86E-01 1.40E-01 5.09E-01
Asthma CA23 Nasal and bronchial airway 3.09E-04 1.12E-01 1.84E-01
Atopic dermatitis EA80 Skin 6.45E-02 5.12E-01 6.47E-01
Autism 6A02 Whole blood 1.47E-02 -2.03E-01 -7.10E-01
Autoimmune uveitis 9A96 Peripheral monocyte 1.78E-01 -3.47E-01 -7.95E-01
Autosomal dominant monocytopenia 4B04 Whole blood 7.75E-01 -1.60E-01 -3.42E-01
Bacterial infection of gingival 1C1H Gingival tissue 2.02E-08 -2.28E-01 -8.60E-01
Batten disease 5C56.1 Whole blood 6.69E-01 7.68E-02 3.80E-01
Behcet's disease 4A62 Peripheral blood 3.81E-01 -3.49E-02 -1.19E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 3.88E-01 -4.75E-02 -1.50E-01
Bladder cancer 2C94 Bladder tissue 8.92E-05 1.04E+00 2.59E+00
Breast cancer 2C60-2C6Z Breast tissue 2.48E-22 6.63E-01 5.73E-01
Cardioembolic stroke 8B11.20 Whole blood 3.28E-04 3.59E-01 1.33E+00
Cervical cancer 2C77 Cervical tissue 7.74E-05 -6.05E-01 -1.29E+00
Childhood onset rheumatic disease FA20.Z Peripheral blood 3.31E-01 8.30E-02 9.74E-02
Chronic hepatitis C 1E51.1 Whole blood 6.51E-01 -2.88E-01 -6.16E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 3.81E-01 8.43E-03 3.12E-02
Chronic obstructive pulmonary disease CA22 Small airway epithelium 7.28E-07 -4.36E-01 -9.78E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 4.34E-01 1.26E-01 5.26E-01
Colon cancer 2B90 Colon tissue 1.24E-53 6.30E-01 1.72E+00
Coronary artery disease BA80-BA8Z Peripheral blood 7.41E-01 5.40E-01 4.48E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 4.50E-02 -3.27E-01 -9.60E-01
Endometriosis GA10 Endometrium tissue 3.41E-01 -2.23E-01 -2.29E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 2.08E-01 -1.55E-01 -4.97E-01
Familial hypercholesterolemia 5C80.00 Whole blood 9.43E-16 1.13E+00 2.26E+00
Gastric cancer 2B72 Gastric tissue 1.42E-01 1.04E+00 8.99E-01
Glioblastopma 2A00.00 Nervous tissue 7.42E-36 -8.94E-01 -1.02E+00
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 8.69E-01 -7.78E-02 -4.08E-01
Glioma 2A00.0Y-2A00.0Z White matter tissue 2.86E-02 8.62E-01 1.03E+00
Head and neck cancer 2D42 Head and neck tissue 2.38E-04 3.42E-01 6.25E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 3.79E-01 -6.50E-01 -7.09E-01
Huntington's disease 8A01.10 Whole blood 7.88E-01 2.38E-02 6.64E-02
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 2.39E-02 2.77E-01 1.04E+00
Immunodeficiency 4A00-4A20 Peripheral blood 1.53E-04 1.58E-01 1.92E+00
Influenza 1E30 Whole blood 4.28E-03 -2.05E+00 -1.50E+01
Interstitial cystitis GC00.3 Bladder tissue 4.93E-01 -2.04E-01 -4.89E-01
Intracranial aneurysm 8B01.0 Intracranial artery 7.02E-03 2.26E-01 3.88E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 1.54E-02 -9.79E-02 -3.11E-01
Ischemic stroke 8B11 Peripheral blood 5.28E-01 -5.82E-02 -1.75E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 1.57E-03 2.63E-01 4.81E-01
Lateral sclerosis 8B60.4 Skin 4.99E-01 -3.03E-02 -1.90E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 8.47E-01 -3.16E-01 -2.64E-01
Liver cancer 2C12.0 Liver tissue 1.22E-12 -1.39E+00 -1.73E+00
Liver failure DB99.7-DB99.8 Liver tissue 5.54E-07 -1.91E+00 -4.11E+00
Lung cancer 2C25 Lung tissue 2.85E-152 1.49E+00 3.51E+00
Lupus erythematosus 4A40 Whole blood 5.39E-07 3.59E-01 6.83E-01
Major depressive disorder 6A70-6A7Z Hippocampus 3.94E-01 8.33E-02 2.82E-01
Major depressive disorder 6A70-6A7Z Whole blood 6.97E-01 1.92E-02 5.59E-02
Melanoma 2C30 Skin 2.59E-08 -1.61E+00 -1.75E+00
Multiple myeloma 2A83.1 Peripheral blood 8.11E-01 -3.27E-02 -7.79E-02
Multiple myeloma 2A83.1 Bone marrow 8.45E-22 1.40E+00 1.73E+01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 1.40E-01 -4.92E-01 -9.30E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 2.94E-02 2.00E-01 5.58E-01
Myelofibrosis 2A20.2 Whole blood 3.32E-01 1.24E-01 4.17E-01
Myocardial infarction BA41-BA50 Peripheral blood 3.87E-01 6.56E-03 1.09E-02
Myopathy 8C70.6 Muscle tissue 2.46E-01 1.29E-01 6.84E-01
Neonatal sepsis KA60 Whole blood 1.62E-05 2.25E-01 7.20E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 8.67E-07 1.80E+00 3.26E+00
Non-alcoholic fatty liver disease DB92 Liver tissue 5.55E-01 4.94E-02 9.78E-02
Obesity related type 2 diabetes 5A11 Omental adipose tissue 9.55E-01 3.18E-02 1.18E-01
Olive pollen allergy CA08.00 Peripheral blood 4.30E-01 8.17E-02 1.74E-01
Oral cancer 2B6E Oral tissue 2.42E-02 1.54E-01 1.14E-01
Osteoarthritis FA00-FA0Z Synovial tissue 1.11E-01 7.04E-01 6.87E-01
Osteoporosis FB83.1 Bone marrow 2.93E-02 -6.93E-01 -4.88E+00
Ovarian cancer 2C73 Ovarian tissue 3.46E-05 1.38E+00 2.55E+00
Pancreatic cancer 2C10 Pancreas 2.88E-05 8.04E-01 1.49E+00
Parkinson's disease 8A00.0 Substantia nigra tissue 2.10E-01 -7.49E-01 -8.57E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 4.23E-04 6.32E-01 1.29E+00
Pituitary cancer 2D12 Pituitary tissue 1.43E-03 9.58E-01 1.58E+00
Pituitary gonadotrope tumour 2D12 Pituitary tissue 1.14E-02 8.76E-01 1.45E+00
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 8.48E-01 -7.77E-02 -3.88E-01
Polycythemia vera 2A20.4 Whole blood 8.30E-04 1.36E-01 5.31E-01
Pompe disease 5C51.3 Biceps muscle 4.33E-01 1.12E-01 3.63E-01
Preterm birth KA21.4Z Myometrium 6.30E-01 -5.04E-02 -3.50E-01
Prostate cancer 2C82 Prostate 3.97E-06 9.35E-01 1.49E+00
Psoriasis EA90 Skin 5.19E-01 7.44E-02 1.16E-01
Rectal cancer 2B92 Rectal colon tissue 5.21E-03 5.70E-01 2.02E+00
Renal cancer 2C90-2C91 Kidney 1.16E-02 4.64E-01 7.86E-01
Retinoblastoma 2D02.2 Uvea 1.06E-06 9.19E-01 2.60E+00
Rheumatoid arthritis FA20 Synovial tissue 8.44E-03 4.56E-01 8.44E-01
Rhinovirus infection CA42.1 Nasal epithelium tissue 5.74E-01 5.22E-02 1.18E-01
Schizophrenia 6A20 Prefrontal cortex 9.59E-02 -5.00E-02 -7.61E-02
Schizophrenia 6A20 Superior temporal cortex 4.88E-01 5.25E-02 8.83E-02
Scleroderma 4A42.Z Whole blood 1.67E-09 8.27E-01 5.17E+00
Seizure 8A60-8A6Z Whole blood 7.61E-01 8.81E-02 2.74E-01
Sensitive skin EK0Z Skin 4.42E-01 4.28E-03 9.28E-03
Sepsis with septic shock 1G41 Whole blood 2.64E-01 -1.43E-02 -4.84E-02
Shwachman-Diamond syndrome 3A70.0 Bone marrow 6.72E-02 -4.08E-01 -1.35E+00
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 2.65E-02 -1.37E-01 -4.70E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 9.05E-01 2.20E-01 3.81E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 2.71E-01 1.01E-01 1.35E+00
Skin cancer 2C30-2C3Z Skin 1.61E-44 -1.04E+00 -1.33E+00
Thrombocythemia 3B63 Whole blood 1.94E-01 1.43E-01 5.24E-01
Thrombocytopenia 3B64 Whole blood 3.93E-01 -1.84E-01 -4.70E-01
Thyroid cancer 2D10 Thyroid 1.09E-18 3.08E-01 9.72E-01
Tibial muscular dystrophy 8C75 Muscle tissue 4.97E-04 4.48E-01 1.47E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 2.10E-01 -3.12E-01 -2.67E+00
Type 2 diabetes 5A11 Liver tissue 6.58E-01 -3.45E-01 -4.94E-01
Ureter cancer 2C92 Urothelium 6.43E-01 -1.10E-01 -2.91E-01
Uterine cancer 2C78 Endometrium tissue 2.86E-10 5.47E-01 5.23E-01
Vitiligo ED63.0 Skin 9.19E-01 5.82E-02 1.16E-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 Steroid 5-alpha-reductase 1 (SRD5A1) DTT Info
DME DTT Type Clinical trial
1 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
FR-146687 DMGO45I Prostate disease GA91 Phase 2 [1]
3 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
MK-386 DM48ELZ Acne vulgaris ED80 Discontinued in Phase 2 [2]
AS-601811 DMINF80 Acne vulgaris ED80 Discontinued in Phase 1 [3], [1]
Bexlosteride DMH7YD4 N. A. N. A. Terminated [2]
18 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(3-fluoro-4-(4-phenoxybenzoyl)phenyl)acetic acid DMPHM23 Discovery agent N.A. Investigative [4]
(3-methyl-4-(4-phenoxybenzoyl)phenyl)acetic acid DMX5CY3 Discovery agent N.A. Investigative [4]
(E)-3-(4-(4-phenoxybenzoyl)phenyl)acrylic acid DMOWGT3 Discovery agent N.A. Investigative [4]
1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one DM7BAU2 Discovery agent N.A. Investigative [5]
1-Methyl-5-(4-phenylazo-phenyl)-piperidin-2-one DM4HS92 Discovery agent N.A. Investigative [6]
1-Methyl-5-phenyl-piperidin-2-one DMB3JO2 Discovery agent N.A. Investigative [6]
2,3,5,6-Tetrafluoro-4-pentafluorophenylazo-phenol DMRVYKQ Discovery agent N.A. Investigative [7]
3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one DMKOE9I Discovery agent N.A. Investigative [5]
4,4'-dihydroxyoctafluoroazobenzene DM1ONBT Discovery agent N.A. Investigative [7]
4-(4-phenoxybenzoyl)benzoic acid DMOHB6U Discovery agent N.A. Investigative [4]
4-Methyl-5,6-dihydro-pyrido[1,2-a]quinolin-3-one DM7LPON Discovery agent N.A. Investigative [5]
4-[4-(benzhydryloxy)benzoyl]benzoic acid DM8MVE9 Discovery agent N.A. Investigative [4]
4-[4-benzyloxy)benzoyl]benzoic acid DMQ9IN4 Discovery agent N.A. Investigative [4]
5-(4-Chloro-phenyl)-1-methyl-piperidin-2-one DMJKAF0 Discovery agent N.A. Investigative [6]
5-(4-Chloro-phenyl)-1-methyl-piperidine-2-thione DMQB1UI Discovery agent N.A. Investigative [6]
GP515 DMRUIX3 Discovery agent N.A. Investigative [8]
LY-266111 DMX5H3T Discovery agent N.A. Investigative [6]
{4-[4-(4-bromophenoxy)benzoyl]phenyl}acetic acid DMX53OY Discovery agent N.A. Investigative [4]
⏷ Show the Full List of 18 Investigative Drug(s)

References

1 Pharmacokinetics and pharmacodynamics of TF-505, a novel nonsteroidal 5alpha-reductase inhibitor, in normal subjects treated with single or multiple doses. Br J Clin Pharmacol. 2002 Sep;54(3):283-94.
2 Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1. Bioorg Med Chem Lett. 2000 Feb 21;10(4):353-6.
3 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013228)
4 Novel 5alpha-reductase inhibitors: synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids. J Med Chem. 2006 Jan 26;49(2):748-59.
5 Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1. J Med Chem. 2000 Oct 5;43(20):3718-35.
6 Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1909-11.
7 Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. J Med Chem. 1990 Sep;33(9):2452-5.
8 19-nor-10-azasteroids: a novel class of inhibitors for human steroid 5alpha-reductases 1 and 2. J Med Chem. 1997 Mar 28;40(7):1112-29.
9 Androgen physiology. Semin Reprod Med. 2006 Apr;24(2):71-7.
10 Molecular analysis of the SRD5A1 and SRD5A2 genes in patients with benign prostatic hyperplasia with regard to metabolic parameters and selected hormone levels. Int J Environ Res Public Health. 2017 Oct 30;14(11).