Target Information

Target General Infomation
Target ID
T70309
Former ID
TTDR01182
Target Name
3-oxo-5-alpha-steroid 4-dehydrogenase 1
Gene Name
SRD5A1
Synonyms
5-alpha reductase 1; S5AR; SR type 1; Steroid 5-alpha-reductase 1; SRD5A1
Target Type
Clinical Trial
Disease Acne vulgaris [ICD9: 706.1; ICD10: L70.0]
Prostate disease [ICD10: N42.9]
Function
Converts testosterone into 5-alpha-dihydrotestosterone and progesterone or corticosterone into their corresponding 5- alpha-3-oxosteroids. It plays a central role in sexual differentiation and androgen physiology.
BioChemical Class
Oxidoreductases acting on CH-CH group of donors
Target Validation
T70309
UniProt ID
P18405
EC Number
EC 1.3.1.22
Sequence
MATATGVAEERLLAALAYLQCAVGCAVFARNRQTNSVYGRHALPSHRLRVPARAAWVVQE
LPSLALPLYQYASESAPRLRSAPNCILLAMFLVHYGHRCLIYPFLMRGGKPMPLLACTMA
IMFCTCNGYLQSRYLSHCAVYADDWVTDPRFLIGFGLWLTGMLINIHSDHILRNLRKPGD
TGYKIPRGGLFEYVTAANYFGEIMEWCGYALASWSVQGAAFAFFTFCFLSGRAKEHHEWY
LRKFEEYPKFRKIIIPFLF
Drugs and Mode of Action
Drug(s) FR-146687 Drug Info Phase 2 Prostate disease [526428]
MK-386 Drug Info Discontinued in Phase 2 Acne vulgaris [546066]
AS-601811 Drug Info Discontinued in Phase 1 Acne vulgaris [547124]
Bexlosteride Drug Info Terminated Discovery agent [546722]
Inhibitor (3-fluoro-4-(4-phenoxybenzoyl)phenyl)acetic acid Drug Info [527979]
(3-methyl-4-(4-phenoxybenzoyl)phenyl)acetic acid Drug Info [527979]
(E)-3-(4-(4-phenoxybenzoyl)phenyl)acrylic acid Drug Info [527979]
1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one Drug Info [525881]
1-Methyl-5-(4-phenylazo-phenyl)-piperidin-2-one Drug Info [525866]
1-Methyl-5-phenyl-piperidin-2-one Drug Info [525866]
19-nor-10-azasteroid skeleton Drug Info [538023]
2,3,5,6-Tetrafluoro-4-pentafluorophenylazo-phenol Drug Info [532449]
3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one Drug Info [525881]
4,4'-dihydroxyoctafluoroazobenzene Drug Info [532449]
4-(4-phenoxybenzoyl)benzoic acid Drug Info [527979]
4-Methyl-5,6-dihydro-pyrido[1,2-a]quinolin-3-one Drug Info [525881]
4-[4-(benzhydryloxy)benzoyl]benzoic acid Drug Info [527979]
4-[4-benzyloxy)benzoyl]benzoic acid Drug Info [527979]
5-(4-Chloro-phenyl)-1-methyl-piperidin-2-one Drug Info [525866]
5-(4-Chloro-phenyl)-1-methyl-piperidine-2-thione Drug Info [525866]
AS-601811 Drug Info [526428], [547125]
Bexlosteride Drug Info [525719]
FR-146687 Drug Info [526428]
LY-266111 Drug Info [525866]
MK-386 Drug Info [525719]
{4-[4-(4-bromophenoxy)benzoyl]phenyl}acetic acid Drug Info [527979]
Pathways
BioCyc Pathway Superpathway of steroid hormone biosynthesis
Allopregnanolone biosynthesis
Androgen biosynthesis
KEGG Pathway Steroid hormone biosynthesis
NetPath Pathway IL2 Signaling Pathway
PathWhiz Pathway Androgen and Estrogen Metabolism
Reactome Androgen biosynthesis
References
Ref 526428Pharmacokinetics 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.
Ref 546066Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006173)
Ref 546722Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009929)
Ref 547124Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013228)
Ref 525719Bioorg Med Chem Lett. 2000 Feb 21;10(4):353-6.Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1.
Ref 525866Bioorg Med Chem Lett. 2000 Sep 4;10(17):1909-11.Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase.
Ref 525881J Med Chem. 2000 Oct 5;43(20):3718-35.Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1.
Ref 526428Pharmacokinetics 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.
Ref 527979J Med Chem. 2006 Jan 26;49(2):748-59.Novel 5alpha-reductase inhibitors: synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids.
Ref 532449J Med Chem. 1990 Sep;33(9):2452-5.Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis.
Ref 53802319-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.
Ref 547125Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013228)
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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