Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01182

Target Information
Name3-oxo-5-alpha-steroid 4-dehydrogenase 1    
Type of targetResearch target    
Synonyms5-alpha reductase 1    
S5AR    
SR type 1    
Steroid 5-alpha-reductase 1    
DiseaseAcne
[ICD9: 706.1   ICD10: L70.0]
[1]
Alopecia, unspecified
[ICD9: 704.09   ICD10: L65.9]
[1]
Benign prostate hyperplasia
[ICD9: 600   ICD10: N40]
[1][2]
Hirsutism
[ICD9: 704.1   ICD10: L68.0]
[1]
Prostate cancer
[ICD9: 185   ICD10: C61]
[1]
BioChemical ClassOxidoreductases acting on the CH-CH group of donors    
EC NumberEC 1.3.99.5
PathwayAndrogen and estrogen metabolism
UniProt IDP18405
FunctionConverts 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.    
SequenceMATATGVAEERLLAALAYLQCAVGCAVFARNRQTNSVYGRHALPSHRLRVPARAAWVVQE LPSLALPLYQYASESAPRLRSAPNCILLAMFLVHYGHRCLIYPFLMRGGKPMPLLACTMA IMFCTCNGYLQSRYLSHCAVYADDWVTDPRFLIGFGLWLTGMLINIHSDHILRNLRKPGD TGYKIPRGGLFEYVTAANYFGEIMEWCGYALASWSVQGAAFAFFTFCFLSGRAKEHHEWY LRKFEEYPKFRKIIIPFLF
Related US Patent6,552,034
6,555,549
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3-fluoro-4-[3]
(3-methyl-4-[3]
(E)-3-[3]
1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one[4]
1-Methyl-5- (4-phenylazo-phenyl)-piperidin-2-one[5]
1-Methyl-5-phenyl-piperidin-2-one[5]
19-nor-10-azasteroid skeleton[6]
2,3,5,6-Tetrafluoro-4-pentafluorophenylazo-phenol[7]
3,4,5,6-Tetrahydrobenzo[c]quinolizin-3- (4aH)-one[4]
4,4'-dihydroxyoctafluoroazobenzene[7]
4- (4-phenoxybenzoyl)benzoic acid[3]
4-Methyl-5,6-dihydro-pyrido[1,2-a]quinolin-3-one[4]
4-[4- (benzhydryloxy)benzoyl]benzoic acid[3]
4-[4-benzyloxy)benzoyl]benzoic acid[3]
5- (4-Chloro-phenyl)-1-methyl-piperidin-2-one[5]
5- (4-Chloro-phenyl)-1-methyl-piperidine-2-thione[5]
Bexlosteride,   LY-191704[8]
FK-143[9]
LY-266111[5]
MK-386[8]
ONO-3805[9]
{4-[4- (4-bromophenoxy)benzoyl]phenyl}acetic acid[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Clinical application of 5alpha-reductase inhibitors. J Endocrinol Invest. 2001 Mar;24(3):199-203. To Reference
Ref 2C16 and C17 substituted derivatives of pregnenolone and progesterone as inhibitors of 17alpha-hydroxylase-C17, 20-lyase: synthesis and biological evaluation. Arch Pharm (Weinheim). 2002;335(11-12):526-34. To Reference
Ref 3J Med Chem. 2006 Jan 26;49(2):748-59.Novel 5alpha-reductase inhibitors: synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids. To Reference
Ref 4J 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. To Reference
Ref 5Bioorg Med Chem Lett. 2000 Sep 4;10(17):1909-11.Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase. To Reference
Ref 619-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. To Reference
Ref 7J Med Chem. 1990 Sep;33(9):2452-5.Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. To Reference
Ref 8Bioorg 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. To Reference
Ref 9Bioorg Med Chem Lett. 1999 Jun 7;9(11):1553-8.Dual-acting agents with alpha1-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory activities. Synthesis and evaluation of arylpiperazine derivatives. To Reference



 

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