Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTT02K8)

• DTT Name: Steroid 5-alpha-reductase 2 (SRD5A2)
• Synonyms: Type 2 steroid 5alpha-reductase (5alpha-R); SRD5A2; SR type 2; 5-alpha reductase 2; 5 alpha-SR2
• Gene Name: SRD5A2
• DTT Type: Successful target; [1]
• Related Disease: Prostate hyperplasia [ICD-11: GA90]
• BioChemical Class: CH-CH donor oxidoreductase
• UniProt ID: S5A2_HUMAN
• TTD ID: T71390
• EC Number: EC 1.3.1.22
• Sequence:
  MQVQCQQSPVLAGSATLVALGALALYVAKPSGYGKHTESLKPAATRLPARAAWFLQELPS
  FAVPAGILARQPLSLFGPPGTVLLGLFCVHYFHRTFVYSLLNRGRPYPAILILRGTAFCT
  GNGVLQGYYLIYCAEYPDGWYTDIRFSLGVFLFILGMGINIHSDYILRQLRKPGEISYRI
  PQGGLFTYVSGANFLGEIIEWIGYALATWSLPALAFAFFSLCFLGLRAFHHHRFYLKMFE
  DYPKSRKALIPFIF
• Function: Converts testosterone (T) into 5-alpha- dihydrotestosterone (DHT) and progesterone or corticosterone into their corresponding 5-alpha-3-oxosteroids. It plays a central role in sexual differentiation and androgen physiology.
• Reactome Pathway: Androgen biosynthesis (R-HSA-193048)
• BioCyc Pathway: MetaCyc:HS00619-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Finasteride	DMWV3TZ	Benign prostatic hyperplasia	GA90	Approved	[1]

15 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	[2]
(3-methyl-4-(4-phenoxybenzoyl)phenyl)acetic acid	DMX5CY3	Discovery agent	N.A.	Investigative	[2]
(E)-3-(4-(4-phenoxybenzoyl)phenyl)acrylic acid	DMOWGT3	Discovery agent	N.A.	Investigative	[2]
2,3,5,6-Tetrafluoro-4-pentafluorophenylazo-phenol	DMRVYKQ	Discovery agent	N.A.	Investigative	[3]
3-[4-(4-phenoxybenzoyl)phenyl]propanoic acid	DM75F1Q	Discovery agent	N.A.	Investigative	[2]
4,4'-dihydroxyoctafluoroazobenzene	DM1ONBT	Discovery agent	N.A.	Investigative	[3]
4-(4-phenoxybenzoyl)benzoic acid	DMOHB6U	Discovery agent	N.A.	Investigative	[2]
4-(4-phenoxybenzoyl)phenylacetic acid	DMQ0JWZ	Discovery agent	N.A.	Investigative	[2]
4-[3-(benzyloxy)benzoyl]benzoic acid	DMZU23D	Discovery agent	N.A.	Investigative	[2]
4-[4-(benzhydryloxy)benzoyl]benzoic acid	DM8MVE9	Discovery agent	N.A.	Investigative	[2]
4-[4-(benzoylamino)benzoyl]benzoic acid	DM9VPFL	Discovery agent	N.A.	Investigative	[2]
4-[4-(benzylamino)benzoyl]benzoic acid	DMQC5EH	Discovery agent	N.A.	Investigative	[2]
4-[4-benzyloxy)benzoyl]benzoic acid	DMQ9IN4	Discovery agent	N.A.	Investigative	[2]
GP515	DMRUIX3	Discovery agent	N.A.	Investigative	[4]
{4-[4-(4-bromophenoxy)benzoyl]phenyl}acetic acid	DMX53OY	Discovery agent	N.A.	Investigative	[2]

The Drug-Metabolizing Enzyme (DME) Role of This DTT

• DTT DME Name: Steroid 5-alpha-reductase 2 (SRD5A2) DME Info
• Gene Name: SRD5A2

2 Approved Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Testosterone cypionate	DMC1TEV	Testosterone deficiency	5A81.1	Approved	[5]
Testosterone enanthate	DMB6871	Testosterone deficiency	5A81.1	Approved	[5]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] 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.
• [3] Hydroxyperfluoroazobenzenes: novel inhibitors of enzymes of androgen biosynthesis. J Med Chem. 1990 Sep;33(9):2452-5.
• [4] 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.
• [5] 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).