Information on EC 1.3.1.22 - 3-oxo-5alpha-steroid 4-dehydrogenase (NADP+) and Organism(s) Homo sapiens and UniProt Accession P18405

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Homo sapiens
UNIPROT: P18405


The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
1.3.1.22
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RECOMMENDED NAME
GeneOntology No.
3-oxo-5alpha-steroid 4-dehydrogenase (NADP+)
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
a 3-oxo-5alpha-steroid + NADP+ = a 3-oxo-DELTA4-steroid + NADPH + H+
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
oxidation
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redox reaction
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reduction
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PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
allopregnanolone biosynthesis
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androgen biosynthesis
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cardenolide biosynthesis
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Steroid hormone biosynthesis
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Brassinosteroid biosynthesis
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Metabolic pathways
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Biosynthesis of secondary metabolites
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SYSTEMATIC NAME
IUBMB Comments
3-oxo-5alpha-steroid:NADP+ DELTA4-oxidoreductase
The enzyme catalyses the conversion of assorted 3-oxo-Delta4 steroids into their corresponding 5alpha form. Substrates for the mammalian enzyme include testosterone, progesterone, and corticosterone. Substrates for the plant enzyme are brassinosteroids such as campest-4-en-3-one and (22alpha)-hydroxy-campest-4-en-3-one. cf. EC 1.3.99.5, 3-oxo-5alpha-steroid 4-dehydrogenase (acceptor).
CAS REGISTRY NUMBER
COMMENTARY hide
37255-34-8
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72412-84-1
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9029-09-8
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
isoform steroid 5-alpha-reductase 1
UniProt
Manually annotated by BRENDA team
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
20-alpha-hydroxypregn-4-ene-3one + NADPH
20-alpha-hydroxy-5alpha-pregnan-3-one + NADP+
show the reaction diagram
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androstenedione + NADPH + H+
5alpha-androstan-3,17-dione + NADP+
show the reaction diagram
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cholest-4-en-3-one + NADPH
5-alpha-cholestan-3-one + NADP+
show the reaction diagram
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deoxycorticosterone + NADPH
21-hydroxy-5alpha-pregnan-3,20-dione
show the reaction diagram
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-
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progesterone + NADPH
5alpha-pregnan-3,20-dione + NADP+
show the reaction diagram
progesterone + NADPH
5alpha-pregnan-3-20-dione + NADP+
show the reaction diagram
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-
-
-
?
testosterone + NADPH
17beta-hydroxy-5alpha-androstan-3-one + NADP+
show the reaction diagram
testosterone + NADPH
5alpha-dihydrotestosterone + NADP+
show the reaction diagram
testosterone + NADPH
5alpha-dihydrotestosterone + NADP+ + H+
show the reaction diagram
testosterone + NADPH + H+
5alpha-dihydrotestosterone + NADP+
show the reaction diagram
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?
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
testosterone + NADPH
5alpha-dihydrotestosterone + NADP+
show the reaction diagram
testosterone + NADPH + H+
5alpha-dihydrotestosterone + NADP+
show the reaction diagram
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?
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
17a-(2-propionoxyethyl)-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.01 mM, 8.5% inhibition
17a-allyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.01 mM, 0.4% inhibition
17a-ethyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.01 mM, 32.3% inhibition
17a-methyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.01 mM, 18.9% inhibition
(+/-)-LY191704
-
i.e. (4aS,10aR)-7-chloro-1-methyl-3,4,4a,9,10,10a-hexahydrophenanthren-2(1H)-one, non-steroidal, most potent benzoquinoline mimicing 4-azasteroid inhibitors, and specific for isozyme 5alphaR-1, IC50 is 30 nM
(10bR)-8-chloro-4,10b-dimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one
-
isoform II, 49% inhibition at 0.02 mM
(10bR)-8-chloro-4,5,10b-trimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one
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isoform II, 57% inhibition at 0.029 mM
(10bR)-8-chloro-5,10b-dimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one
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isoform II, 42% inhibition at 0.03 mM
(1E,4E,6E)-1,7-bis(3-hydroxy-4-methoxyphenyl)hepta-1,4,6-trien-3-one
-
-
(1E,4E,6E)-1,7-bis(3-hydroxyphenyl)hepta-1,4,6-trien-3-one
-
-
(1E,4E,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,4,6-trien-3-one
-
-
(1E,4E,6E)-1,7-bis(4-hydroxyphenyl)hepta-1,4,6-trien-3-one
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-
(1E,4E,6E)-1,7-diphenylhepta-1,4,6-trien-3-one
-
-
(1E,4E,6E)-1-(2-chlorophenyl)-7-phenylhepta-1,4,6-trien-3-one
-
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(1E,4E,6E)-1-(3-hydroxy-4-methoxyphenyl)-7-(3-hydroxyphenyl)hepta-1,4,6-trien-3-one
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(1E,4E,6E)-1-(3-nitrophenyl)-7-phenylhepta-1,4,6-trien-3-one
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(1E,4E,6E)-1-(4-hydroxy-3-methoxyphenyl)-7-(3-hydroxyphenyl)hepta-1,4,6-trien-3-one
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(1E,4E,6E)-1-(4-methoxyphenyl)-7-phenylhepta-1,4,6-trien-3-one
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(1E,4E,6E)-7-(3-hydroxyphenyl)-1-(4-hydroxyphenyl)hepta-1,4,6-trien-3-one
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(1E,4E,6E)-7-[3-(cycloprop-2-en-1-yloxy)phenyl]-1-(2-hydroxyphenyl)hepta-1,4,6-trien-3-one
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(1E,6E)-1,7-bis(3,4-dihydroxyphenyl)hepta-1,6-diene-3,5-dione
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(2E)-3-(4-hydroxy-3-methoxycyclohexa-1,5-dien-1-yl)-N-[2-(4-hydroxy-3-methoxyphenyl)ethyl]prop-2-enamide
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(2E)-3-(4-hydroxy-3-methoxycyclohexa-1,5-dien-1-yl)-N-[2-(4-hydroxyphenyl)ethyl]prop-2-enamide
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(2E)-3-(4-hydroxy-3-methoxycyclohexa-1,5-dien-1-yl)-N-[2-(4-methoxyphenyl)ethyl]prop-2-enamide
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(4aS)-7-chloro-4a-methyl-2,3,4,4a-tetrahydrophenanthrene-2-carboxylic acid
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(4aS,10bS)-4,10b-dimethyl-8-[(E)-2-naphthylylvinyl]-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 6 nM, isoform II, 50% inhibition at 0.00134 mM
(4aS,10bS)-4,10b-dimethyl-8-[(E)-2-phenylvinyl]-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 6 nM, isoform II, 50% inhibition at 0.0014 mM
(4aS,10bS)-4,8-dimethyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 11 nM
(4aS,10bS)-8-(2-furyl)-4,10b-dimethyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 59 nM, isoform II, 50% inhibition above 10 nM
(4aS,10bS)-8-bromo-4-methyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 35 nM
(4aS,10bS)-8-chloro-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 60 nM
(4aS,10bS)-8-chloro-4,10b-dimethyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 17 nM
(4aS,10bS)-8-chloro-4-methyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 8 nM, isoform II, 50% inhibition above 0.01 mM
(4aS,10bS)-8-fluoro-4-methyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 35 nM
(4aS,10bS)-8-methoxy-4-methyl-1,4,4a,5,6,10b-hexahydrobenzo[f]quinolin-3(2H)-one
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isoform I, 50% inhibition at 120 nM
(4E,6E)-1-(4-hydroxyphenyl)-7-phenylhepta-4,6-dien-3-one
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(4R)-4,8-dimethyl-4,4a,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
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isoform I, 50% inhibition at 312 nM
(4R)-8-chloro-4-methyl-4,4a,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
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isoform I, 50% inhibition at 141 nM
(4S)-4,8-dimethyl-4,4a,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
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isoform I, 50% inhibition at 137 nM
(6E)-1-(4-hydroxyphenyl)-7-phenylhept-6-en-3-one
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(6R)-8-chloro-6-methyl-4,4a,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
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isoform I, 50% inhibition at 188 nM
1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
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isoform I, 50% inhibition at 298 nM
1-methyl-5-(4-(2-phenylacetyl)phenyl)pyridin-2(1H)-one
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61% inhibition of type 1 steroid 5alpha reductase at 0.01 mM
10-azasteroids
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several
17-diisopropylcarbamoyl-2-androsten-3-carboxylate
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17-diisopropylcarbamoyl-3,5-androstadien-3-carboxylate
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17-diisopropylcarbamoyl-3-androsten-3-carboxyate
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17-diisopropylcarbamoyl-androstan-3-carboxylate
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17-tert-butylcarbamoyl-3,5-androstadien-3-carbaldehyde
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17-tert-butylcarbamoyl-3,5-androstadien-3-carboxylate
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dead-end inhibition versus testosterone
17-tert-butylcarbamoyl-3,5-androstadien-3-ol
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17a-(2-propionoxyethyl)-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.01 mM, 100% inhibition
17a-allyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.01 mM, 99% inhibition
17a-ethyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.01 mM, 100% inhibition
17a-methyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.01 mM, 99% inhibition
17alpha-p-bromophenylcarbamoyloxy-4-pregnen-3 20-dione
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17alpha-p-bromophenylcarbamoyloxy-4-pregnen-3,20-dione
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17alpha-phenylcarbamoyloxy-4-pregnen-3,20-dione
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17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
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17beta-Carbamoyl-1,3,5(10)-estratriene-3-carboxylic acids
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formation of enzyme-NADP+-inhibitor complex
17beta[3-(N-4-bromophenyl)tetrahydrooxazin-2-on-6-yl]androst-4-en-3-one
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17beta[3-(N-4-chlorophenyl)tetrahydrooxazin-2-on-6-yl]androst-4-en-3-one
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17beta[3-(N-4-ethoxyphenyl)tetrahydrooxazin-2-on-6-yl]androst-4-en-3-one
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17beta[3-(N-4-ethylphenyl)tetrahydrooxazin-2-on-6-yl]androst-4-en-3-one
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17beta[3-(N-4-methoxyphenyl)tetrahydrooxazin-2-on-6-yl]androst-4-en-3-one
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17beta[3-(N-4-phenyl)tetrahydrooxazin-2-on-6-yl]androst-4-en-3-one
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17beta[3-(N-4-tolyl)tetrahydrooxazin-2-on-6-yl]androst-4-en-3-one
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slight inhibition
2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
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2-(16-(acetylthio)hexadecanamido)ethyl 6-(2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamido)hex-4-enoate
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43% inhibition of type 1 steroid 5alpha reductase at 0.01 mM
2-(2-(16-(acetylthio)hexadecanamido)ethoxy)ethyl 6-(2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamido)hex-4-enoate
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33% inhibition of type 1 steroid 5alpha reductase at 0.01 mM
2-hydroxy-4-[(4E,6E)-3-oxo-7-phenylhepta-4,6-dien-1-yl]phenyl acetate
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2-methoxy-5-[(6E)-3-methoxy-7-phenylhept-6-en-1-yl]benzene-1,4-diol
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3-Androstene-3-carboxylic acids
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3beta-(3'-oxapentanoyloxy)-androst-5-en-17-one
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good in vitro inhibitory activity, but compound does not bind to the androgen receptors
3beta-acetoxyandrost-5-en-17-one
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good in vitro inhibitory activity, but compound does not bind to the androgen receptors
3beta-hexanoyloxyandrost-5-en-17-one
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good in vitro inhibitory activity, but compound does not bind to the androgen receptors
4,6,8-trimethyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
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isoform I, 50% inhibition at 15.8 nM
4,8-dimethyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
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isoform I, 50% inhibition at 20 nM
4-(1-[4-[acetyl(methyl)amino]-3-methylphenyl]-1-ethylpropyl)-2-methylphenyl diethylcarbamate
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22% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]-3-methylphenyl]-1-ethylpropyl)phenyl diethylcarbamate
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25% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)-2-methylphenyl diethylcarbamate
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56% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl 4-methylpiperazine-1-carboxylate
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17% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl azepane-1-carboxylate
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70% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl azocane-1-carboxylate
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20% inhibition at 0.001 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl bis(1-methylethyl)carbamate
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72% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl bis(1-methylpropyl)carbamate
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22% inhibition at 0.001 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl dibenzylcarbamate
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51% inhibition at 0.001 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl dibutylcarbamate
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32% inhibition at 0.001 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl diethylcarbamate
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57% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl dimethylcarbamate
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29% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl dipropylcarbamate
-
77% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl morpholine-4-carboxylate
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15% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl piperidine-1-carboxylate
-
68% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-ethylpropyl)phenyl pyrrolidine-1-carboxylate
-
57% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-methylethyl)phenyl diethylcarbamate
-
16% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]-1-propylbutyl)phenyl diethylcarbamate
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27% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]cyclobutyl)phenyl diethylcarbamate
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16% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]cycloheptyl)phenyl diethylcarbamate
-
25% inhibition at 0.01 mM; 46% inhibition at 0.01 mM
4-(1-[4-[acetyl(methyl)amino]phenyl]cyclopentyl)phenyl diethylcarbamate
-
5% inhibition at 0.01 mM
4-(2-[5-[(diphenylmethyl)carbamoyl]-1-benzofuran-2-yl]phenoxy)butanoic acid
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isoform I, 50% inhibition at 310 nM, isoform II, 50% inhibition above 0.1 mM
4-(2-[6-[(diphenylmethyl)carbamoyl]-1-benzofuran-2-yl]phenoxy)butanoic acid
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isoform I, 50% inhibition at 62 nM, isoform II, 50% inhibition at 270 nM
4-(3-(4-(N-methylacetamido)phenyl)pentan-3-yl)phenyl dibenzylcarbamate
-
competitive inhibitor
4-(4'-formylphenoxy)benzoic acid
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.007 mM
4-(biphenyl-4'-yloxy)phenylacetic acid
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.00006 mM
4-(biphenyl-4'-yloxy)phenylformic acid
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.000006 mM
4-(N-(diphenyl)acetyl-4-piperidinyloxy)benzoic acid
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.0013 mM
4-(N-(diphenyl)carbamoyl-4-piperidinyloxy)benzoic acid
-
pH 5.5, 37C, DU145 cells, 10% inhibition at 0.01 mM, BPH tissue, 68% inhibition at 0.01 mM
4-(N-(tert-butyloxycarbonyl)-4-piperidinyloxy)benzoic acid
-
pH 5.5, 37C, DU145 cells, 2% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.0078 mM
4-(N-adamantanoyl-4-piperidinyloxy)benzoic acid
-
pH 5.5, 37C, DU145 cells, 7% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00043 mM
4-Androsten-3-one-17beta-carboxylic acid
-
competitive
4-azasteroids
4-carboxy-4'-(N,N-dicyclohexyl)-aminobiphenyl
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.0047 mM, DU145 cells, 44% inhibition at 0.001 mM
4-carboxy-4'-(N,N-diisobutyl)-aminobiphenyl
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.004 mM, DU145 cells, 16% inhibition at 0.001 mM
4-carboxy-4'-(N,N-diisopropyl)-aminobiphenyl
-
pH 5.5, 37C, BPH tissue, 15% inhibition at 0.001 mM, DU145 cells, 9% inhibition at 0.001 mM
4-carboxy-4'-(N,N-diphenyl)-aminobiphenyl
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.00233 mM, DU145 cells, 28% inhibition at 0.001 mM
4-carboxy-4'-(N-adamantyl)-aminobiphenyl
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.0019 mM, DU145 cells, 16% inhibition at 0.001 mM
4-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 185 nM
4-methyl-4-azasteroids
-
4-methyl-5,6-dihydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 1400 nM
4-methyl-azasteroid
-
-
4-[(6E)-3-oxo-7-phenylhept-6-en-1-yl]phenyl acetate
-
-
4-[1-[4-(acetylamino)-3-methylphenyl]-1-ethylpropyl]-2-methylphenyl diethylcarbamate
-
17% inhibition at 0.01 mM
4-[2-(6-[[bis(4-fluorophenyl)methyl]carbamoyl]-1-benzofuran-2-yl)phenoxy]butanoic acid
-
isoform I, 50% inhibition at 50 nM, isoform II, 50% inhibition at 340 nM
4-[2-(6-[[bis(4-methoxyphenyl)methyl]amino]-1-benzofuran-2-yl)phenoxy]butanoic acid
-
isoform I, 50% inhibition at 42 nM, isoform II, 50% inhibition at 480 nM
4-[2-(6-[[bis(4-methoxyphenyl)methyl]carbamoyl]-1-benzofuran-2-yl)phenoxy]butanoic acid
-
isoform I, 50% inhibition at 130 nM, isoform II, 50% inhibition at 930 nM
4-[3-[(2,2-diphenyl-1,3-benzodioxol-5-yl)oxy]-2-methyl-1H-indol-1-yl]butanoic acid
-
isoform I, 50% inhibition at 10 nM, isoform II, 50% inhibition at 6300 nM
6,8-dimethyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 14.3 nM
6-azasteroids
-
several
7-bromo-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
-
-
7-chloro-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
-
-
8-bromo-4-methyl-1,4,5,6-tetrahydrobenzo[f]quinolin-3(2H)-one
-
50% inhibition at 60 nM, isoform I
8-chloro-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 49 nM
8-chloro-1,4,5,6-tetrahydrobenzo[f]quinolin-3(2H)-one
-
50% inhibition at 460 nM, isoform I
8-chloro-1-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 204 nM
8-chloro-4,4a,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 459 nM
8-chloro-4,5-dimethyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 15.6 nM
8-chloro-4,6-dimethyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 8.5 nM
8-chloro-4-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 7.6 nM
8-chloro-4-methyl-1,4,5,6-tetrahydrobenzo[f]quinolin-3(2H)-one
-
50% inhibition at 30 nM, isoform I
8-chloro-5-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 346 nM
8-chloro-6-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 14.4 nM
8-fluoro-1,4,5,6-tetrahydrobenzo[f]quinolin-3(2H)-one
-
50% inhibition at 600 nM, isoform I
8-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 376 nM
8-methyl-4,4a,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I, 50% inhibition at 176 nM
acrylate episteride
-
-
-
alpha-4-azasteroids
-
substitution of finasteride N-group by 6-azasteroids increased the rate of inhibition of type-1 5-alpha-reductases
benzoquilizin-3-ones
-
diverse, mimics of 10-azasteroids, overview, structure-activity relationships
benzoquinolines
-
compounds as mimics of 4-azasteroid inhibitors, diverse, overview, compounds derived from 6-azasteroids, overview
bisdemethoxycurcumin
-
22.2% inhibition at 0.3 mM
curcumin
-
complete inhibition at 0.3 mM
dehydroepiandrosterone
-
good in vitro inhibitory activity, but compound does not bind to the androgen receptors
demethoxycurcumin
-
complete inhibition at 0.3 mM
deoxycorticosterone acetate
-
competitive
docosanol
-
isoform 1, 50% inhibition above 0.1 mM, isoform 2, 50% inhibition above 0.1 mM
dutasteride
epristeride
-
-
estradiol
-
in female genital skin fibroblasts
estradiol-17beta
-
-
finasteride
FK143
-
i.e. 4-[3-(3-[[bis-(4-isobutyl-phenyl)-methyl]amino]-benzoyl)-indol-1-yl]-butyric acid, a non-steroidal bi-substrate inhibitor
lauric acid
-
isoform 1, 50% inhibition at 0.0167 mM, isoform 2, 50% inhibition at 0.0186 mM
lauric acid ethyl ester
-
isoform 1, 50% inhibition above 0.1 mM, isoform 2, 50% inhibition above 0.1 mM
linoleic acid
-
isoform 1, 50% inhibition at 0.013 mM, isoform 2, 50% inhibition at 0.035 mM
LY306089
-
a non steroid, non-competitive inhibitor of type I 5alpha-reductase in DU145 cells
MK386
myristic acid
-
isoform 2, 50% inhibition at 0.004 mM
N,N-bis(1-methylethyl)-4-(1-methyl-2-oxo-1,2-dihydroquinolin-6-yl)benzamide
-
isoform I, 50% inhibition at 510 nM, isoform II, 9% inhibition at 0.01 mM
N,N-dicyclohexyl-4-(4'-carboxyphenoxy)benzamide
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.0067 mM, DU145 cells, 4% inhibition at 0.001 mM
N,N-diisobutyl-4-(4'-carboxyphenoxy)benzamide
-
pH 5.5, 37C, BPH tissue, 46% inhibition at 0.01 mM
N,N-diisopropyl-2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamide
-
8% inhibition of type 1 steroid 5alpha reductase at 0.01 mM
N,N-diisopropyl-2-(4-(1-methyl-6-oxopiperidin-3-yl)phenoxy)acetamide
-
6% inhibition of type 1 steroid 5alpha reductase at 0.01 mM
N,N-diisopropyl-2-(4-(2-methyl-4-oxo-3,4-dihydropyridin-1(2H)-yl)phenoxy)acetamide
-
3% inhibition of type 1 steroid 5alpha reductase at 0.01 mM
N,N-diisopropyl-4-(4'-carboxyphenoxy)benzamide
-
pH 5.5, 37C, BPH tissue, 36% inhibition at 0.01 mM, DU145 cells, 4% inhibition at 0.001 mM
N,N-diphenyl-4-(4'-carboxyphenoxy)benzamide
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.00085 mM
N-(1-adamantanoyl)piperdine-4-(2-methoxybenzyliden-4-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 10% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.0012 mM
N-(1-adamantanoyl)piperidine-4-(2-fluorobenzylidene-4-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 20% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00021 mM
N-(3,3-diphenyl)propanoylpiperidine-4-(benzylidene-4-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 8% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.0011 mM
N-(dicyclohexyl)acetylpiperidine-4-(2-fluorobenzylidene-4-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 12% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.000011 mM
N-(dicyclohexyl)acetylpiperidine-4-(2-methoxybenzylidene-4-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 5% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00013 mM
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-3-carboxylic acid)
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.0007mM
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-4-acetic acid)
-
pH 5.5, 37C, DU145 cells, 6% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.000006 mM
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-4-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 46% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00006 mM
N-(diphenyl)acetylpiperidine-4-(2-fluorobenzylidene-4-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 2% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00041 mM
N-(diphenyl)acetylpiperidine-4-(2-methoxybenzylidene-4-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 8% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.0035 mM
N-(diphenyl)acetylpiperidine-4-(benzylidene-3-carboxylic acid)
-
pH 5.5, 37C, DU145 cells, 6% inhibition at 0.01 mM, BPH tissue, 57% inhibition at 0.01 mM
N-(diphenyl)acetylpiperidine-4-(benzylidene-4-acetic acid)
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.000075 mM
N-adamantyl-4-(4'-carboxyphenoxy)benzamide
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.00038 mM
N-allyl-2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamide
-
6% inhibition of type 1 steroid 5alpha reductase at 0.01 mM
N-allyl-2-(4-(2-methyl-4-oxo-3,4-dihydropyridin-1(2H)-yl)phenoxy)acetamide
-
8% inhibition of type 1 steroid 5alpha reductase at 0.01 mM and 12% inhibition of type 2 steroid 5alpha reductase at 0.01 mM
N-cyclohexyl-4-(4'-carboxyphenoxy)benzamide
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.0023 mM
N-phenyl-4-(4'-carboxyphenoxy)benzamide
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.001 mM
N-tert-butyl-4-(4'-carboxyphenoxy)benzamide
-
pH 5.5, 37C, BPH tissue, 50% inhibition at 0.0028 mM
non-steroidal bi-substrate inhibitors
-
several, structures, overview
-
oleic acid
-
isoform 1, 50% inhibition at 0.004 mM, isoform 2, 50% inhibition above 0.1 mM
oleic acid ethyl ester
-
isoform 1, 50% inhibition above 0.1 mM, isoform 2, 50% inhibition above 0.1 mM
ONO 3805
-
-
ONO-3805
-
a non-steroidal bi-substrate inhibitor
palmitic acid
-
isoform 1, 50% inhibition above 0.1 mM, isoform 2, 50% inhibition above 0.1 mM
penta-O-galloyl-beta-D-glucose
-
from Thea sativa, inhibits the expression of androgen receptor and reduce secretion of prostate-specific antigen in LNCaP prostate cancer cells
progesterone
-
competitive
sitosterol
-
isoform 1, 50% inhibition above 0.1 mM, isoform 2, 50% inhibition above 0.1 mM
SKF105657
-
a steroidal type II 5alpha-reductase specific inhibitor
stearic acid
-
isoform 1, 50% inhibition above 0.1 mM, isoform 2, 50% inhibition above 0.1 mM
steroid carboxylic acid compounds
-
diverse, tricyclic aryl acid mimics of, overview
theaflavin-3,3'-digallate
-
from Thea sativa, inhibits the expression of androgen receptor and reduce secretion of prostate-specific antigen in LNCaP prostate cancer cells
tocopherol
-
isoform 1, 50% inhibition above 0.1 mM, isoform 2, 50% inhibition above 0.1 mM
turosteride
-
-
Unsaturated 3-carboxysteroids
-
-
-
Zn2+
-
0.1 mM ZnCl2
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
androstandione
-
in male foreskin fibroblasts
androstenedione
-
in male foreskin fibroblasts
Oxytocin
-
increases activity in human prostate epithelial cells
testosterone
-
in female genital skin fibroblasts
additional information
-
oxytocin does not stimulate enzyme activity or expression in human prostate epithelial cells
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0002 - 0.0004
20alpha-hydroxyprogesterone
0.0008 - 0.001
androstenedione
0.004 - 0.018
corticosterone
0.015 - 0.65
NADPH
0.0003 - 0.00069
progesterone
0.0000013 - 0.014
testosterone
additional information
additional information
-
variations of Km with various concentrations of zearaleone, zearalanol or estradiol-17beta
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000006
(+)-LY191704
-
-
0.000004
(-)-LY191704
-
-
0.00092
(10bR)-8-chloro-4,10b-dimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one
-
isoform I
0.0011
(10bR)-8-chloro-4,5,10b-trimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one
-
isoform I
0.00026 - 0.0012
(4aS)-7-chloro-4a-methyl-2,3,4,4a-tetrahydrophenanthrene-2-carboxylic acid
0.000085
17-diisopropylcarbamoyl-2-androsten-3-carboxylate
-
-
0.000007 - 0.000018
17-diisopropylcarbamoyl-3,5-androstadien-3-carboxylate
-
-
0.00003
17-diisopropylcarbamoyl-3-androsten-3-carboxyate
-
-
0.0022
17-diisopropylcarbamoyl-androstan-3-carboxylate
-
-
0.0045
17-tert-butylcarbamoyl-3,5-androstadien-3-carbaldehyde
-
-
0.000033
17-tert-butylcarbamoyl-3,5-androstadien-3-carboxylate
-
-
0.0042
17-tert-butylcarbamoyl-3,5-androstadien-3-ol
-
-
0.000036 - 0.0093
17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
0.000315 - 0.01
2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
0.0000058
4,8-dimethyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I
0.000003 - 0.000004
4-methyl-azasteroid
0.000026 - 0.01
7-bromo-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
0.00032 - 0.0025
7-chloro-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
0.0000027
8-chloro-4-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I
0.0000003 - 0.0041
acylate episteride
-
0.0000043 - 0.000017
dutasteride
0.000001 - 0.005
finasteride
0.000004
LY306089
-
-
additional information
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00003
(+/-)-LY191704
Homo sapiens;
-
i.e. (4aS,10aR)-7-chloro-1-methyl-3,4,4a,9,10,10a-hexahydrophenanthren-2(1H)-one, non-steroidal, most potent benzoquinoline mimicing 4-azasteroid inhibitors, and specific for isozyme 5alphaR-1, IC50 is 30 nM
0.00892
(1E,4E,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,4,6-trien-3-one
Homo sapiens;
-
at pH 7.4 and 37C
0.0935
(1E,4E,6E)-1,7-bis(4-hydroxyphenyl)hepta-1,4,6-trien-3-one
Homo sapiens;
-
at pH 7.4 and 37C
0.0788
(1E,4E,6E)-1-(4-hydroxy-3-methoxyphenyl)-7-(3-hydroxyphenyl)hepta-1,4,6-trien-3-one
Homo sapiens;
-
at pH 7.4 and 37C
0.0886
(1E,4E,6E)-7-(3-hydroxyphenyl)-1-(4-hydroxyphenyl)hepta-1,4,6-trien-3-one
Homo sapiens;
-
at pH 7.4 and 37C
0.0153
(1E,6E)-1,7-bis(3,4-dihydroxyphenyl)hepta-1,6-diene-3,5-dione
Homo sapiens;
-
at pH 7.4 and 37C
0.000026
17a-(2-propionoxyethyl)-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
Homo sapiens;
P18405, P31213
pH not specified in the publication, 37C
0.000073
17a-allyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
Homo sapiens;
P18405, P31213
pH not specified in the publication, 37C
0.000022
17a-ethyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
Homo sapiens;
P18405, P31213
pH not specified in the publication, 37C
0.000054
17a-methyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
Homo sapiens;
P18405, P31213
pH not specified in the publication, 37C
0.00005
17alpha-p-bromophenylcarbamoyloxy-4-pregnen-3 20-dione
Homo sapiens;
-
in the presence of 1 mM dithiothreitol, in 40 mM sodium phosphate buffer, at pH 6.5
0.00005
17alpha-p-bromophenylcarbamoyloxy-4-pregnen-3,20-dione
Homo sapiens;
-
with 1 mM dithiothreitol in 40 mM sodium phosphate buffer, at pH 6.5 and 37C
0.00001
17alpha-phenylcarbamoyloxy-4-pregnen-3,20-dione
Homo sapiens;
-
in the presence of 1 mM dithiothreitol, in 40 mM sodium phosphate buffer, at pH 6.5; with 1 mM dithiothreitol in 40 mM sodium phosphate buffer, at pH 6.5 and 37C
0.0000011
3beta-(3'-oxapentanoyloxy)-androst-5-en-17-one
Homo sapiens;
-
pH 6.5, 37C
0.0000052
3beta-acetoxyandrost-5-en-17-one
Homo sapiens;
-
pH 6.5, 37C
0.000000002
3beta-hexanoyloxyandrost-5-en-17-one
Homo sapiens;
-
pH 6.5, 37C
0.00084
4-(3-(4-(N-methylacetamido)phenyl)pentan-3-yl)phenyl dibenzylcarbamate
Homo sapiens;
-
-
0.3
bisdemethoxycurcumin
Homo sapiens;
-
at pH 7.4 and 37C
0.0134
curcumin
Homo sapiens;
-
at pH 7.4 and 37C
0.000025
dehydroepiandrosterone
Homo sapiens;
-
pH 6.5, 37C
0.0225
demethoxycurcumin
Homo sapiens;
-
at pH 7.4 and 37C
0.0000085 - 0.008
finasteride
0.0005
MK386
Homo sapiens;
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
significant differences in 5 alpha-R2 activity levels between the cancerous and non-cancerous groups are observed
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.2 - 5.6
-
mutant G34R
6 - 6.5
-
mutant P181L
6.2
-
female
6.5
-
assay at
7 - 9
-
human: 2 forms, 1. pH-optimum 5.5 (only in fibroblasts derived from genital skin), 2. pH-optimum 7-9 (in both genital and nongenital skin regions and in fibroblast from all skin regions)
7.4
-
assay at, isoform 1
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
4.5 - 9
-
recombinant human 5alpha-reductase isozyme 1
4.5 - 9.5
-
recombinant human 5alpha-reductase isozyme 2
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
from beard and axillary hair and frontal scalp hair
Manually annotated by BRENDA team
-
the enzyme is detected in biopsies of pelvic endometriosis
Manually annotated by BRENDA team
-
both type 1 and type 2 isoenzyme, copy number of mRNA and activity of type 1 isoenzyme is significantly higher than type 2
Manually annotated by BRENDA team
-
type 2 isoenzyme
Manually annotated by BRENDA team
additional information
-
isozymes show different tissue distribution in androgen target organs
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
24000
-
5alphaR2, immunoblotting
26000
-
5alphaR1, SDS-PAGE
42000
-
5alpha-reductase isoenzyme 2, SDS-PAGE, after treatment with O-glycosidase and neuraminidase a protein of an apparent molecular weight of 30 kDa appears
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
0.5% n-octyl beta-D-glucopyranoside stabilizes
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
5alpha-reductase 2 purified using a four-step chromatographic procedure
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
transfection of HEK-293 cell
into pCMV7 and transfered to COS-1 cells
-
recombinant expression of isozymes 5alphaR-1 and 5alphaR-2 in e.g. human DU145 cells, in COS-1 cells, and in CHO 1827 and CHO 1829 cells, isozymes are chromosomal differently localized
-
transfection of HEK-293 cell
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
androgen regulates the mRNA level of 5alpha reductase isoenzymes in a cell type-specific manner. Regulation occurs at the transcriptional level, and the androgen receptor is necessary for this regulation
androgen regulates the mRNA level of 5alpha reductase isoenzymes in a cell type-specific manner. Regulation occurs at the transcriptional level, and the androgen receptor is necessary for this regulation. The androgen receptor is recruited to a negative androgen response element on the promoter of isoform SRD5A3 in vivo and directly binds to the negative androgen response element in vitro
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A207D
-
the mutation is associated with 5alpha-reductase type 2 deficiency
A248V
-
somatic variant, reduction of the apparent Ki for both finasteride and dutasteride
A51T
-
constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride
C133G
-
the mutation is associated with 5alpha-reductase type 2 deficiency
C5R
-
constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride
F118L
-
somatic variant, no significant change of the apparent Ki for both finasteride and dutasteride
F194L
-
constitutional variant, time-independent inhibition, displays lower apparent Ki for finasteride than dutasteride
F234L
-
constitutional variant, reduction of the apparent Ki for finasteride but not for dutasteride
G183D
-
somatic variant, reduction of the apparent Ki for both finasteride and dutasteride
G183S
-
mutant of 5alpha-reductase isozyme type-2
G191E
-
somatic variant, reduction of the apparent Ki for both finasteride and dutasteride
G34R
-
mutant of 5alpha-reductase isozyme type-2
G34W
-
the mutation is associated with 5alpha-reductase type 2 deficiency
H231R
-
mutant of 5alpha-reductase isozyme type-2
H264Q
-
mutant of 5alpha-reductase isozyme type-2
L221P
-
somatic variant, reduction of the apparent Ki for both finasteride and dutasteride
L226P
-
somatic variant, reduction of the apparent Ki for finasteride but not for dutasteride
N193S
-
mutant of 5alpha-reductase isozyme type-2
P181L
-
mutant of 5alpha-reductase isozyme type-2
P30L
-
constitutional variant, more than 100fold lower apparent Ki for dutasteride than for finasteride
P48R
-
constitutional variant, displays lower apparent Ki for finasteride than dutasteride in the 10 min reaction
R145W
-
mutant of 5alpha-reductase isozyme type-2
R171S
-
mutant of 5alpha-reductase isozyme type-2
R227Q
-
constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride
R246W
-
mutant of 5alpha-reductase isozyme type-2
T187M
-
constitutional variant, reduction of the apparent Ki for both finasteride and dutasteride
V189A
-
somatic variant, reduction of the apparent Ki for both finasteride and dutasteride
V3I
-
somatic variant, reduction of the apparent Ki for both finasteride and dutasteride
V63M
-
somatic variant, reduction of the apparent Ki for both finasteride and dutasteride
W53X
-
the mutation is associated with 5alpha-reductase type 2 deficiency
Y235F
-
the mutation is associated with 5alpha-reductase type 2 deficiency
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
pharmacology
-
enzyme is a target for drug developement