1.3.1.22 additional information - additional information inhibition kinetics 655182 1.3.1.22 additional information - additional information isozyme-specific IC50-values of diverse inhibitors, overview 656656 1.3.1.22 additional information - additional information the majority of the enzyme variants result in a reduction of the apparent Ki for both finasteride and dutasteride from 10 min to the 30 min reaction like the wild-type enzyme, but several variants result in an increase of the apparent Ki for each inhibitor or no significant change between the 10 min and 30 min reactions, thus exhibiting time independent inhibition 675475 1.3.1.22 0.0000003 - acylate episteride iosenzyme 2 396219 1.3.1.22 0.0000005 - acylate episteride iosenzyme 2 396219 1.3.1.22 0.000001 - finasteride iosenzyme 2 396219 1.3.1.22 0.000002 - 4-methyl-azasteroid iosenzyme 2 396219 1.3.1.22 0.0000027 - 8-chloro-4-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one isoform I 656656 1.3.1.22 0.000003 - 4-methyl-azasteroid iosenzyme 1 396219 1.3.1.22 0.000003 - 4-methyl-azasteroid iosenzyme 2 396219 1.3.1.22 0.000004 - (-)-LY191704 - 656656 1.3.1.22 0.000004 - 4-methyl-azasteroid iosenzyme 2 396219 1.3.1.22 0.000004 - acylate episteride iosenzyme 2 396219 1.3.1.22 0.000004 - finasteride iosenzyme 2 396219 1.3.1.22 0.000004 - LY306089 - 396222 1.3.1.22 0.0000043 - dutasteride wild-type, 30 min reaction time 675475 1.3.1.22 0.000005 - finasteride iosenzyme 2 396219 1.3.1.22 0.000005 - finasteride isozyme 5alphaR-2 656656 1.3.1.22 0.0000058 - 4,8-dimethyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one isoform I 656656 1.3.1.22 0.000006 - (+)-LY191704 - 656656 1.3.1.22 0.000006 - finasteride iosenzyme 1 396219 1.3.1.22 0.0000062 - 4-Aza-4-methyl-5alpha-pregnane-3,20-dione versus progesterone 389561, 390659 1.3.1.22 0.000007 0.000018 17-diisopropylcarbamoyl-3,5-androstadien-3-carboxylate - 390657 1.3.1.22 0.000008 - 4-methyl-azasteroid iosenzyme 1 396219 1.3.1.22 0.0000084 - 4-methyl-azasteroid - 396218 1.3.1.22 0.0000118 - 4-Aza-4-methyl-5alpha-pregnane-3,20-dione versus NADPH 389561, 390659 1.3.1.22 0.000017 - dutasteride wild-type, 10 min reaction time 675475 1.3.1.22 0.00002 - acylate episteride iosenzyme 1 396219 1.3.1.22 0.000023 - finasteride wild-type, 30 min reaction time 675475 1.3.1.22 0.000026 - 7-bromo-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid isoform I, Ki,app-value 656656 1.3.1.22 0.00003 - 17-diisopropylcarbamoyl-3-androsten-3-carboxyate - 390657 1.3.1.22 0.000033 - 17-tert-butylcarbamoyl-3,5-androstadien-3-carboxylate - 390657 1.3.1.22 0.000035 - (5alpha,20-R)-4-Diazo-21-hydroxy-20-methylpregnan-3-one at 25°C formation of the reversible EI complex is not rate-limiting for enzyme inactivation, and this is expressed as saturation kinetics for the inhibition reaction 396204 1.3.1.22 0.000036 - 17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid pH 7.0, 30°C, low Km-isoform from prostate 656681 1.3.1.22 0.00006 - 20alpha-hydroxypregn-4-en-3-one - 390662 1.3.1.22 0.00006 - finasteride wild-type, 10 min reaction time 675475 1.3.1.22 0.000085 - 17-diisopropylcarbamoyl-2-androsten-3-carboxylate - 390657 1.3.1.22 0.00022 - finasteride iosenzyme 1 396219 1.3.1.22 0.00026 - (4aS)-7-chloro-4a-methyl-2,3,4,4a-tetrahydrophenanthrene-2-carboxylic acid isoform II, Ki,app-value 656656 1.3.1.22 0.0003 - finasteride isozyme 5alphaR-1 656656 1.3.1.22 0.000315 - 2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid isoform I, Ki,app-value 656656 1.3.1.22 0.00032 - 7-chloro-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid isoform I, Ki,app-value 656656 1.3.1.22 0.00033 - finasteride - 396218 1.3.1.22 0.00036 - finasteride - 396215 1.3.1.22 0.00036 - theaflavin-3,3'-digallate pH 6.5, 37°C, versus NADPH 655182 1.3.1.22 0.00048 - penta-O-galloyl-beta-D-glucose pH 6.5, 37°C, versus NADPH 655182 1.3.1.22 0.0005 - acylate episteride iosenzyme 1 396219 1.3.1.22 0.00086 - progesterone - 396222 1.3.1.22 0.00092 - (10bR)-8-chloro-4,10b-dimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one isoform I 656656 1.3.1.22 0.001 - finasteride iosenzyme 1 396219 1.3.1.22 0.0011 - (10bR)-8-chloro-4,5,10b-trimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one isoform I 656656 1.3.1.22 0.0012 - (4aS)-7-chloro-4a-methyl-2,3,4,4a-tetrahydrophenanthrene-2-carboxylic acid isoform I, Ki,app-value 656656 1.3.1.22 0.0013 - finasteride pH 7.0, 30°C, low Km-isoform from prostate 656681 1.3.1.22 0.00154 - finasteride pH 6.0, 25°C 657353 1.3.1.22 0.0022 - 17-diisopropylcarbamoyl-androstan-3-carboxylate - 390657 1.3.1.22 0.0025 - 7-chloro-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid isoform II, Ki,app-value 656656 1.3.1.22 0.0026 - theaflavin-3'-gallate pH 6.5, 37°C, versus NADPH 655182 1.3.1.22 0.0027 - penta-O-galloyl-beta-D-glucose pH 6.5, 37°C, versus testosterone 655182 1.3.1.22 0.0028 - finasteride pH 7.0, 30°C, high Km-isoform from prostate 656681 1.3.1.22 0.0031 - MK434 - 396222 1.3.1.22 0.0041 - acylate episteride iosenzyme 1 396219 1.3.1.22 0.0042 - 17-tert-butylcarbamoyl-3,5-androstadien-3-ol - 390657 1.3.1.22 0.0043 - NADP+ versus NADPH 390659 1.3.1.22 0.0045 - 17-tert-butylcarbamoyl-3,5-androstadien-3-carbaldehyde - 390657 1.3.1.22 0.0049 - 17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid pH 7.0, 30°C, high Km-isoform from prostate 656681 1.3.1.22 0.0049 - 4,16-androstadien-3-one - 396222 1.3.1.22 0.005 - finasteride pH 7.0, 30°C, isoform from breast skin 656681 1.3.1.22 0.0056 - theaflavin-3,3'-digallate pH 6.5, 37°C, versus testosterone 655182 1.3.1.22 0.0065 - theaflavin-3'-gallate pH 6.5, 37°C, versus testosterone 655182 1.3.1.22 0.0093 - 17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid pH 7.0, 30°C, isoform from breast skin 656681 1.3.1.22 0.01 - 2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid isoform II, Ki,app-value 656656 1.3.1.22 0.01 - 7-bromo-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid isoform II, Ki,app-value 656656 1.3.1.22 0.0126 - 4-bromo-17alpha-(p-fluorobenzoyloxy)-4-pregnene-3,20-dione pH 6.0, 25°C 657353 1.3.1.22 0.026 - 17beta-estradiol intercept inhibition constant 390662 1.3.1.22 0.0319 - NADP+ versus progesterone 390659 1.3.1.22 0.036 - 17beta-estradiol slope inhibition constant 390662 1.3.1.22 0.146 - 17beta-hydroxyandrosta-1,4-diene-3-one - 390765