3.4.21.B6: prostasin
This is an abbreviated version!
For detailed information about prostasin, go to the full flat file.
Word Map on EC 3.4.21.B6
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3.4.21.B6
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matriptase
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aldosterone
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hai-1
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furin
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gpi-anchored
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aprotinin
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amiloride-sensitive
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glycosylphosphatidylinositol-anchored
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hepsin
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nexin-1
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kunitz-type
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camostat
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medicine
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profilaggrin
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enac-mediated
- 3.4.21.B6
- matriptase
- aldosterone
- hai-1
- furin
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gpi-anchored
- aprotinin
-
amiloride-sensitive
-
glycosylphosphatidylinositol-anchored
- hepsin
- nexin-1
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kunitz-type
- camostat
- medicine
- profilaggrin
-
enac-mediated
Reaction
endoprotease activity. Trypsin-like enzymatic activity =
Synonyms
CAP-1, CAP1, CAP1/PRSS8, channel activating protease 1, channel activating protease-1, channel-activating protease 1, channel-activating protease-1, LD47230p, prostasin, prostasin/PRSS8, PRSS8, S01.159, tracheal-prostasin
ECTree
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Inhibitors
Inhibitors on EC 3.4.21.B6 - prostasin
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(3R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-3-phenyl-L-prolinamide
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(3S)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-3-methyl-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-(cyclohexylmethoxy)-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-(cyclopentylmethoxy)-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-([[4-(methylsulfonyl)benzyl]carbamoyl]oxy)-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-hydroxy-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[(4-chlorobenzyl)oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[(4-fluorobenzyl)oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[(4-methylbenzyl)oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[(dimethylcarbamoyl)oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[(morpholin-4-ylcarbonyl)oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[(phenylcarbamoyl)oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[(piperidin-1-ylcarbonyl)oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[(pyrrolidin-1-ylcarbonyl)oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[[3-(trifluoromethyl)benzyl]oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-4-[[4-(trifluoromethyl)benzyl]oxy]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-4-(benzyloxy)-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-L-prolinamide
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(4R)-N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-4-[(benzylcarbamoyl)oxy]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-L-prolinamide
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benzyl [(1S)-2-[[(1S)-1-[[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]carbamoyl]-3-phenylpropyl]amino]-1-(1H-imidazol-4-ylmethyl)-2-oxoethyl]carbamate
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benzyl [(1S)-5-amino-1-[[(1S)-1-[[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]carbamoyl]-3-phenylpropyl]carbamoyl]pentyl]carbamate
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camostat mesilate
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potent inhibitor; potent prostasin inhibitor, 0.1 mM almost completely inhibits prostasin activity in vitro by 98.3%
N-[(1S)-1-[[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]carbamoyl]-3-methylbutyl]-N2-[(benzyloxy)carbonyl]-L-lysinamide
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N-[(1S)-1-[[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]carbamoyl]-3-methylbutyl]-Nalpha-[(benzyloxy)carbonyl]-L-histidinamide
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N-[(1S)-5-amino-1-(1,3-benzoxazol-2-ylcarbonyl)pentyl]-1-[(2R)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-L-prolinamide
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spironolactone
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decreases urinary prostasin in nomotensives in whom the renin/aldosterone axis is activated by a low Na+ intake, ineffective in individuals with high Na+ intake
TGF-beta1
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suppresses prostasin promoter activity in a time- and concentration-dependent manner, inhibition of prostasin expression by the induction of IkappaBalpha and the subsequent inhibition of NF-kappaB/Rel activity, may inhibit sodium reabsorption through a reduction in prostasin expression and subsequent inhibition of ENaC activity
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additional information
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not inhibited by alpha1-antitrypsin, alpha1-antitrypsinPDX, alpha1-antichymotrypsin, and soybean trypsin inhibitor
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viral promoter-driven expression of the human prostasin in the bladder of transgenic mice attenuates the bacterial lipopolysaccharide induction of nitric oxide synthase, whereas induction of cyclooxygenase-2, TNF-alpha, IL-1beta and IL-6 expression is not reduced
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bacterial lipopolysaccharide
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downregulation of mPro mRNA expression in the bladder, upregulation of inducible nitric oxide synthase, cyclooxygenase-2, interferon-gamma, TNF-alpha, IL-1beta, and IL-6
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of mouse seminal vesicle fluid, binds covalently to prostasin, complete inhibition
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inhibits prostasin´s serine protease activity, capable of binding to membrane-anchored prostasin
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