3.4.21.94: proprotein convertase 2
This is an abbreviated version!
For detailed information about proprotein convertase 2, go to the full flat file.
Word Map on EC 3.4.21.94
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3.4.21.94
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neuropeptides
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proopiomelanocortin
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medicine
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secretogranin
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prodynorphin
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peptidomic
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convertase-1
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molecular biology
- 3.4.21.94
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neuropeptides
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proopiomelanocortin
- medicine
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secretogranin
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prodynorphin
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peptidomic
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convertase-1
- molecular biology
Reaction
release of protein hormones and neuropeptides from their precursors, generally by hydrolysis of -Lys-Arg-/- bonds =
Synonyms
EGL-3/KPC2, More, Neuroendocrine convertase 2, PC2, PC2-like enzyme, PCSK2, pro-protein convertase-2, pro-protein convertase-2/carboxypeptidase-E, prohormone convertase, prohormone convertase 2, prohormone convertase-2, proneuropeptide convertase 2, proprotein convertase 2, proprotein convertase subtilisin/kexin-type 2
ECTree
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Inhibitors
Inhibitors on EC 3.4.21.94 - proprotein convertase 2
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(2R)-1-[2-[3,5-bis(trifluoromethyl)phenyl]ethyl]-4-[(1R)-2-cyclohexyl-1-[[(2S)-2-[[(2R)-2-(cyclohexylmethyl)piperazin-1-yl]methyl]pyrrolidin-1-yl]methyl]ethyl]-2-(cyclohexylmethyl)piperazine
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(2R)-4-((R)-1-cyclohexyl-3-((S)-2-(((R)-2-(cyclohexylmethyl)piperazin-1-yl)methyl)pyrrolidin-1-yl)propan-2-yl)-2-(cyclohexylmethyl)-1-(2-(4-isobutylphenyl)propyl)piperazine
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(2R)-4-((R)-1-cyclohexyl-3-((S)-2-(((S)-2-(cyclohexylmethyl)piperazin-1-yl)methyl)pyrrolidin-1-yl)propan-2-yl)-2-(cyclohexylmethyl)-1-(2-(4-isobutylphenyl)propyl)piperazine
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(R)-1-((4-tert-butylcyclohexyl)methyl)-4-((R)-1-cyclohexyl-3-((S)-2-(((S)-2-(cyclohexylmethyl)piperazin-1-yl)methyl)pyrrolidin-1-yl)propan-2-yl)-2-(cyclohexylmethyl)piperazine
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N-((R)-1-((2R,5R)-2,5-bis(4-hydroxybenzyl)-2,3,5,6-tetrahydro-1H-imidazo[1,2-a]imidazol-1-yl)-3-(4-hydroxyphenyl)propan-2-yl)-3-(3,4,5-trimethoxyphenyl)propanamide
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N-((R)-1-((2R,5R)-2,5-bis(4-hydroxybenzyl)-2,3,5,6-tetrahydro-1H-imidazo[1,2-a]imidazol-1-yl)-3-(4-methoxyphenyl)propan-2-yl)-3,4-dimethoxybenzamide
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N-((R)-1-((2R,5R)-2,5-bis(4-hydroxybenzyl)-2,3,5,6-tetrahydro-1H-imidazo[1,2-a]imidazol-1-yl)-3-(4-methoxyphenyl)propan-2-yl)-3-(3,4-dimethoxyphenyl)propanamide
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after screening 38 small-molecule positional scanning libraries against PC2, two promising chemical scaffolds are identified: bicyclic guanidines, and pyrrolidine bis-piperazines. A set of individual compounds is designed from each library and tested against PC2. Pyrrolidine bis-piperazines are irreversible, time-dependent inhibitors of PC2, exhibiting noncompetitive inhibition kinetics
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additional information
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starvation reduces the serum levels of leptin which decreases PC1 expression, the effect can be reversed by administration of exogenous leptin
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additional information
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stable expression of antisense PC2 mRNA in rMTC 6-23 cells results in a drastic decrease in PC2 protein synthesis by more than 90%, accompanied by a marked reduction in pro-neurotensin/neuromedin N cleavage by more than 80% at sites 2, 3, and 4
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additional information
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oxygen and glucose deprivation inhibit the PC2 activity, the pro-PC2 maturation, and thus the neuropeptide pro-protein processing system
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