3.4.21.93: Proprotein convertase 1
This is an abbreviated version!
For detailed information about Proprotein convertase 1, go to the full flat file.
Reaction
release of protein hormones, neuropeptides and renin from their precursors, generally by hydrolysis of -Lys-Arg-/- bonds
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Synonyms
Furin homolog, More, mPC1, mPC1/3, mPC3, mSPC3, murine PC1/3, murine proprotein convertase-1, murine proprotein convertase-1/3, Neuroendocrine convertase 1, PC 1/3, PC1, PC1/3, PC1/PC3, PC3, PCI, PCSK1, prohormone convertase, prohormone convertase 1, prohormone convertase 1/3, Prohormone convertase 3, prohormone convertase PC3, prohormone-convertase 1, propeptide convertase, Propeptide processing protease, proprotein convertase 1, proprotein convertase 1/3, proprotein convertase PC1, proprotein convertase PC1/3, protein convertase 1/3
ECTree
Inhibitors
Inhibitors on EC 3.4.21.93 - Proprotein convertase 1
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PC1 pro-peptide
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inhibits the mature PC1
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PC1/3 CT peptide
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decreases PC1/3 activity at high concentrations (micromol range)
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PenLen (rSAAS-(221-2546))
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profurin 39-62 DYYHFWHRGVKRSLSPHRPRHSR
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profurin 48-62 VTKRSLSPHRPRHSR
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proPC1/3 39-62/A NAYLF KAKSAPRRSRRSALAITKR
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proPC1/3 39-62/A NHYLF KHKSHPRRSALAITKR
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proPC1/3 50-62/A RRSRR SALHITKR
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proPC1/3 50-83 RRSRRSALHITKRLSDDDRVTWAEQQYEKERSKR
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proPC1/3 55-62 SALHITKR
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proPC1/3 55-62/A SALAITKR
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proPC1/3 55-83 SALHITKRLSDDDRVTWAEQQYEKERSKR
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proPC1/3 74-83 QQYEKERSKR
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proSAAS CT peptide
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endogenous inhibitor, inhibits the C-terminal PC1 processing
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Synthetic inhibitor
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can be used for developing an affinity purification procedure
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morphine
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human prohormone convertase 1/3 promoter activity is 73.1% in GH3-mu-opioid receptor cells receiving morphine compared with cells receiving media, and this reduction is reversed by naltrexone. In cells transfected with the prohormone convertase 1/3-minusCRE1/2 promoter construct, morphine does not reduce prohormone convertase 1/3-promoter activity. In wild-type GH3 cells (without the mu-opioid receptor), human prohormone convertase 1/3 promoter does not respond to morphine treatment. Regulation of prohormone convertase 1/3 promoter activity by morphine is mediated through the mu-opioid receptor
morphine
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short-term morphine (24 h) exposure downregulates prohormone convertase 1/3 protein levels in the rat hypothalamus. The cyclic-AMP response element in the promoter of prohormone convertase 1/3 is required for morphine-induced regulation of prohormone convertase 1/3
PC1 propeptide
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PC1 propeptide
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inhibits the mature PC1
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PC1/3 propeptide
inhibits the mature enzyme competitively, inhibition mechanism, interaction with the enzyme at the 50RRSRR54, 61KR62 and 65DDD67 sequences, molecular modeling, overview
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PC1/3 propeptide
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20 nanomol leads to a 50% reduction in enzymatic activity
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profurin 54-62 SPHRPRHSR
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profurin 54-62 SPHRPRHSR
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additional information
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proprotein convertase 1/3 expression is reduced in Bon-1 cells overexpressing Pdcd4
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additional information
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in wild-type mice prohormone convertase 1/3 mRNA levels show a 75% reduction with food deprivation and exceed ad libitum-fed levels after leptin treatment. Hypothalamic prohormone convertase 1/3 mRNA levels in N2KO mice show no significant variation between the deprived condition and ad libitum feeding. Leptin-treated N2KO mice have significantly lower prohormone convertase 1/3 mRNA levels than leptin-treated wild-type mice
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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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hyperthyroidism suppresses enzyme expression in hypothalamus and cerebral cortex
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