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3.4.21.61: Kexin

This is an abbreviated version!
For detailed information about Kexin, go to the full flat file.

Word Map on EC 3.4.21.61

Reaction

Cleavage of -Lys-Arg-/- and -Arg-Arg-/- bonds to process yeast alpha-factor pheromone and killer toxin precursors =

Synonyms

adrenorphin-Gly-generating enzyme, ASP, BLI-4, corin activating enzyme, EC 3.4.22.23, endoproteinase Kex2p, Gene KEX2 dibasic proteinase, HuPCSK6, Kex 2p proteinase, Kex2, Kex2 endopeptidase, Kex2 endoprotease, Kex2 endoproteinase, Kex2 protease, Kex2 proteinase, Kex2-660, Kex2-like endoproteinase, Kex2-like precursor protein processing endoprotease, Kex2p, kexin, More, NARC-1, Paired-basic endopeptidase, PC 1/3, PC1, PC1/3, PC2, PCSK type 9, PCSK6, PCSK9, plasma proprotein convertase subtilisin-kexin type 9, pro-protein convertase subtilisin/kexin type 9, prohormone convertase 1, prohormone convertase 1/3, prohormone convertase 2, prohormone processing protease, Prohormone-processing endoprotease, Prohormone-processing KEX2 proteinase, Prohormone-processing proteinase, Proprotein convertase, proprotein convertase 1/3, proprotein convertase Kex2, proprotein convertase subtilisin kexin type 9, proprotein convertase subtilisin kexin-9, proprotein convertase subtilisin-like/kexin type 9, proprotein convertase subtilisin/kexin 6, proprotein convertase subtilisin/kexin type 6, proprotein convertase subtilisin/kexin type 9, proprotein convertase subtilisin/kexin type 9 (PCSK9)Proprotein convertase subtilisin/kexin type 9, proprotein processing protease, Protease KEX2, Proteinase Kex2p, Proteinase yscF, Proteinase, prohormone-processing, Yeast KEX2 protease

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.61 Kexin

Inhibitors

Inhibitors on EC 3.4.21.61 - Kexin

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(3S,4S,5S,6R)-2-([(2R,3S,4S,5S,6S)-3,5-dihydroxy-2-(hydroxymethyl)-6-methoxytetrahydro-2H-pyran-4-yl]amino)-6-(hydroxymethyl)tetrahydro-2H-thiopyran-3,4,5-triol
-
i.e. BJ-12-26-1, greatly reduces the processing of substrate proopiomelanocortin
(3S,4S,5S,6R)-2-([(2S,3S,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3-yl]amino)-6-(hydroxymethyl)tetrahydro-2H-thiopyran-3,4,5-triol
-
i.e. BJ-12-21-2, greatly reduces the processing of substrate proopiomelanocortin
5alpha,6alpha-epoxy-(22E,24R)-ergosta-8(14),22-diene-3beta,7beta-diol
isolated from fruiting bodies of Sparassis crispa
Ac-R-E-R-K-chloromethylketone
-
alternate binding site and resultant displacement of the scissile bond in the active site results in a decrease in the acylation rate
adenosine
-
Ala-Lys-Arg boronic acid
-
Ala-Lys-Arg chloromethyl ketone
-
-
Berberine
-
CT-peptide
-
decreases PC1/3 activity at high concentrations (micromol)
-
D-Tyr-Ala-Lys-Arg-CH2Cl
-
-
D-Tyr-Pro-Gly-Lys-Arg-CH2Cl
-
-
Decanoyl-Arg-Ala-Lys-Arg-CH2Cl
-
-
Decanoyl-Arg-Glu(OMe)-Lys-Arg-CH2Cl
-
-
Decanoyl-Phe-Ala-Lys-Arg-CH2Cl
-
-
decanoyl-R-V-K-R-chloromethylketone
-
-
decanoyl-R-V-R-K-chloromethylketone
-
-
diisopropyl fluorophosphate
-
-
eglin c mutant D42R
-
-
-
eglin c mutant L45R
-
-
-
eglin c mutant Tyr replaced with Glu at P4
-
-
-
eglin variant M1 RVTR
-
-
-
eglin variant M2 RVKR
-
-
-
eglin variant M3 RVTRDERY
-
-
-
eglin variant M4 RVTRDRRY
-
-
-
eglin variant M5 RVTRDLDY
-
-
-
eglin variant M6 RVTRDLRR
-
-
-
eglin variant M7 RVTRDLRE
-
-
-
eglin variant M8 RVTRDARY
-
-
-
hanabiratakelide A
isolated from fruiting bodies of Sparassis crispa
human urine trypsin inhibitor
-
most potent inhibitor
-
ISIS 394814
-
most potent antisense oligonucleotide. Administration to high fat-fed mice for 6 weeks reduces hepatic PCSK9 mRNA levels by 92%, total cholesterol and LDL by 53% and 38%, respectively. Inhibition of PCSK9 expression results in a 2fold increase in hepatic LDLR protein levels
-
Mercurials
-
-
-
p-chloromercuribenzoate
-
-
Peptidyl chloromethanes
-
-
Phe-Ala-Lys-Arg-CH2Cl
-
-
phenylmethylsulfonyl fluoride
Pro-norvaline-Tyr-Lys-Arg-CH2Cl
-
-
propeptide
-
addition of purified recombinant propeptide (20 nanomol) to PC1/3 enzymatic reaction leads to a 50% reduction in enzymatic activity. In the presence of 5 nanomol CT-peptide and 20 nanomol propeptide, inhibition is reduced to 35%
-
sparoside A
isolated from fruiting bodies of Sparassis crispa
sterol
-
completely blocks increase in PCSK9 mRNA by lovastatin
TIMP-3
-
completely abolishes the production of the 34-kDa PCSK9 product
-
Tyr-Ala-Arg-Ala-Lys-Arg-CH2Cl
-
-
additional information
-