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3.4.21.B25: PACE4 proprotein convertase

This is an abbreviated version!
For detailed information about PACE4 proprotein convertase, go to the full flat file.

Word Map on EC 3.4.21.B25

Reaction

releases mature proteins from their proproteins by cleavage of Arg-Xaa-Yaa-Arg-Zaa bonds, where Xaa can be any amino acid and Yaa is Arg or Lys =

Synonyms

PACE 4, PACE-4, PACE4, PACE4/SPC4, paired basic amino acid cleaving enzyme 4, paired basic amino acid-cleaving enzyme 4, paired basic amino-acid-cleaving enzyme-4, PC7, proprotein convertase PACE4, S08.075, SPC4, subtilisin-like proprotein convertase, subtilisin-like proprotein convertase 4, subtilisin-like proprotein convertase PACE4, XPACE4

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.B25 PACE4 proprotein convertase

Inhibitors

Inhibitors on EC 3.4.21.B25 - PACE4 proprotein convertase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid
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3,3',3'',3'''-(benzene-1,4-diyldimethanetriyl)tetrakis(4-hydroxy-2H-chromen-2-one)
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3,3'-(1,3-benzodioxol-5-ylmethanediyl)bis(4-hydroxy-2H-chromen-2-one)
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3,3'-(2,3-dihydro-1H-inden-5-ylmethanediyl)bis(4-hydroxy-2H-chromen-2-one)
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A23187
-
if reticulocalbin-3 binds to proPACE4 transiently during its biosynthesis, this Ca2+-specific ionophore can block the maturation of proPACE4 to PACE4, accumulation of the proPaCE4-recticulocalbin-3 complex in the cells
Ac-(D)LLLLRVK-2,3-dehydroagmatine
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Ac-(D)LLLLRVK-4-amidinobenzylamide
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Ac-(D)LLLLRVKR-NH2
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Ac-LLLLR-((2S)-amino-3S-guanidinobutyryl)-KR-NH2
Ki(furin)/Ki(PACE4): 40
Ac-LLLLR-((2S,3R)-diaminobutyryl)-KR-NH2
Ki(furin)/Ki(PACE4): 9
Ac-LLLLR-((2S,3S)-diaminobutyryl)-KR-NH2
Ki(furin)/Ki(PACE4): 18
Ac-LLLLR-(2,3-diaminobutyryl)-KR-NH2
Ki(furin)/Ki(PACE4): 12
Ac-LLLLR-(2,3-diaminopropionyl)-KR-NH2
Ki(furin)/Ki(PACE4): 51
Ac-LLLLR-(2-amino-3-guanidinopropionyl)-KR-NH2
Ki(furin)/Ki(PACE4): 19
Ac-LLLLR-(2-amino-4-guanidinobutyryl)-KR-NH2
Ki(furin)/Ki(PACE4): 10
Ac-LLLLR-Orn-KR-NH2
Ki(furin)/Ki(PACE4): 21
Ac-LLLLRAKR-NH2
Ki(furin)/Ki(PACE4): 7
Ac-LLLLRKKR-NH2
Ki(furin)/Ki(PACE4): 18
Ac-LLLLRRKR-NH2
Ki(furin)/Ki(PACE4): 12
Ac-LLLLRVK-2,3-dehydroagmatine
-
Ac-LLLLRVK-4-amidinobenzylamide
-
Ac-LLLLRVKR-NH2
Ac-[C8](D)LLLLRVK-4-amidinobenzylamide
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Ac-[C8](D)LLLLRVKR-NH2
-
Ac-[C8]LLLLRVK-4-amidinobenzylamide
-
Ac-[C8]LLLLRVKR-NH2
-
Ac-[PEG2](D)LLLLRVK-4-amidinobenzylamide
-
Ac-[PEG2]LLLLRVKR-NH2
-
Ac-[PEG4]LLLLRVKR-NH2
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Ac-[PEG8](D)LLLLRVK-2,3-dehydroagmatine
-
Ac-[PEG8](D)LLLLRVK-4-amidinobenzylamide
-
Ac-[PEG8](D)LLLLRVKR-NH2
-
Ac-[PEG8]LLLLRVK-2,3-dehydroagmatine
-
Ac-[PEG8]LLLLRVK-4-amidinobenzylamide
-
Ac-[PEG8]LLLLRVKR-NH2
-
alpha1-antitrypsin
-
-
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alpha1-antitrypsin variant AVRR
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50% inhibition above 0.002 mM
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alpha1-antitrypsin variant PDX
-
50% inhibition above 0.00002 mM, forms a complex with the enzyme
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alpha1-antitrypsin variant Portland
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contains a minimal consensus sequence (Arg-X-X-Arg) for efficient cleavage by furin in its reactive site loop
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alpha1-antitrypsin variant RRRRSA
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rat alpha-antitrypsin showing substitution of Arg-Arg-Arg-Arg for Ala-Val-Pro-Met352 at P4-P1 and Ala for Leu354 at P2'
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alpha1-antitrypsin variant RRRRSL
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rat alpha-antitrypsin showing substitution of Arg-Arg-Arg-Arg for Ala-Val-Pro-Met352 at P4-P1
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alpha1-antitrypsin variant RVRR
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antisense oligo 5
depletes XPACE4 to 5-10% of control levels; depletes XPACE4 to 5-10% of control levels
Ca2+
-
Ca2+ ionophore inhibits protein maturation
carboxyterminal sequence of PACE4
-
inhibits autocatalytic processing
-
decanoyl-Arg-Val-Lys-Arg-chloromethylketone
decanoyl-L-Arg-L-Val-L-Lys-chloromethylketone
-
potent inhibitor
decanoyl-L-Arg-L-Val-L-Lys-L-Arg-chloromethylketone
-
potent inhibitor
decanoyl-RVKR-chloromethyl ketone
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H2N-[C8](D)LLLLRVK-2,3-dehydroagmatine
-
H2N-[C8](D)LLLLRVKR-NH2
-
H2N-[C8]LLLLRVK-2,3-dehydroagmatine
-
H2N-[C8]LLLLRVK-4-amidinobenzylamide
-
H2N-[C8]LLLLRVKR-NH2
-
HgCl2
-
99% inhibition at 1 mM
L-Arg-L-Tyr-L-Lys-L-Arg-L-Thr
-
peptide inhibitor of PACE4
leupeptin
-
94% inhibition at 1 mM
phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide
-
-
reticulocalbin-1
-
reduces efficiency of PACE4 secretion by 21%
-
ZnCl2
-
100% inhibition at 2 mM
[C8](D)LLLLRVK-2,3-dehydroagmatine
-
[C8](D)LLLLRVK-4-amidinobenzylamide
-
[C8](D)LLLLRVKR-NH2
-
[C8]LLLLRVK-2,3-dehydroagmatine
-
[C8]LLLLRVK-4-amidinobenzylamide
-
[C8]LLLLRVKR-NH2
-
additional information
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