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Literature summary for 3.4.99.B1 extracted from

  • Porter, S.B.; Hildebrandt, E.R.; Breevoort, S.R.; Mokry, D.Z.; Dore, T.M.; Schmidt, W.K.
    Inhibition of the CaaX proteases Rce1p and Ste24p by peptidyl (acyloxy)methyl ketones (2007), Biochim. Biophys. Acta, 1773, 853-862.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
benzyloxycarbonyl-Phe-Ala-2,4,6-trimethylbenzoyloxymethyl ketone 0.25 mM, 8% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Arabidopsis thaliana
benzyloxycarbonyl-Phe-Ala-2,4,6-trimethylbenzoyloxymethyl ketone 0.25 mM, 12% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Homo sapiens
benzyloxycarbonyl-Phe-Ala-2,4,6-trimethylbenzoyloxymethyl ketone 0.25 mM, 10% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Saccharomyces cerevisiae
benzyloxycarbonyl-Phe-Lys-2,4,6-trimethylbenzoyloxymethyl ketone 0.25 mM, 61% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM), inhibition is not readily reversible Arabidopsis thaliana
benzyloxycarbonyl-Phe-Lys-2,4,6-trimethylbenzoyloxymethyl ketone 0.25 mM, 94% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM), inhibition is not readily reversible Homo sapiens
benzyloxycarbonyl-Phe-Lys-2,4,6-trimethylbenzoyloxymethyl ketone 0.25 mM, 75% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM), inhibition is not readily reversible Saccharomyces cerevisiae
tosyl-L-lysyl-chloromethylketone 0.25 mM, 26% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Arabidopsis thaliana
tosyl-L-lysyl-chloromethylketone 0.25 mM, 54% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobvenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Homo sapiens
tosyl-L-lysyl-chloromethylketone 0.25 mM, 12% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Saccharomyces cerevisiae
tosyl-L-phenylalanyl-chloromethylketone 0.25 mM, complete inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Arabidopsis thaliana
tosyl-L-phenylalanyl-chloromethylketone 0.25 mM, 93% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Homo sapiens
tosyl-L-phenylalanyl-chloromethylketone 0.25 mM, 68% inhibition of cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM). No significant inhibition of a-factor production Saccharomyces cerevisiae

Organism

Organism UniProt Comment Textmining
Arabidopsis thaliana
-
-
-
Homo sapiens
-
-
-
Saccharomyces cerevisiae
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM + H2O cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (ABZ-KSKTKC(farnesyl)QLIM) Saccharomyces cerevisiae ?
-
?
2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM + H2O cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (aminobenzoylZ-KSKTKC(farnesyl)-K(Dnp)-IM) Arabidopsis thaliana ?
-
?
2-aminobenzoyl-KSKTKC(farnesyl)QLIM + H2O cleavage of a quenched fluorogenic farnesylated peptide that is based on the C-terminal sequence of the K-Ras4b precursor (2-aminobenzoyl-KSKTKC(farnesyl)-K(Dnp)-IM) Homo sapiens ?
-
?
YIIKGVFWDPAC(farnesyl)-VIA + H2O
-
Saccharomyces cerevisiae a-factor + ?
-
?

Synonyms

Synonyms Comment Organism
At Rce1p
-
Arabidopsis thaliana
Hs Rce1p
-
Homo sapiens
Sc Rce1p
-
Saccharomyces cerevisiae

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
-
Saccharomyces cerevisiae

pH Range

pH Minimum pH Maximum Comment Organism
6 7.5 pH 6.0: 65% of maximal activity, pH 7.5: optimal activity Saccharomyces cerevisiae