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Literature summary extracted from
- Inhibition of the CaaX proteases Rce1p and Ste24p by peptidyl (acyloxy)methyl ketones (2007), Biochim. Biophys. Acta, 1773, 853-862.
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.24.84 | benzyloxycarbonyl-Phe-Ala-2,4,6-trimethylbenzoyloxymethyl ketone | 0.25 mM, 21% inhibition, inhibition is not reversible | Arabidopsis thaliana |  |
| 3.4.24.84 | benzyloxycarbonyl-Phe-Ala-2,4,6-trimethylbenzoyloxymethyl ketone | 0.25 mM, 41% inhibition, inhibition is not reversible | Homo sapiens | |
| 3.4.24.84 | benzyloxycarbonyl-Phe-Ala-2,4,6-trimethylbenzoyloxymethyl ketone | 0.25 mM, 22% inhibition, inhibition is not reversible | Saccharomyces cerevisiae | |
| 3.4.24.84 | benzyloxycarbonyl-Phe-Lys-2,4,6-trimethylbenzoyloxymethyl ketone | 0.25 mM, 76% inhibition, inhibition is not reversible | Arabidopsis thaliana | |
| 3.4.24.84 | benzyloxycarbonyl-Phe-Lys-2,4,6-trimethylbenzoyloxymethyl ketone | 0.25 mM, 68% inhibition, inhibition is not reversible | Homo sapiens | |
| 3.4.24.84 | benzyloxycarbonyl-Phe-Lys-2,4,6-trimethylbenzoyloxymethyl ketone | 0.25 mM, 76% inhibition, inhibition is not reversible | Saccharomyces cerevisiae | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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 | |
| 3.4.99.B1 | 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
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.24.84 | Arabidopsis thaliana | - |
- |
- |
| 3.4.24.84 | Homo sapiens | - |
- |
- |
| 3.4.24.84 | Saccharomyces cerevisiae | - |
- |
- |
| 3.4.99.B1 | Arabidopsis thaliana | - |
- |
- |
| 3.4.99.B1 | Homo sapiens | - |
- |
- |
| 3.4.99.B1 | Saccharomyces cerevisiae | - |
- |
- |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.99.B1 | 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 | ? | - |
? | |
| 3.4.99.B1 | 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 | ? | - |
? | |
| 3.4.99.B1 | 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 | ? | - |
? | |
| 3.4.99.B1 | YIIKGVFWDPAC(farnesyl)-VIA + H2O | - |
Saccharomyces cerevisiae | a-factor + ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.4.24.84 | At Ste24p | - |
Arabidopsis thaliana |
| 3.4.24.84 | Hs Ste24p | - |
Homo sapiens |
| 3.4.24.84 | Sc Ste24p | - |
Saccharomyces cerevisiae |
| 3.4.99.B1 | At Rce1p | - |
Arabidopsis thaliana |
| 3.4.99.B1 | Hs Rce1p | - |
Homo sapiens |
| 3.4.99.B1 | Sc Rce1p | - |
Saccharomyces cerevisiae |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 3.4.99.B1 | 7.5 | - |
- |
Saccharomyces cerevisiae |
pH Range
| EC Number | pH Minimum | pH Maximum | Comment | Organism |
|---|---|---|---|---|
| 3.4.99.B1 | 6 | 7.5 | pH 6.0: 65% of maximal activity, pH 7.5: optimal activity | Saccharomyces cerevisiae |
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