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Literature summary for 2.5.1.58 extracted from
- Protein farnesyltransferase isoprenoid substrate discrimination is dependent on isoprene double bonds and branched methyl groups (2001), Biochemistry, 40, 12254-12265.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | evidence that inhibitors of enzyme could be effective therapeutic agents in treatment of many human cancers | Rattus norvegicus |
| medicine | prime target for development of anticancer therapeutics | Rattus norvegicus |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression in Escherichia coli | Rattus norvegicus |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| X-ray crystal structure, modelling indicates that geranylgeranyl diphosphate adopts a different conformation than the farnesyl chain of farnesyl diphosphate | Rattus norvegicus |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | correlation between Km and analogue hydrophobicity and length | Rattus norvegicus | |
| 0.046 | - |
farnesyl diphosphate | - |
Rattus norvegicus |  |
| 0.056 | - |
8-benzyloxy-3-methyl-2-octen-1-ol-diphosphate | - |
Rattus norvegicus | |
| 0.089 | - |
10-benzyloxy-3-methyl-2-decen-1-ol-diphosphate | - |
Rattus norvegicus | |
| 0.091 | - |
9-benzyloxy-3-methyl-2-nonen-1-ol-diphosphate | - |
Rattus norvegicus | |
| 0.13 | - |
7-benzyloxy-3-methyl-2-hepten-1-ol-diphosphate | - |
Rattus norvegicus | |
| 0.45 | - |
geranylgeranyl diphosphate | - |
Rattus norvegicus | |
| 0.89 | - |
6-benzyloxy-3-methyl-2-hexen-1-ol-diphosphate | - |
Rattus norvegicus | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Rattus norvegicus | |
| Mg2+ | appears to coordinate the diphosphate moiety of farnesyl diphosphate | Rattus norvegicus | |
| Zn2+ | required | Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| farnesyl diphosphate + protein-cysteine | Rattus norvegicus | process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics | S-farnesyl protein + diphosphate | - |
? | |
| farnesyl diphosphate + protein-cysteine | Rattus norvegicus | process necessary for the subcellular localisation of substrate to the plasma membrane | S-farnesyl protein + diphosphate | - |
? | |
| farnesyl diphosphate + protein-cysteine | Rattus norvegicus | enzyme responsible for catalysing isoprene lipid modifications | S-farnesyl protein + diphosphate | - |
? | |
| farnesyl diphosphate + protein-cysteine | Rattus norvegicus | A series of steps modifies the C-terminus of Ras. Enzyme catalyses the first of these steps by transferring the farnesyl group from farnesyl diphosphates to the cysteine side chain in the CAAX sequence motif at the C-terminus of Ras | S-farnesyl protein + diphosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Rattus norvegicus | - |
- |
- |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| farnesyl diphosphate + protein-cysteine = S-farnesyl protein + diphosphate | kinetic mechanism | Rattus norvegicus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 10-benzyloxy-3-methyl-2-decen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser | - |
Rattus norvegicus | diphosphate + N-dansyl-Gly-S-(10-benzyloxy-3-methyl-2-decenyl)-Cys-Val-Leu-Ser | - |
? | |
| 6-benzyloxy-3-methyl-2-hexen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser | - |
Rattus norvegicus | diphosphate + N-dansyl-Gly-S-(6-benzyloxy-3-methyl-2-hexenyl)-Cys-Val-Leu-Ser | - |
? | |
| 7-benzyloxy-3-methyl-2-hepten-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser | - |
Rattus norvegicus | diphosphate + N-dansyl-Gly-S-(7-benzyloxy-3-methyl-2-heptenyl)-Cys-Val-Leu-Ser | - |
? | |
| 8-benzyloxy-3-methyl-2-octen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser | - |
Rattus norvegicus | diphosphate + N-dansyl-Gly-S-(8-benzyloxy-3-methyl-2-octenyl)-Cys-Val-Leu-Ser | - |
? | |
| 9-benzyloxy-3-methyl-2-nonen-1-ol-diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser | - |
Rattus norvegicus | diphosphate + N-dansyl-Gly-S-(9-benzyloxy-3-methyl-2-nonenyl)-Cys-Val-Leu-Ser | - |
? | |
| farnesyl diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser | the best substrate | Rattus norvegicus | diphosphate + N-dansyl-Gly-S-farnesyl-Cys-Val-Leu-Ser | - |
? | |
| farnesyl diphosphate + protein-cysteine | posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins, the reactive cysteine is located in the C-terminal Ca1a2X motif in which C is the modified cysteine, a1 and a2 are often an aliphatic residue, and X is Ser, Met, Ala or Gln | Rattus norvegicus | diphosphate + S-farnesyl protein | - |
? | |
| farnesyl diphosphate + protein-cysteine | process required for the transforming activity of oncogenic variants of Ras, making enzyme a prime target for anticancer therapeutics | Rattus norvegicus | S-farnesyl protein + diphosphate | - |
? | |
| farnesyl diphosphate + protein-cysteine | process necessary for the subcellular localisation of substrate to the plasma membrane | Rattus norvegicus | S-farnesyl protein + diphosphate | - |
? | |
| farnesyl diphosphate + protein-cysteine | enzyme responsible for catalysing isoprene lipid modifications | Rattus norvegicus | S-farnesyl protein + diphosphate | - |
? | |
| farnesyl diphosphate + protein-cysteine | A series of steps modifies the C-terminus of Ras. Enzyme catalyses the first of these steps by transferring the farnesyl group from farnesyl diphosphates to the cysteine side chain in the CAAX sequence motif at the C-terminus of Ras | Rattus norvegicus | S-farnesyl protein + diphosphate | - |
? | |
| geranylgeranyl diphosphate + N-dansyl-Gly-Cys-Val-Leu-Ser | - |
Rattus norvegicus | diphosphate + N-dansyl-Gly-S-geranylgeranyl-Cys-Val-Leu-Ser | - |
? | |
| geranylgeranyl diphosphate + protein-cysteine | - |
Rattus norvegicus | diphosphate + S-geranylgeranylcysteinyl protein | - |
? | |
| additional information | not: geranylgeranyl diphosphate | Rattus norvegicus | ? | - |
? | |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.84 | - |
7-benzyloxy-3-methyl-2-hepten-1-ol-diphosphate | - |
Rattus norvegicus | |
| 15 | - |
geranylgeranyl diphosphate | - |
Rattus norvegicus | |
| 25 | - |
10-benzyloxy-3-methyl-2-decen-1-ol-diphosphate | - |
Rattus norvegicus | |
| 27 | - |
8-benzyloxy-3-methyl-2-octen-1-ol-diphosphate | - |
Rattus norvegicus | |
| 43 | - |
9-benzyloxy-3-methyl-2-nonen-1-ol-diphosphate | - |
Rattus norvegicus | |
| 44 | - |
6-benzyloxy-3-methyl-2-hexen-1-ol-diphosphate | - |
Rattus norvegicus | |
| 100 | - |
farnesyl diphosphate | - |
Rattus norvegicus | |
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Release 2023.1 (January 2023)
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