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 (Comment) | Organism |
---|---|
enzyme produced using an Sf9 cell overexpression | Rattus norvegicus |
Crystallization (Comment) | Organism |
---|---|
two crystal structures of enzyme complex: one containing farnesylated Ras peptide product alone and a complex that contains both the farnesylated peptide and an additional farnesyl diphosphate substrate | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | two primary modes of inhibition: blocking the peptide substrate site and blocking the exit groove | Rattus norvegicus |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Rattus norvegicus | |
Zn2+ | the zinc ion activates the cysteine thiolate for nucleophilic attack on the C1 atom of the farnesyl diphosphate substrate | Rattus norvegicus |
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 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
- |
- |
Reaction | Comment | Organism | Reaction ID |
---|---|---|---|
farnesyl diphosphate + protein-cysteine = S-farnesyl protein + diphosphate | kinetic mechanism | Rattus norvegicus | |
farnesyl diphosphate + protein-cysteine = S-farnesyl protein + diphosphate | enzyme constitutes the protein prenyltransferase family of enzymes | Rattus norvegicus |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
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 | - |
? |