Target type: molecularfunction
Catalysis of the reaction: 2-trans,6-trans-farnesyl diphosphate + isopentenyl diphosphate = diphosphate + geranylgeranyl diphosphate. [EC:2.5.1.29, RHEA:17653]
Farnesyltransferase activity refers to the enzymatic process of transferring a farnesyl group from a farnesyl diphosphate molecule to a specific protein substrate. Farnesyl diphosphate, a 15-carbon isoprenoid, acts as the donor molecule, while the acceptor protein typically possesses a cysteine residue within a conserved CAAX motif at its C-terminal end. The catalytic mechanism involves a two-step process. First, the enzyme binds both farnesyl diphosphate and the substrate protein. Subsequently, the farnesyl group is transferred from the diphosphate to the cysteine residue of the protein, forming a stable thioether linkage. This covalent modification, known as farnesylation, significantly alters the properties of the target protein. It can enhance membrane association, promote protein-protein interactions, and influence protein trafficking and signaling pathways. Farnesyltransferases play crucial roles in various cellular processes, including cell growth, differentiation, and signaling. They are essential for the proper functioning of several key proteins involved in membrane trafficking, cytoskeletal organization, and signal transduction. Dysregulation of farnesyltransferase activity has been implicated in various diseases, including cancer and cardiovascular disorders.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Squalene synthase | [no definition available] | Bos taurus (cattle) |
| Squalene synthase | A squalene synthase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P37268] | Homo sapiens (human) |
| Geranylgeranyl pyrophosphate synthase | A geranylgeranyl pyrophosphate synthase that is encoded in the genome of human. [PRO:DNx, UniProtKB:O95749] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| alendronate | alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups. | 1,1-bis(phosphonic acid); primary amino compound | bone density conservation agent; EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor |
| amiodarone | amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias. Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance. | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
| pamidronate | phosphonoacetic acid | ||
| risedronic acid | Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION. | pyridines | |
| nadp | NADP | fundamental metabolite | |
| ibandronic acid | Ibandronic Acid: Aminobisphosphonate that is a potent inhibitor of BONE RESORPTION. It is used in the treatment of HYPERCALCEMIA associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of POSTMENOPAUSAL OSTEOPOROSIS. | ||
| zoledronic acid | zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position. Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS. | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| 6-amino-1-hydroxyhexane-1,1-diphosphonate | 6-amino-1-hydroxyhexane-1,1-diphosphonate: used for therapy of Paget's disease of bone & malignant hypercalcaemia | 1,1-bis(phosphonic acid) | |
| ne 58051 | NE 58051: inhibits tumor cell adhesion to extracellular matrices; structure in first source | ||
| ym 529 | YM 529: inhibits osteoclastic bone resorption; structure given in first source | ||
| b 581 | B 581 : A dipeptide obtained from the tetrapeptide Cys-Val-Phe-Met by reduction of the amide carbonyl groups of the Cys and Val residues. B 581: blocks farnesylated but not geranylgeranylated or myristylated, oncogenic Ras signaling & transformation | dipeptide | EC 2.5.1.58 (protein farnesyltransferase) inhibitor; peptidomimetic |
| 1-hydroxypentane-1,1-bisphosphonate | |||
| 1,1-hydroxyoctanodiphosphonate | |||
| farnesyl pyrophosphate | 2-trans,6-trans-farnesyl diphosphate : The trans,trans-stereoisomer of farnesyl diphosphate. farnesyl pyrophosphate: a sesquiterpene that dimerizes to SQUALENE; RN given refers to cpd without isomeric designation | farnesyl diphosphate | Escherichia coli metabolite; mouse metabolite |
| sq 109 | N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine: has antitubercular activity | ||
| tak 475 | 1-((1-(3-acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl)acetyl)piperidine-4-acetic acid: inhibits squalene synthase; structure in first source | ||
| digeranyl bisphosphonate | digeranyl bisphosphonate: structure in first source |