Page last updated: 2024-10-24

farnesyl-diphosphate farnesyltransferase activity

Definition

Target type: molecularfunction

Catalysis of the reaction: 2 farnesyl diphosphate = diphosphate + presqualene diphosphate. [EC:2.5.1.21]

Farnesyl-diphosphate farnesyltransferase (FPPS) is a critical enzyme in the biosynthesis of isoprenoids, a diverse class of organic compounds that play vital roles in cellular signaling, membrane structure, and other fundamental processes. FPPS catalyzes the head-to-tail condensation of two molecules of farnesyl diphosphate (FPP) to form geranylgeranyl diphosphate (GGPP). This reaction occurs in two steps: first, FPPS binds to two molecules of FPP, aligning them in a specific orientation. Then, the enzyme utilizes a divalent metal ion, typically magnesium, to facilitate the removal of a pyrophosphate group from one FPP molecule and its transfer to the other FPP molecule, forming a C15-C15 bond and releasing one molecule of inorganic pyrophosphate. The resulting GGPP molecule serves as a precursor for a variety of isoprenoids, including dolichol, sterols, and ubiquinone. These isoprenoids are essential for the proper functioning of membranes, the synthesis of proteins, and other key cellular processes. Mutations in FPPS can lead to a number of human diseases, including retinitis pigmentosa and various metabolic disorders.'
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Proteins (1)

ProteinDefinitionTaxonomy
Squalene synthaseA squalene synthase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P37268]Homo sapiens (human)

Compounds (6)

CompoundDefinitionClassesRoles
amiodaroneamiodarone : 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
nadpNADPfundamental metabolite
b 581B 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
dipeptideEC 2.5.1.58 (protein farnesyltransferase) inhibitor;
peptidomimetic
farnesyl pyrophosphate2-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 diphosphateEscherichia coli metabolite;
mouse metabolite
sq 109N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine: has antitubercular activity
tak 4751-((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