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Farnesyltransferase information


Protein farnesyltransferase
Identifiers
EC no.2.5.1.58
CAS no.131384-38-8
Databases
IntEnzIntEnz view
BRENDABRENDA entry
ExPASyNiceZyme view
KEGGKEGG entry
MetaCycmetabolic pathway
PRIAMprofile
PDB structuresRCSB PDB PDBe PDBsum
Gene OntologyAmiGO / QuickGO
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PMCarticles
PubMedarticles
NCBIproteins

Farnesyltransferase (EC 2.5.1.58) is one of the three enzymes in the prenyltransferase group. Farnesyltransferase (FTase) adds a 15-carbon isoprenoid called a farnesyl group to proteins bearing a CaaX motif: a four-amino acid sequence at the carboxyl terminus of a protein. Farnesyltransferase's targets include members of the Ras superfamily of small GTP-binding proteins critical to cell cycle progression. For this reason, several FTase inhibitors are undergoing testing as anti-cancer agents. FTase inhibitors have shown efficacy as anti-parasitic agents, as well. FTase is also believed to play an important role in development of progeria and various forms of cancers.

Farnesyltransferase catalyzes the chemical reaction

farnesyl diphosphate + protein-cysteine S-farnesyl protein + diphosphate

Thus, the two substrates of this enzyme are farnesyl diphosphate and protein-cysteine, whereas its two products are S-farnesyl protein and diphosphate.

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Farnesyltransferase

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Farnesyltransferase (EC 2.5.1.58) is one of the three enzymes in the prenyltransferase group. Farnesyltransferase (FTase) adds a 15-carbon isoprenoid...

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Farnesyltransferase inhibitor

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The farnesyltransferase inhibitors (FTIs) are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of...

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Prenylation

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methylation. Carboxyl methylation only occurs on prenylated proteins. Farnesyltransferase and geranylgeranyltransferase I are very similar proteins. They consist...

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Presqualene diphosphate synthase

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systematic name (2E,6E)-farnesyl-diphosphate:(2E,6E)-farnesyl-diphosphate farnesyltransferase (presqualene diphosphate forming). This enzyme catalyses the following...

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Progeria

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triggers three sequential enzymatic modifications. First, protein farnesyltransferase catalyzes the addition of a farnesyl moiety to the cysteine. Second...

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Tipifarnib

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name Zarnestra) is a farnesyltransferase inhibitor. Farnesyltransferase inhibitors block the activity of the farnesyltransferase enzyme by inhibiting...

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FNTB

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Protein farnesyltransferase subunit beta is an enzyme that in humans is encoded by the FNTB gene. GRCm38: Ensembl release 89: ENSMUSG00000033373 – Ensembl...

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COX10

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Protoheme IX farnesyltransferase, mitochondrial is an enzyme that in humans is encoded by the COX10 gene. Cytochrome c oxidase (COX), the terminal component...

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FTI

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Australia Fair Trials International, a British human rights organization Farnesyltransferase inhibitor, a class of cancer drugs Federation of Thai Industries...

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Ras GTPase

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manipulate the regulation of the above-mentioned localization of Ras. Farnesyltransferase inhibitors have been developed to stop the farnesylation of Ras and...

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Lonafarnib

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midazolam and certain cholesterol-lowering medications. Lonafarnib, a farnesyltransferase inhibitor, is an oral medication that helps prevent the buildup of...

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Optical rotation

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are used infrequently in English. Sebti; Hamilton, eds. (2001). Farnesyltransferase inhibitors in cancer therapy. p. 126. ISBN 9780896036291. Retrieved...

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FNTA

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Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha is an enzyme that in humans is encoded by the FNTA gene. Prenyltransferases...

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Guard cell

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Ghassemian M, Kwak CM, McCourt P, & Schroeder JI (1998) Role of farnesyltransferase in ABA regulation of guard cell anion channels and plant water loss...

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Costello syndrome

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treatment he devised for children affected by Progeria. He discussed how farnesyltransferase inhibitors (FTIs) affects H-Ras. After his presentation, members...

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Channing Der

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prompted intense pharmaceutical industry pursuit of inhibitors of the farnesyltransferase enzyme that catalyzes this lipid modification on RAS and other proteins...

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Chromosome 8

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protein F-box protein 16 FDFT1 encoding protein Farnesyl-diphosphate farnesyltransferase 1 FGFR1: fibroblast growth factor receptor 1 (fms-related tyrosine...

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Geranylgeranylation

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onto the C-terminal consensus sequence CAAL (somewhat similar to farnesyltransferase reactions), where C=cysteine, A=any aliphatic amino acid, and L=leucine...

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Clavaric acid

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random screening of natural extracts. Clavaric acid is a reversible farnesyltransferase inhibitor with an IC50 of 1.3 μM. Lingham RB, Silverman KC, Jayasuriya...

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Andrastin A

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Andrastin A is a farnesyltransferase inhibitor isolate of Penicillium species including Penicillium albocoremium and Penicillium roqueforti. It has been...

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Janus kinase inhibitor

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COMT Thymidylate synthase 2.4 PARP 2.5 Dihydropteroate synthetase Farnesyltransferase 2.6 GABA transaminase 2.7 Nucleotidyltransferase Integrase Reverse...

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Dicarboxylic acid

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basis for the development of anticancer drugs due to their strong farnesyltransferase inhibitory effects. A series of alkyl- and alkenyl-itaconates, known...

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Geranylgeranyltransferase type 1

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attack on the geranylgeranyl diphosphate, displacing the diphosphate. Farnesyltransferase Prenylation Rab geranylgeranyltransferase – Geranylgeranyltransferase...

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Neurofibroma

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as drug R115777) inhibits the activation of RAS. This drug is a Farnesyltransferase inhibitor which inhibits the Ras kinase in a post translational modification...

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Large granular lymphocytic leukemia

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Sokol L, Chen X, et al. (December 2008). "Clinical improvement by farnesyltransferase inhibition in NK large granular lymphocyte leukemia associated with...

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