Protein Prenyltransferases

Protein prenyltransferases are enzymes that transfer isoprenoid lipids (such as farnesyl or geranylgeranyl groups) to acceptor molecules. The attachment of these groups is known as prenylation, and it is catalyzed by FTase and GGTase 1.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
2407 FTI 277
Prodrug form of FTI 276 (Cat. No. 2406)
2430 GGTI 298
Geranylgeranyltransferase I (GGTase I) inhibitor
2637 Gliotoxin
Farnesyltransferase and geranylgeranyltransferase I inhibitor
4294 LB 42708
Selective farnesyltransferase (FTase) inhibitor
6265 Lonafarnib
Potent farnesyl transferase inhibitor

Protein prenyltransferases are enzymes that transfer isoprenoid lipids (such as farnesyl or geranylgeranyl groups) to acceptor molecules. The attachment of these groups is known as prenylation. Farnesyltransferase (FTase) and geranylgeranyltransferase type 1 (GGTase 1) catalyze this modification, which takes place at a conserved cysteine residue in a CaaX motif in the protein substrate (in which 'C' is cysteine, 'a' is an aliphatic amino acid, and 'X' is variable). The attachment of a farnesyl group or a geranyl group permits membrane localization of proteins lacking a transmembrane domain, and occurs post-translationally.

FTase and GGTase 1 are heterodimeric enzymes that share a common α-subunit and different β-subunits. Target proteins include Ras, which is suggestive of a role for prenylation in tumor development. Ras requires farnesylation for malignant activity, and many of the downstream proteins it targets are also subject to farnesylation or geranylgeranylation in order to mediate the growth, survival and migration of tumor cells. Prenyltransferase inhibitors are therefore of interest in the development of cancer therapeutics. Farnesyltransferase inhibitors (FTIs) exhibit antitumor effects by inducing apoptosis and cell cycle arrest, and inhibiting cell proliferation, migration and angiogenesis. Geranylgeranyltransferase type 1 inhibitors (GGTIs) also induce apoptosis and inhibit the growth of tumor cells.

Literature for Protein Prenyltransferases

Cancer

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Protein Prenyltransferase Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Farnesyltransferase (α subunit) Human FNTA NM_002027 L10413
Mouse Fnta NM_008033 Q61239
Rat Fnta NM_012847 Q04631
Farnesyltransferase (β subunit) Human FNTB NM_002028 NM_145927
Mouse Fntb NM_145927 NM_145927
Rat Fntb NM_172034 NM_145927
Rab Geranylgeranyltransferase (α subunit) Human RABGGTA NM_182836 -
Mouse Rabggta NM_019519 Q9JHK4
Rat Rabggta NM_031654 Q08602
Rab Geranylgeranyltransferase (β subunit) Human RABGGTB NM_004582 U49245
Mouse Rabggtb NM_028096 P53612
Rat Rabggtb NM_138708 Q08603