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Farnesyltransferase

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Revision as of 11:49, 11 March 2012 by Michal Harel (Talk | contribs)
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Farnesyltransferase (FTase) is part of the prenyltransferase group. FTase modifies proteins by adding farnesyl diphosphate (FPP) – an isoprenoid lipid – to a cysteine near the C terminal. This addition forms a thioether linkage, makes the protein more hydrophobic and associates it with the membrane. Farnesylated proteins – like those of the Ras family - are involved in cellular signaling. Thus, FTase inhibitors are being tested as anti-cancer agents. FTase are composed of 2 subunits. The β subunit coordinates a Zn atom.

3D structures of farnesyltransferase

1ft1 – rFTase – rat
3q73 – CnFTase – Cryptococcus neoformans

FTase binary complex with FPP

1ft2, 1fpp – rFTase + FPP
1o1r, 1o1s - rFTase + FPP-analog

FTase binary complex with peptide

1kzp, 1o1t - rFTase + farnesylated peptide
2h6f - hFTase + farnesylated peptide
2h6g, 2h6h, 2h6i - hFTase α subunit + β subunit (mutant) + farnesylated peptide
3q79 - CnFTase + farnesylated peptide

FTase binary complex with inhibitor

3eu5 – rFTase + biotin-GPP
3euv - rFTase α subunit + β subunit (mutant)+ biotin-GPP
1n94, 1n95, 1n9a, 1o5m, 1ni1, 1x81, 2bed, 2r2l - rFTase + inhibitor
1nl4 - rFTase α subunit (mutant) + β subunit + inhibitor

FTase ternary complex with FPP and peptide

1d8d, 1tn8 - rFTase + Ras peptide + FPP-analog
1kzo - rFTase + farnesylated Ras peptide + FPP
1tn7, 3dpy - rFTase + peptide + FPP
1jcr, 1jcs - rFTase + tetrapeptide inhibitor + FPP
1d8e - rFTase no Zn + Ras peptide + FPP-analog
1tn6 - hFTase + Rap2a peptide + FPP-analog
3q75, 3q78 - CnFTase + peptide + FPP-analog

FTase ternary complex with FPP and inhibitor

1sa5, 3e30, 3e32, 3e33, 3e34, 3e37 - rFTase + inhibitor + FPP
2zir, 2zis - rFTase α subunit (mutant) + β subunit + inhibitor + FPP
1jcq – hFTase α subunit (mutant) + β subunit + inhibitor + FPP– human
1ld7, 1ld8, 1mzc, 1sa4, 1s63, 2f0y - hFTase + inhibitor + FPP
2iej - hFTase + inhibitor + FPP-analog
3pz4 - FTase + inhibitor + FPP – mouse
3q7a, 3q7f - CnFTase + inhibitor + FPP
3fsx, 3sfy - CnFTase + inhibitor + FPP-analog

Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky, Joel L. Sussman

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