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2.5.1.59: protein geranylgeranyltransferase type I

This is an abbreviated version!
For detailed information about protein geranylgeranyltransferase type I, go to the full flat file.

Word Map on EC 2.5.1.59

Reaction

geranylgeranyl diphosphate
+
protein-cysteine
=
S-geranylgeranyl-protein
+
diphosphate

Synonyms

CAAX geranylgeranyltransferase, CaaX prenyltransferase, CaGGTase-I, CDC43, geranylgeranyl protein transferase type I, geranylgeranyltransferase I, geranylgeranyltransferase type I, geranylgeranyltransferase type-I, geranylgeranyltransferase-1, geranylgeranyltransferase-I, geranylgeranyltransferaseI, GGT, GGT I, GGTalpha, GGTase, GGTase I, Ggtase-1, GGTase-I, GGTaseI, GGTbeta, GGTI, mammalian GGTase-I, PGGT, PGGT beta, PGGT I, PGGT-I, PGGTase-I, PGGTaseI, Ppggb, protein geranylgeranyltransferase, protein geranylgeranyltransferase I, protein geranylgeranyltransferase type I, protein geranylgeranyltransferase type-I, protein geranylgeranyltransferase-I, type I protein geranylgeranyltransferase

ECTree

     2 Transferases
         2.5 Transferring alkyl or aryl groups, other than methyl groups
             2.5.1 Transferring alkyl or aryl groups, other than methyl groups (only sub-subclass identified to date)
                2.5.1.59 protein geranylgeranyltransferase type I

Crystallization

Crystallization on EC 2.5.1.59 - protein geranylgeranyltransferase type I

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CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
enzyme in complex with its substrate geranylgeranylpyrophosphate, hanging drop method, PCB buffer, pH 7.0 and 25% PEG 1500, cryoprotection in PCB vuffer, pH 7.0, 30% PEG 1500, and 10% ethylene glycol, flash frozen in liquid nitrogen, diffraction data collection at -173°C
hanging-drop method, crystal structure of GGTase-I in complex with its cognate lipid substrate, geranylgeranylpyrophosphate
molecular docking of inhibitor (S)-N-(1-amino-3-(4-fluorophenyl)-1-oxopropan-2-yl)-4-((1-(3,4-dichlorophenyl)-4-(2-(methylthio)ethyl)-3-(pyridin-3-yl)-1H-pyrazol-5-yl)oxy)butanamide shows several hydrogen bonding interactions and pi-pi contacts to the binding pocket of GGT1
1. binary complex with geranylgeranyl diphosphate, 2. ternary complex with a non-hydrolyzable geranylgeranyl diphosphate analog and CaaX peptide, 3. binary complex with prenyl-peptide product and 4. ternary complex with prenylated product and geranylgeranyl diphosphate. GGTase-I crystals belong to the I222 space group, with three complete 91 kDa heterodimers in the asymmetric unit. GGTase-I crystals are grown at 17°C in hanging drops using equal volumes of protein and reservoir solution (1.3 M (NH4)2SO4, 175 mM Na3 citrate pH 6.5, 20 mM dithiothreitol and 100 mM MES pH 6.3)
-
low-affinity ternary complex of L-778,123 bound in GGTase-I peptide-binding site and geranylgeranyl diphosphate bound in the lipid-binding site and complex of GGTase-I with L-778,123 and a sulfate anion
-