Information on EC 2.5.1.60 - protein geranylgeranyltransferase type II and Organism(s) Homo sapiens and UniProt Accession P53611

P53611

GDP-bound form of Rab3 is preferred substrate of enzyme

-

?

(2E,6E,10Z)-3,7,11-trimethyl-12-[(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]dodeca-2,6,10-trien-1-yl diphosphate + Rab7 GTPase

(2E,6E,10Z)-3,7,11-trimethyl-12-[(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]dodeca-2,6,10-trien-1-yl-Rab7 GTPase + diphosphate

-

in vitro prenylation assay with 4 microM Rab7 wild type or mutants, 6 mircoM Rab escort protein, 6 microM enzyme, 50 mM HEPES buffer, pH 7.2, containing 50 mM NaCl, 5 mM dithioerythritol, 2 mM MgCl2, and 10 mircoM GDP, 25°C, 50 microM of the geranylgeranyl diphosphate analogue (3,7,11-trimethyl-12-(7-nitro-benzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,10-triem-1) diphosphate, end-point assay with 6 microM Rab7 wild type or mutants, 10 microM Rab escort protein, 6 microM enzyme in the same buffer mixture, and 40 microM (3,7,11-trimethyl-12-(7-nitro-benzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,10-triem-1) diphosphate, 1.5 hours at 25°C

709014

-

?

(3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate + Rab7

(3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1)-Rab7 + diphosphate

-

geranylgeranyl diphosphate analogue and Rab7 as substrates in the presence of Rab escort protein, in vitro inhibition assays

-

?

biotinylated geranyl diphosphate + EYFP-Rab7

S-biotin-geranyl-Rab7 + diphosphate

-

COS-7 cells are transfected with EYFP-Rab7 fusion protein and incubated with inhibitors, cells lysed after 24 h, clarified supernatant incubated in biotinylated geranyl diphosphate (geranylgeranyl diphosphate substrate analogue), recombinant RabGGTase and Rab escort protein, in vivo inhibitor studies

-

?

geranylgeranyl diphosphate + FBXL2

geranylgeranyl-FBXL2 + diphosphate

P53611; Q7Z6K3

FBXL2 is an ubiquitin-ligase

759843

-

?

geranylgeranyl diphosphate + protein-cysteine

S-geranylgeranyl-protein + diphosphate

3 entries

geranylgeranyl diphosphate + Rab

S-geranylgeranyl-Rab + diphosphate

-

His6- and gluthathione S-transferase-tagged Rab proteins such as canine Rab1a, human Rab27a, Rab5a, Rab18, Rab6a, Rab13, and mouse Rab23

-

?

additional information

?

-

3 entries

geranylgeranyl diphosphate + protein-cysteine

S-geranylgeranyl-protein + diphosphate

-

the enzyme catalyzes posttranslational modification of proteins, the farnesyl moieties attached to the substrates are directly involved in protein-protein interactions as well as in protein-membrane interactions

658829

-

?

geranylgeranyl diphosphate + Rab

S-geranylgeranyl-Rab + diphosphate

-

His6- and gluthathione S-transferase-tagged Rab proteins such as canine Rab1a, human Rab27a, Rab5a, Rab18, Rab6a, Rab13, and mouse Rab23

-

?

additional information

?

-

(2-[(1-geranylgeranyl)-1H-1,2,3-triazol-4-yl]ethane-1,1-diyl)bis(phosphonate)

-

compound is able to induce cytotoxicity in human myeloma cells, IC50 value 1 mM

721823

2-fluoro-3-(1-methyl-1H-imidazol-5-yl)-2-phosphonopropanoic acid

compound inhibits isoform Rab11A, but not Rap1A/Rap1B prenylation in HeLa cells

759076

2-fluoro-3-(1H-imidazol-4(5)-yl)-2-phosphonopropanoic acid

compound inhibits isoform Rab11A, but not Rap1A/Rap1B prenylation in HeLa cells

759076

2-fluoro-3-(6-methylimidazo[1,2-a]pyridin-3-yl)-2-phosphonopropanoic acid

compound is an micromolar inhibitor of Rab11A prenylation, is inactive against Rap1A/Rap1B modification, and able to inhibit proliferation of HeLa cell line with IC50 value of 0.36 mM

2-fluoro-3-(6-phenylimidazo[1,2-a]pyridin-3-yl)-2-phosphonopropanoic acid

compound is an micromolar inhibitor of Rab11A prenylation, is inactive against Rap1A/Rap1B modification, and able to inhibit proliferation of HeLa cell line with IC50 value of 0.51 mM

2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid

-

3-PEHPC, weak inhibitor, 100% activity remain with concentrations up to 1 microM inhibitor and substrate Rab1a, with 10 microM inhibitor about 60% activity remain, with 100 microM and more inhibitor the activity falls to 30% and below

2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid

-

(+)-3-IPEHPC, the (+)-enantiomer is selective towards the enzyme and more potent than the (-)-enantiomer, mixed type inhibitor with respect to geranylgeranyl diphosphate, uncompetitive inhibitor with respect to Rab substrate, 25fold more potent than 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid, with 1 microM inhibitor activity falls to about 50%, with 10 microM inhibitor and more activity falls below 20%

3-(6-bromoimidazo[1,2-a]pyridin-3-yl)-2-fluoro-2-phosphonopropanoic acid

compound is an micromolar inhibitor of Rab11A prenylation, is inactive against Rap1A/Rap1B modification, and able to inhibit proliferation of HeLa cell line with IC50 value of 0.50 mM

3-(6-chloroimidazo[1,2-a]pyridin-3-yl)-2-fluoro-2-phosphonopropanoic acid

compound is an micromolar inhibitor of Rab11A prenylation, is inactive against Rap1A/Rap1B modification, and able to inhibit proliferation of HeLa cell line with IC50 value of 0.52 mM

methyl N-undecanoyl-L-tyrosyl-L-histidyl-L-tyrosinate

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-([[2-(benzyloxy)benzyl]oxy]carbonyl)-D-histidyl-L-tyrosyl-L-phenylalanine

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini)

N-([[2-(benzyloxy)benzyl]oxy]carbonyl)-L-histidyl-L-tyrosyl-L-phenylalanine

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini)

N-butanoyl-L-histidyl-L-phenylalanyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-octanoyl-L-histidyl-L-phenylalanyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-pentadecanoyl-L-histidyl-L-phenylalanyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-undecanoyl-L-histidyl-L-histidyl-N-(4-aminobutyl)-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-undecanoyl-L-histidyl-L-histidyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide), not cytotoxic to COS-7 cells, fluorescence titration reveals competitive inhibition

N-undecanoyl-L-histidyl-L-phenylalanyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide), not cytotoxic to COS-7 cells, fluorescence titration reveals partial competitive inhibition which points to a different binding site

N-undecanoyl-L-histidyl-L-phenylalanyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-undecanoyl-L-tyrosyl-L-histidyl-N-(4-aminobutyl)-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-undecanoyl-L-tyrosyl-L-histidyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide), not cytotoxic to COS-7 cells, fluorescence titration reveals competitive inhibition

N-[(2,5-dimethyl-1,3-oxazol-4-yl)carbonyl]glycyl-L-phenylalanyl-1-trityl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2,5-dimethyl-1,3-oxazol-4-yl)carbonyl]glycyl-L-phenylalanyl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]-1-trityl-L-histidylglycyl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]-1-trityl-L-histidylglycyl-L-phenylalanine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]-L-histidylglycyl-1-trityl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus), not cytotoxic to COS-7 cells, fluorescence titration reveals competitive inhibition

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]-L-histidylglycyl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]glycyl-L-phenylalanyl-1-(tert-butoxycarbonyl)-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]glycyl-L-phenylalanyl-1-benzyl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]glycyl-L-phenylalanyl-1-trityl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]glycyl-L-phenylalanyl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]histidylglycyl-L-phenylalanine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[(2E)-3-(biphenyl-4-yl)prop-2-enoyl]-D-histidyl-L-tyrosyl-L-tyrosine

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini)

N-[(2E)-3-[2-[(1Z)-pent-1-en-1-yl]phenyl]prop-2-enoyl]-D-histidyl-L-tyrosyl-D-phenylalanine

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini)

N-[(benzyloxy)carbonyl]-D-tyrosyl-L-phenylalanyl-L-tyrosine

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), fluorescence titration reveals competitive inhibition

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-L-tyrosine

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), fluorescence titration reveals competitive inhibition

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-N-hydroxy-D-tyrosinamide

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini)

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-N-hydroxy-L-tryptophanamide

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), not cytotoxic to COS-7 cells

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-N-hydroxy-L-tyrosinamide

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), not cytotoxic to COS-7 cells

N-[3-(4-pentylphenyl)propanoyl]-D-histidyl-N-methyl-L-phenylalanyl-L-phenylalanine

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini)

N-[3-(4-pentylphenyl)propanoyl]-D-tyrosyl-L-tyrosyl-L-phenylalanine

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini)

N-[4-(undecyloxy)benzoyl]-L-histidyl-L-histidyl-N-(4-aminobutyl)-L-histidinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-[4-(undecyloxy)benzoyl]-L-histidyl-L-histidyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-histidinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-[4-(undecyloxy)benzoyl]-L-histidyl-L-tyrosyl-N-[3-(1H-imidazol-1-yl)propyl]-L-phenylalaninamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-[4-(undecyloxy)benzoyl]-L-tyrosyl-L-tyrosyl-N-(4-aminobutyl)-L-tyrosinamide

-

class III inhibitors (comprising a lipophilic N-terminus and an amine or N-heterocycle containing a C-terminal amide)

N-[[2-(pyridin-3-yl)-1,3-thiazol-4-yl]carbonyl]glycyl-L-phenylalanyl-1-trityl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[[2-(pyridin-3-yl)-1,3-thiazol-4-yl]carbonyl]glycyl-L-phenylalanyl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[[2-(thiophen-2-yl)-1,3-thiazol-4-yl]carbonyl]glycyl-L-phenylalanyl-1-trityl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

N-[[2-(thiophen-2-yl)-1,3-thiazol-4-yl]carbonyl]glycyl-L-phenylalanyl-L-histidine

-

class II inhibitors (combining a heterocyclic ring system at the N-terminus with a free carboxylate at the C-terminus)

additional information

-

peptidic library based on the farnesyl transferase inhibitor pepticinnamin E, a natural tripeptide from Streptomyces OH-4652

-

Rab escort protein

-

additional information

P53611

comparison of KM of Rab3a proteins

-

0.005 - 0.03356

2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid

0.0011

N-undecanoyl-L-histidyl-L-histidyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

displacement titration

0.0054

N-undecanoyl-L-histidyl-L-phenylalanyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

displacement titration

0.0028

N-undecanoyl-L-tyrosyl-L-histidyl-N-methyl-N-[2-(pyridin-2-yl)ethyl]-L-tyrosinamide

-

displacement titration

0.0053

N-[(2-phenyl-1,3-oxazol-4-yl)carbonyl]-L-histidylglycyl-1-trityl-L-histidine

-

displacement titration

0.0045

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-L-tyrosine

0.0145

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-N-hydroxy-L-tyrosinamide

-

displacement titration

0.1

(2-[(1-geranylgeranyl)-1H-1,2,3-triazol-4-yl]ethane-1,1-diyl)bis(phosphonate)

Homo sapiens

-

temperature not specified in the publication, pH not specified in the publication

721823

0.03185 - 0.86

2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid

4 entries

0.0156

N-([[2-(benzyloxy)benzyl]oxy]carbonyl)-D-histidyl-L-tyrosyl-L-phenylalanine

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.0193

N-([[2-(benzyloxy)benzyl]oxy]carbonyl)-L-histidyl-L-tyrosyl-L-phenylalanine

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.0227

N-[(2E)-3-(biphenyl-4-yl)prop-2-enoyl]-D-histidyl-L-tyrosyl-L-tyrosine

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.0152

N-[(2E)-3-[2-[(1Z)-pent-1-en-1-yl]phenyl]prop-2-enoyl]-D-histidyl-L-tyrosyl-D-phenylalanine

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.0041

N-[(benzyloxy)carbonyl]-D-tyrosyl-L-phenylalanyl-L-tyrosine

Homo sapiens

-

most potent of the class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.0227

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-L-tyrosine

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.0136

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-N-hydroxy-D-tyrosinamide

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.0052

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-N-hydroxy-L-tryptophanamide

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.009

N-[(benzyloxy)carbonyl]-L-histidyl-N-methyl-L-phenylalanyl-N-hydroxy-L-tyrosinamide

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.019

N-[3-(4-pentylphenyl)propanoyl]-D-histidyl-N-methyl-L-phenylalanyl-L-phenylalanine

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

0.011

N-[3-(4-pentylphenyl)propanoyl]-D-tyrosyl-L-tyrosyl-L-phenylalanine

Homo sapiens

-

class I inhibitors (compounds possessing a free carboxylic or hydroxamic acid at the C-terminus and lipophilic N-termini), 9 microM (3,7,11-trimethyl-12-(7-nitrobenzo[1,2,5]oxadiazo-4-ylamino)-dodeca-2,6,19-trien-1) diphosphate, 3 microM Rab7, 3 microM Rab escort protein, 400 nM enzyme

additional information

-

-

SwissProt

-

-

-

adenocarcinoma of colon, significant overexpression of RabGGT-beta compared to normal tissue

-

-

large cell lung carcinomas, significant overexpression of RabGGT-beta compared to normal tissue

658377

melanoma cell

-

significant overexpression of RabGGT-beta and Rab-GGT-alpha compared to normal tissue

-

-

significant overexpression of RabGGT-beta and RabGGT-alpha compared to normal tissue

-

-

malfunction

physiological function

P53611 pBLAST

PGTB2_HUMAN

331

0

36924

Swiss-Prot

Show Sequence

other Location (Reliability: 2)

5 entries

heterodimer

-

2 * ?, computational model based on crystals of subcomplexes

709014

enzyme-inhibitor complex with an engeneered enzyme lacking the LRR- and Ig-domains, complexes are prepared by soaking of co-crystallization, diffraction data collection at -173°C

-

structure of the full-length GGTase3-FBXL2-SKP1 complex reveals an extensive multivalent interface specifically formed between the leucine-rich repeat domain of substrate FBXL2 and subunit PTAR1

P53611; Q7Z6K3

759843

additional information

nickel-Sepharose affinity chromatography

-

685017, 709077

cloning of the beta subunit of enzyme by means of the yeast two-hybrid system

-

-

expressed in Sf9 cells

-

685017

expression in Sf9 cells with recombinant baculovirus

-

medicine

-

RabGGT is a therapeutically relevant target for modulation of apoptosis

658377

Johannes, L.; Perez, F.; Laran-Chich, M.P.; Henry, J.P.; Darchen, F.

Characterization of the interaction of the monomeric GTP-binding protein Rab3a with geranylgeranyl transferase II

Eur. J. Biochem.

239

362-368

1996

Rattus norvegicus, Homo sapiens (P53611)

8706741

658377

Lackner, M.R.; Kindt, R.M.; Carroll, P.M.; Brown, K.; Cancilla, M.R.; Chen, C.; de Silva, H.; Franke, Y.; Guan, B.; Heuer, T.; Hung, T.; Keegan, K.; Lee, J.M.; Manne, V.; O'Brien, C.; Parry, D.; Perez-Villar, J.J.; Reddy, R.K.; Xiao, H.; Zhan, H.; Cockett, M.; Plowman, G.; Fitzgerald, K.; Costa, M.; Ross-Macdonald, P.

Chemical genetics identifies Rab geranylgeranyl transferase as an apoptotic target of farnesyl transferase inhibitors

Cancer Cell

7

325-336

2005

Caenorhabditis elegans, Homo sapiens

15837622

658829

Maurer-Stroh, S.; Washietl, S.; Eisenhaber, F.

Protein prenyltransferases

Genome Biol.

4

212

2003

Homo sapiens

12702202

685017

Baron, R.A.; Seabra, M.C.

Rab geranylgeranylation occurs preferentially via the pre-formed REP-RGGT complex and is regulated by geranylgeranyl pyrophosphate

Biochem. J.

415

67-75

2008

Homo sapiens

18532927

709014

Wu, Y.W.; Goody, R.S.; Abagyan, R.; Alexandrov, K.

Structure of the disordered C terminus of Rab7 GTPase induced by binding to the Rab geranylgeranyl transferase catalytic complex reveals the mechanism of Rab prenylation

J. Biol. Chem.

284

13185-13192

2009

Homo sapiens

19240028

Baron, R.A.; Tavare, R.; Figueiredo, A.C.; B?azewska, K.M.; Kashemirov, B.A.; McKenna, C.E.; Ebetino, F.H.; Taylor, A.; Rogers, M.J.; Coxon, F.P.; Seabra, M.C.

Phosphonocarboxylates inhibit the second geranylgeranyl addition by Rab geranylgeranyl transferase

J. Biol. Chem.

284

6861-6868

2009

Homo sapiens

19074143

Tan, K.T.; Guiu-Rozas, E.; Bon, R.S.; Guo, Z.; Delon, C.; Wetzel, S.; Arndt, S.; Alexandrov, K.; Waldmann, H.; Goody, R.S.; Wu, Y.W.; Blankenfeldt, W.

Design, synthesis, and characterization of peptide-based rab geranylgeranyl transferase inhibitors

J. Med. Chem.

52

8025-8037

2009

Homo sapiens

19894725

721823

Zhou, X.; Hartman, S.V.; Born, E.J.; Smits, J.P.; Holstein, S.A.; Wiemer, D.F.

Triazole-based inhibitors of geranylgeranyltransferase II

Bioorg. Med. Chem. Lett.

23

764-766

2013

Homo sapiens

23266123

739491

Koehnke, M.; Delon, C.; Hastie, M.L.; Nguyen, U.T.; Wu, Y.W.; Waldmann, H.; Goody, R.S.; Gorman, J.J.; Alexandrov, K.

Rab GTPase prenylation hierarchy and its potential role in choroideremia disease

PLoS ONE

8

e81758

2013

Homo sapiens

24358126

759076

Joachimiak, L.; Marchwicka, A.; Gendaszewska-Darmach, E.; Blazewska, K.M.

Synthesis and biological evaluation of imidazole-bearing alpha-phosphonocarboxylates as inhibitors of Rab geranylgeranyl transferase (RGGT)

ChemMedChem

13

842-851

2018

Homo sapiens (P24386)

29498238