2.5.1.60: protein geranylgeranyltransferase type II

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

Reaction

Synonyms

AtRGTA1, AtRGTA2, AtRGTB1, Chm, geranylgeranyl transferase type I subunit alpha 1, geranylgeranyl transferase type I subunit alpha 2, geranylgeranyl transferase type II subunit beta 1, geranylgeranyl transferase type II subunit beta 2, geranylgeranyl transferase type-1 subunit alpha 1, geranylgeranyl transferase type-2 subunit alpha 2, geranylgeranyl transferase type-2 subunit beta 1, geranylgeranyl transferase type-2 subunit beta 2, geranylgeranyltransferase II, geranylgeranyltransferase type II, GGT2, GGTase-II, GGTase3, GGTaseII, PGGT-II, protein geranylgeranyltransferase type-II, PTAR1, Rab geranylgeranyl transferase, Rab geranylgeranyl transferase alpha subunit 2, Rab geranylgeranyl transferase beta subunit 1, Rab geranylgeranyl transferase beta subunit 2, Rab geranylgeranyl transferase lpha subunit 1, Rab geranylgeranyl-transferase, Rab geranylgeranyltransferase, Rab geranylgeranyltransferase type II, Rab GG transferase, Rab GGTase, Rab proteins geranylgeranyltransferase component A 1, RAB-GGT, Rab-GGT alpha 1, Rab-GGT alpha 2, Rab-GGT beta 1, Rab-GGT beta 2, Rab11a, RabGGT, RabGGTase, Rabggtb, REP/GGTase, RGGT, RGT alphabeta, RGTA1, RGTA2, RGTB1, RGTB2

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)

                2.5.1.60 protein geranylgeranyltransferase type II

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Results	in table
8	Activating Compound
6396	AA Sequence
3	Application
1	CAS Registry Number
18	Cloned(Commentary)
2	Cofactor
6	Crystallization (Commentary)
280	Disease/ Diagnostics
2	Expression
16	General Information
32	IC50 Value
89	Inhibitors
10	Ki Value [mM]
9	KM Value [mM]
2	Localization
5	Metals/Ions
6	Molecular Weight [Da]
21	Natural Substrates/ Products (Substrates)
55	Organism
43	PDB ID
2	pH Optimum
6	Protein Variants
11	Purification (Commentary)
19	Reaction
50	Reference
24	Source Tissue
4	Specific Activity [micromol/min/mg]
79	Substrates and Products (Substrate)
10	Subunits
100	Synonyms
1	Systematic Name
1	Temperature Optimum [°C]
2	Turnover Number [1/s]

IC50 Value

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IC50 Value on EC 2.5.1.60 - protein geranylgeranyltransferase type II

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IC50 VALUE [mM]

INHIBITOR

ORGANISM

UNIPROT

COMMENTARY

LITERATURE

IMAGE

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

0.007

(2R,3R,4S,5R)-2-(3,4-dichlorophenyl)-4-(hexylsulfanyl)-1-[(4-methylphenyl)sulfonyl]-5-propylpyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.0036

(2R,3R,4S,5R)-2-(4-bromophenyl)-1-[(4-methylphenyl)sulfonyl]-4-(pentylsulfanyl)-5-propylpyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.0021

(2R,3R,4S,5R)-2-(4-bromophenyl)-4-(hexylsulfanyl)-1-[(4-methylphenyl)sulfonyl]-5-propylpyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.0045

(2R,3R,4S,5R)-2-(4-bromophenyl)-4-[(4-methoxyphenyl)sulfanyl]-1-[(4-methylphenyl)sulfonyl]-5-propylpyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.0048

(2R,3R,4S,5R)-2-(4-bromophenyl)-5-ethyl-4-(hexylsulfanyl)-1-[(4-methylphenyl)sulfonyl]pyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.0022

(2R,3R,4S,5R)-2-(4-bromophenyl)-5-hexyl-4-(hexylsulfanyl)-1-[(4-methylphenyl)sulfonyl]pyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.0047

(2R,3R,4S,5R)-4-[(3-tert-butoxy-3-oxopropyl)sulfanyl]-2-(3-chlorophenyl)-5-(cyclopentylmethyl)-1-[(4-methylphenyl)sulfonyl]pyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.0031

(2R,3R,4S,5R)-4-[(3-tert-butoxy-3-oxopropyl)sulfanyl]-2-(4-chlorophenyl)-1-[(4-chlorophenyl)sulfonyl]-5-(cyclopentylmethyl)pyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.007

(2R,3R,4S,5R)-4-[(3-tert-butoxy-3-oxopropyl)sulfanyl]-2-(4-chlorophenyl)-5-(cyclopentylmethyl)-1-(phenylsulfonyl)pyrrolidine-3-carboxylic acid

Rattus norvegicus

-

-

687811

0.0177

2-bromo-3-(3-pyridinyl)-2-phosphonopropionic acid

Rattus norvegicus

-

-

688263

0.0164

2-chloro-3-(3-pyridinyl)-2-phosphonopropionic acid

Rattus norvegicus

-

-

688263

0.0163

2-fluoro-3-(3-pyridinyl)-2-phosphonopropionic acid

Rattus norvegicus

-

-

688263

0.03185 - 0.86

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

4 entries

0.0353

3-(3-pyridinyl)-2-phosphonopropionic acid

Rattus norvegicus

-

-

688263

0.0241

3-pyridinyl ethylidene hydroxyl phosphonocarboxylate

Rattus norvegicus

-

-

688263

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

709461

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

709461

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

709461

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

709461

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

709461

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

709461

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

709461

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

709461

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

709461

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

709461

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

709461

additional information

additional information

2 entries

-

0.03185

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

Homo sapiens

-

50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 6 microM tritium-labelled geranylgeranyl diphosphate, 4 microM Rab1a-CC (wild type), 2 microM Rab escort protein 1, 50 nM enzyme, 20 min, 37°C

709077

0.03268

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

Homo sapiens

-

50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 6 microM tritium-labelled geranylgeranyl diphosphate, 4 microM Rab27a-CGC (wild type), 2 microM Rab escort protein 1, 50 nM enzyme, 20 min, 37°C

709077

0.04347

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

Homo sapiens

-

50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 6 microM tritium-labelled geranylgeranyl diphosphate, 4 microM Rab5a-CCSN (wild type), 2 microM Rab escort protein 1, 50 nM enzyme, 20 min, 37°C

709077

0.86

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

Homo sapiens

-

50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 6 microM tritium-labelled geranylgeranyl diphosphate, 4 microM Rab5a-CCVLL, 2 microM Rab escort protein 1, 50 nM enzyme, 20 min, 37°C

709077

additional information

additional information

Homo sapiens

-

chemicals that cause an activity decrease of more than 70% at 100 microM are selected for inhibition studies

709461

-

additional information

additional information

Homo sapiens

-

the inhibitory action of 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid with substrates Rab1a-CSC and Rab1a-CCS are not determined, and is not significant (IC50 > 2 mM) with the substrates Rab1a-CS, Rab1aSC, Rab27a-CVLS, Rab5a-CCQNI, Rab5a-CVLL, Rab13-CSLG (wild type), Rab18-CSVL (wild type), and Rab23-CSVP (wild type), and IC50 > 1.592 mM with Rab6a-CSC

709077

-