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Literature summary extracted from

  • 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 (2009), J. Biol. Chem., 284, 6861-6868.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.60 expression in Sf9 cells with recombinant baculovirus Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.60 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 Homo sapiens
2.5.1.60 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% Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.60 geranylgeranyl diphosphate + Rab Homo sapiens His6- and gluthathione S-transferase-tagged Rab proteins such as canine Rab1a, human Rab27a, Rab5a, Rab18, Rab6a, Rab13, and mouse Rab23 S-geranylgeranyl-Rab + diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.60 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.5.1.60 nickel-Sepharose affinity chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.60 geranylgeranyl diphosphate + Rab His6- and gluthathione S-transferase-tagged Rab proteins such as canine Rab1a, human Rab27a, Rab5a, Rab18, Rab6a, Rab13, and mouse Rab23 Homo sapiens S-geranylgeranyl-Rab + diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.60 Rab geranylgeranyltransferase type II
-
 Homo sapiens
2.5.1.60 RGGT
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.5.1.60 0.005
-
 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid mixed-type inhibition with geranylgeranyl diphosphate 1 as variable substrate, 50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 4 microM Rab1a, 50 nM enzyme, 20 min, 37°C Homo sapiens
2.5.1.60 0.03356
-
 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid uncompetitive reaction with Rab1a as variable substrate, 50 mM sodium HEPES, pH 7.2, 5 mM MgCl2, 1 mM Nonidet P-40, 1 mM dithioerythritol, 5 microM geranylgeranyl diphosphate 1, 50 nM enzyme, 20 min, 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.60 additional information
-
 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 Homo sapiens additional information
2.5.1.60 0.03185
-
 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 Homo sapiens 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid
2.5.1.60 0.03268
-
 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 Homo sapiens 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid
2.5.1.60 0.04347
-
 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 Homo sapiens 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid
2.5.1.60 0.86
-
 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 Homo sapiens 2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid