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Literature summary extracted from

  • Lu, J.; Yoshimura, K.; Goto, K.; Lee, C.; Hamura, K.; Kwon, O.; Tamanoi, F.
    Nanoformulation of geranylgeranyltransferase-I inhibitors for cancer therapy: liposomal encapsulation and pH-dependent delivery to cancer cells (2015), PLoS ONE, 10, e0137595.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.59 additional information nanoformulation of geranylgeranyltransferase-I inhibitors for cancer therapy, liposomal encapsulation and pH-dependent delivery to cancer cells, scheme of synthesis of pH-responsive liposome and the proposed intracellular drug release pathway, method, overview. Liposomal GGTI inhibits protein geranylgeranylation inside the cell and this effect is dependent on the low pH of lysosomes; nanoformulation of geranylgeranyltransferase-I inhibitors for cancer therapy, liposomal encapsulation and pH-dependent delivery to cancer cells, scheme of synthesis of pH-responsive liposome and the proposed intracellular drug release pathway, method, overview. Liposomal GGTI inhibits protein geranylgeranylation inside the cell and this effect is dependent on the low pH of lysosomes Homo sapiens
2.5.1.59 P61A6 derived from an allenoate-derived compound library, shows efficiency of the enzyme inhibitor to inhibit tumor growth demonstrated using human pancreatic cancer xenograft; derived from an allenoate-derived compound library, shows efficiency of the enzyme inhibitor to inhibit tumor growth demonstrated using human pancreatic cancer xenograft Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.59 geranylgeranyl diphosphate + protein-cysteine Homo sapiens the enzyme adds a C20 geranylgeranyl group to proteins such as RhoA, RhoC, Rap1 and Ral at the cysteine within the carboxy-terminal tetrapeptide consensus sequence CAAL (C is cysteine, A is an aliphatic amino acid, and the C-terminal residue is leucine or phenylalanine) S-geranylgeranyl-protein + diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.59 Homo sapiens P49354 subunit alpha
-
2.5.1.59 Homo sapiens P53609 subunit beta
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.5.1.59 A-549 cell
-
 Homo sapiens
-
2.5.1.59 BEAS-2B cell
-
 Homo sapiens
-
2.5.1.59 bronchial epithelium cell
-
 Homo sapiens
-
2.5.1.59 H-358 cell
-
 Homo sapiens
-
2.5.1.59 H-596 cell
-
 Homo sapiens
-
2.5.1.59 MCF-7 cell
-
 Homo sapiens
-
2.5.1.59 MiaPaCa-2 cell
-
 Homo sapiens
-
2.5.1.59 non-small cell lung cancer cell
-
 Homo sapiens
-
2.5.1.59 pancreatic cancer cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.59 geranylgeranyl diphosphate + protein-cysteine
-
 Homo sapiens S-geranylgeranyl-protein + diphosphate
-
 ?
2.5.1.59 geranylgeranyl diphosphate + protein-cysteine the enzyme adds a C20 geranylgeranyl group to proteins such as RhoA, RhoC, Rap1 and Ral at the cysteine within the carboxy-terminal tetrapeptide consensus sequence CAAL (C is cysteine, A is an aliphatic amino acid, and the C-terminal residue is leucine or phenylalanine) Homo sapiens S-geranylgeranyl-protein + diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.59 geranylgeranyltransferase-I
-
 Homo sapiens
2.5.1.59 GGTase I
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
2.5.1.59 malfunction GGTase-I inhibition results in proliferation inhibition associated with G1 arrest and accumulation of cell cycle regulators such as p21CIP1/WAF1 Homo sapiens
2.5.1.59 physiological function importance of GGTase-I in cell proliferation and cell cycle progression Homo sapiens