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Literature summary extracted from

  • DeGraw, A.J.; Keiser, M.J.; Ochocki, J.D.; Shoichet, B.K.; Distefano, M.D.
    Prediction and evaluation of protein farnesyltransferase inhibition by commercial drugs (2010), J. Med. Chem., 53, 2464-2471.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.5.1.58 medicine inhibition of protein farnesyltransferase with influence for oncogenesis, potential target for treatment of cancer Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.58 desloratadine
-
 Rattus norvegicus
2.5.1.58 econazole
-
 Rattus norvegicus
2.5.1.58 loratadine
-
 Rattus norvegicus
2.5.1.58 miconazole
-
 Rattus norvegicus
2.5.1.58 rupatadine
-
 Rattus norvegicus
2.5.1.58 ubenimex
-
 Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.58 Rattus norvegicus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.5.1.58
-
 Rattus norvegicus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.58 farnesyl diphosphate + N-dansyl-GCVLS assay at pH 7.5, 30°C Rattus norvegicus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.58 PFTase
-
 Rattus norvegicus
2.5.1.58 protein farnesyltransferase
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.5.1.58 30
-
 assay at Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.5.1.58 7.5
-
 assay at Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.58 0.0133
-
-
 Rattus norvegicus loratadine
2.5.1.58 0.0189
-
-
 Rattus norvegicus miconazole
2.5.1.58 0.0233
-
-
 Rattus norvegicus econazole
2.5.1.58 0.076
-
-
 Rattus norvegicus rupatadine
2.5.1.58 0.1
-
 value above Rattus norvegicus desloratadine
2.5.1.58 0.2
-
 value above Rattus norvegicus ubenimex