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Literature summary for 2.5.1.58 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
Search for more literature for 2.5.1.58

Application

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Rattus norvegicus

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
PFTase
-
 Rattus norvegicus
protein farnesyltransferase
-
 Rattus norvegicus

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

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