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Literature summary for 4.6.1.18 extracted from

  • Vert, A.; Castro, J.; Ruiz-Martinez, S.; Tubert, P.; Escribano, D.; Ribo, M.; Vilanova, M.; Benito, A.
    Generation of new cytotoxic human ribonuclease variants directed to the nucleus (2012), Mol. Pharm., 9, 2894-2902.
    View publication on PubMed
Search for more literature for 4.6.1.18

Application

Application Comment Organism
drug development the enzyme is an antitumor drug candidate Homo sapiens
medicine ribonuclease PE5 is a promising agent for use in anticancer therapy Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of enzyme mutants in Escherichia coli strain BL21(DE3) Homo sapiens

Protein Variants

Protein Variants Comment Organism
G89R/S90R site-directed mutagenesis of mutant PE9 Homo sapiens
additional information engineering a nuclear localization signal into the sequence of the human pancreatic ribonucleases as a strategy to endow this enzyme with cytotoxic activity against tumor cells and to improve the efficiency of the enzyme as an antitumor drug candidate. Generation of mutant PE5 variants carrying an additional NLS or a scrambled NLS sequence Homo sapiens
R4A/K6A/G89R/S90R site-directed mutagenesis of mutant PE10 Homo sapiens
R4A/K6A/Q9E/D16G/S17N/G89R/S90R site-directed mutagenesis, mutant PE5 is constructed from PM5 replacing Gly89 and Ser90 by Arg. PM5 codes for HP-RNase and incorporates the substitutions Arg4 and Lys6 to Ala, Gln9 to Glu, Asp16 to Gly, and Ser17 to Asn Homo sapiens
R4A/K6A/Q9E/D16G/S17N/R31E/R91A site-directed mutagenesis,mutant PE3 is constructed from PM5 replacing Arg31 and Arg91 by Glu and Ala, respectively. PM5 codes for HP-RNase and incorporates the substitutions Arg4 and Lys6 to Ala, Gln9 to Glu, Asp16 to Gly, and Ser17 to Asn Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
cytidine 2',3'-cyclic monophosphate substrate inhibition of PE5 mutant enzyme variants at higher substrate concentration Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information cytidine 2',3'-cyclic monophosphate is used as substrate Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
PE5
-
 Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
4
-
 assay at Homo sapiens

General Information

General Information Comment Organism
evolution the enzyme is a member of the pancreatic ribonuclease (RNase) superfamily Homo sapiens
physiological function cytotoxic human pancreatic ribonuclease variant PE5 is able to cleave nuclear RNA, inducing the apoptosis of cancer cells and reducing the amount of P-glycoprotein in different multidrug-resistant cell lines Homo sapiens