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Literature summary extracted from

  • Samanta, A.; Leonidas, D.D.; Dasgupta, S.; Pathak, T.; Zographos, S.E.; Oikonomakos, N.G.
    Morpholino, piperidino, and pyrrolidino derivatives of pyrimidine nucleosides as inhibitors of ribonuclease A: synthesis, biochemical, and crystallographic evaluation (2009), J. Med. Chem., 52, 932-942.
    View publication on PubMed

Application

EC Number Application Comment Organism
4.6.1.18 pharmacology inhibitors can be the starting point for the development of compounds that can be used as pharmaceuticals against pathologies associated with ribonuclease A homologues such as human angiogenin, which is implicated in tumor induced neovascularization Bos taurus

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
4.6.1.18 vapor diffusion, hanging drop, PEG 4000, sodium citrate, pH 5.5, 289 K, space group C121,ribonuclease A-1-{5-deoxy-5-[4-(ethoxycarbonyl)piperidin-1-yl]-alpha-L-arabinofuranosyl}pyrimidine-2,4(1H,3H)-dione complex, resolution 1.58 A, ribonuclease A-1-(5-deoxy-5-morpholin-4-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione, resolution 1.60 A, ribonuclease A-1-(5-deoxy-5-piperidin-1-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione, resolution 1.60 A, ribonuclease A-1-(5-deoxy-5-pyrrolidin-1-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione, resolution 1.60 A, ribonuclease A-5’-deoxy-5’-piperidin-1-ylthymidine, resolution 1.72 A, ribonuclease A-1-(2,5-dideoxy-5-pyrrolidin-1-yl-beta-L-erythro-pentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione, resolution 1.98 A Bos taurus

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.6.1.18 1-(2,5-dideoxy-5-pyrrolidin-1-yl-beta-L-erythro-pentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 1-(5-deoxy-5-morpholin-4-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 1-(5-deoxy-5-piperidin-1-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 1-(5-deoxy-5-pyrrolidin-1-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 1-(5-deoxy-5-[4-(ethoxycarbonyl)piperidin-1-yl]-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 5'-deoxy-5'-piperidin-1-ylthymidine
-
 Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
4.6.1.18 Bos taurus P61823
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
4.6.1.18 commercial preparation
-
 Bos taurus
-

Synonyms

EC Number Synonyms Comment Organism
4.6.1.18 ribonuclease A
-
 Bos taurus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
4.6.1.18 0.077
-
 1-(5-deoxy-5-[4-(ethoxycarbonyl)piperidin-1-yl]-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 0.172
-
 1-(5-deoxy-5-piperidin-1-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 0.179
-
 1-(5-deoxy-5-morpholin-4-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 0.203
-
 1-(5-deoxy-5-pyrrolidin-1-yl-alpha-L-arabinofuranosyl)pyrimidine-2,4(1H,3H)-dione
-
 Bos taurus
4.6.1.18 0.396
-
 5'-deoxy-5'-piperidin-1-ylthymidine
-
 Bos taurus
4.6.1.18 0.423
-
 1-(2,5-dideoxy-5-pyrrolidin-1-yl-beta-L-erythro-pentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione
-
 Bos taurus