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Literature summary extracted from

  • Oliaro-Bosso, S.; Viola, F.; Matsuda, S.; Cravotto, G.; Tagliapietra, S.; Balliano, G.
    Umbelliferone aminoalkyl derivatives as inhibitors of oxidosqualene cyclases from Saccharomyces cerevisiae, Trypanosoma cruzi, and Pneumocystis carinii (2004), Lipids, 39, 1007-1012.
    View publication on PubMed

Application

EC Number Application Comment Organism
5.4.99.7 drug development results identify a particularly promising new family of OSC inhibitors, for the development of novel antiparasitic agents Saccharomyces cerevisiae
5.4.99.7 drug development results identify a particularly promising new family of OSC inhibitors, for the development of novel antiparasitic agents Trypanosoma cruzi
5.4.99.7 drug development results identify a particularly promising new family of OSC inhibitors, for the development of novel antiparasitic agents Pneumocystis carinii

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.4.99.7
-
 Saccharomyces cerevisiae
5.4.99.7 expression in Saccharomyces cerevisiae Trypanosoma cruzi
5.4.99.7 expression in Saccharomyces cerevisiae Pneumocystis carinii

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.4.99.7 3-beta-(beta-dimethylaminoethoxy)-androst-5en-17one DMAE-DHA Pneumocystis carinii
5.4.99.7 3-beta-(beta-dimethylaminoethoxy)-androst-5en-17one DMAE-DHA Saccharomyces cerevisiae
5.4.99.7 3-beta-(beta-dimethylaminoethoxy)-androst-5en-17one DMAE-DHA Trypanosoma cruzi
5.4.99.7 7-(4-allylmethylamino-but-2-ynyloxy)chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-(4-allylmethylamino-but-2-ynyloxy)chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-(4-allylmethylamino-but-2-ynyloxy)chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 7-(morpholinyl-N-hexyloxy)chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-(morpholinyl-N-hexyloxy)chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-(morpholinyl-N-hexyloxy)chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 7-(morpholinyl-N-octanyloxy)chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-(morpholinyl-N-octanyloxy)chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-(morpholinyl-N-octanyloxy)chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 7-(piperidinyl-N-hexyloxy)chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-(piperidinyl-N-hexyloxy)chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-(piperidinyl-N-hexyloxy)chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 7-[10-(allylmethylamino)-decyloxy]chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-[10-(allylmethylamino)-decyloxy]chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-[10-(allylmethylamino)-decyloxy]chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 7-[4'-(N-diethylamino)-but-2-ynyloxy]chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-[4'-(N-diethylamino)-but-2-ynyloxy]chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-[4'-(N-diethylamino)-but-2-ynyloxy]chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 7-[4'-(N-pyrrolidyn)-but-2-ynyloxy]chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-[4'-(N-pyrrolidyn)-but-2-ynyloxy]chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-[4'-(N-pyrrolidyn)-but-2-ynyloxy]chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 7-[6-(allylmethylamino)-hexyloxy]-chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-[6-(allylmethylamino)-hexyloxy]-chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-[6-(allylmethylamino)-hexyloxy]-chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 7-[8'(dimethylamino-N-octyloxy)]chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 7-[8'(dimethylamino-N-octyloxy)]chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 7-[8'(dimethylamino-N-octyloxy)]chromen-2-one
-
 Trypanosoma cruzi

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
5.4.99.7 spheroplast
-
 Saccharomyces cerevisiae
-
-
5.4.99.7 spheroplast
-
 Trypanosoma cruzi
-
-
5.4.99.7 spheroplast
-
 Pneumocystis carinii
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.4.99.7 2,3-oxidosqualene Saccharomyces cerevisiae
-
 lanosterol
-
 ?
5.4.99.7 2,3-oxidosqualene Trypanosoma cruzi
-
 lanosterol
-
 ?
5.4.99.7 2,3-oxidosqualene Pneumocystis carinii
-
 lanosterol
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
5.4.99.7 Pneumocystis carinii
-
-
-
5.4.99.7 Saccharomyces cerevisiae
-
-
-
5.4.99.7 Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.4.99.7 2,3-oxidosqualene
-
 Saccharomyces cerevisiae lanosterol
-
 ?
5.4.99.7 2,3-oxidosqualene
-
 Trypanosoma cruzi lanosterol
-
 ?
5.4.99.7 2,3-oxidosqualene
-
 Pneumocystis carinii lanosterol
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.4.99.7 OSC
-
 Saccharomyces cerevisiae
5.4.99.7 OSC
-
 Trypanosoma cruzi
5.4.99.7 OSC
-
 Pneumocystis carinii
5.4.99.7 Oxidosqualene cyclase
-
 Saccharomyces cerevisiae
5.4.99.7 Oxidosqualene cyclase
-
 Trypanosoma cruzi
5.4.99.7 Oxidosqualene cyclase
-
 Pneumocystis carinii

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
5.4.99.7 additional information
-
 7-(4-allylmethylamino-but-2-ynyloxy)chromen-2-one above 0.1 mM Trypanosoma cruzi
5.4.99.7 additional information
-
 7-(piperidinyl-N-hexyloxy)chromen-2-one above 0.1 mM Trypanosoma cruzi
5.4.99.7 0.00015
-
 7-[6-(allylmethylamino)-hexyloxy]-chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.00018
-
 7-[10-(allylmethylamino)-decyloxy]chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.00052
-
 7-[4'-(N-pyrrolidyn)-but-2-ynyloxy]chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.00104
-
 7-[8'(dimethylamino-N-octyloxy)]chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.00104
-
 7-[6-(allylmethylamino)-hexyloxy]-chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.00112
-
 7-(4-allylmethylamino-but-2-ynyloxy)chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.00185
-
 7-[4'-(N-diethylamino)-but-2-ynyloxy]chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.00248
-
 7-(piperidinyl-N-hexyloxy)chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.00321
-
 7-[10-(allylmethylamino)-decyloxy]chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.00342
-
 7-(4-allylmethylamino-but-2-ynyloxy)chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.00406
-
 7-[6-(allylmethylamino)-hexyloxy]-chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 0.00414
-
 7-[10-(allylmethylamino)-decyloxy]chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 0.00535
-
 7-(morpholinyl-N-octanyloxy)chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.00603
-
 7-[8'(dimethylamino-N-octyloxy)]chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.01028
-
 7-[4'-(N-pyrrolidyn)-but-2-ynyloxy]chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.02035
-
 7-[4'-(N-diethylamino)-but-2-ynyloxy]chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.02543
-
 7-[8'(dimethylamino-N-octyloxy)]chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 0.03067
-
 7-(morpholinyl-N-octanyloxy)chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.03154
-
 7-(piperidinyl-N-hexyloxy)chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.07266
-
 7-[4'-(N-diethylamino)-but-2-ynyloxy]chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 0.07876
-
 7-(morpholinyl-N-hexyloxy)chromen-2-one
-
 Pneumocystis carinii
5.4.99.7 0.09583
-
 7-(morpholinyl-N-hexyloxy)chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 0.1024
-
 7-(morpholinyl-N-octanyloxy)chromen-2-one
-
 Trypanosoma cruzi
5.4.99.7 0.1028
-
 7-(morpholinyl-N-hexyloxy)chromen-2-one
-
 Saccharomyces cerevisiae
5.4.99.7 0.1063
-
 7-[4'-(N-pyrrolidyn)-but-2-ynyloxy]chromen-2-one
-
 Trypanosoma cruzi