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Literature summary extracted from

  • Gros, L.; Castillo-Acosta, V.M.; Jimenez, C.J.; Sealey-Cardona, M.; Vargas, S.; Estevez, A.M.; Yardley, V.; Rattray, L.; Croft, S.L.; Ruiz-Perez, L.M.; Urbina, J.A.; Gilbert, I.H.; Gonzalez-Pacanowska, D.
    New azasterols against Trypanosoma brucei: role of 24-sterol methyltransferase in inhibitor action (2006), Antimicrob. Agents Chemother., 50, 2595-2601.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.1.1.41 drug development newly synthesized azasterol derivates act at sites other than 24-SMT in Trypanosoma brucei Trypanosoma brucei rhodesiense
2.1.1.41 drug development newly synthesized azasterol derivates act at sites other than 24-SMT in Trypanosoma brucei Trypanosoma brucei brucei

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.1.1.41 into pET28a(+) and expressed with a His tag at the amino terminus in Escherichia coli BL21(DE3) Trypanosoma brucei brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.41 22,26-azasterol
-
 Trypanosoma brucei brucei
2.1.1.41 22,26-azasterol
-
 Trypanosoma brucei rhodesiense
2.1.1.41 azasterol
-
 Trypanosoma brucei brucei
2.1.1.41 methyl ([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)acetate
-
 Trypanosoma brucei rhodesiense
2.1.1.41 methyl 3-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)propanoate
-
 Trypanosoma brucei rhodesiense
2.1.1.41 methyl 4-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)butanoate
-
 Trypanosoma brucei rhodesiense
2.1.1.41 methyl 5-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)pentanoate
-
 Trypanosoma brucei rhodesiense
2.1.1.41 methyl 6-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)hexanoate
-
 Trypanosoma brucei rhodesiense
2.1.1.41 methyl 7-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)heptanoate
-
 Trypanosoma brucei rhodesiense
2.1.1.41 methyl 8-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)octanoate
-
 Trypanosoma brucei rhodesiense
2.1.1.41 additional information newly synthesized azasterols methyl ([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)acetate, methyl 3-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)propanoate, methyl 4-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)butanoate, methyl 5-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)pentanoate, methyl 6-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)hexanoate, methyl 7-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)heptanoate, and methyl 8-([2-[(3S,8S,9S,10R,13S,14S,17R)-3-(acetyloxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]propyl]amino)octanoate, none show any significant inhibition against the recombinant enzyme Trypanosoma brucei brucei

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.41 Trypanosoma brucei brucei Q45KX5
-
-
2.1.1.41 Trypanosoma brucei brucei 427 Q45KX5
-
-
2.1.1.41 Trypanosoma brucei rhodesiense
-
-
-
2.1.1.41 Trypanosoma brucei rhodesiense STIB900
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.41 additional information approximately 3fold higher levels are present in procyclic forms than in bloodstream forms, existence of active enzyme in both forms of the parasite Trypanosoma brucei brucei
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.1.1.41 0.00000082
-
 bloodstream forms Trypanosoma brucei brucei
2.1.1.41 0.00000217
-
 procyclic forms Trypanosoma brucei brucei

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.41 desmosterol + S-adenosyl-L-methionine
-
 Trypanosoma brucei rhodesiense 24-methylenedesmosterol + S-adenosyl-L-homocysteine
-
 ?
2.1.1.41 desmosterol + S-adenosyl-L-methionine
-
 Trypanosoma brucei brucei 24-methylenedesmosterol + S-adenosyl-L-homocysteine
-
 ?
2.1.1.41 desmosterol + S-adenosyl-L-methionine
-
 Trypanosoma brucei rhodesiense STIB900 24-methylenedesmosterol + S-adenosyl-L-homocysteine
-
 ?
2.1.1.41 desmosterol + S-adenosyl-L-methionine
-
 Trypanosoma brucei brucei 427 24-methylenedesmosterol + S-adenosyl-L-homocysteine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.1.1.41 24-SMT
-
 Trypanosoma brucei rhodesiense
2.1.1.41 24-SMT
-
 Trypanosoma brucei brucei
2.1.1.41 DELTA24-sterol methyltransferase
-
 Trypanosoma brucei rhodesiense
2.1.1.41 DELTA24-sterol methyltransferase
-
 Trypanosoma brucei brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.1.1.41 0.00176
-
 recombinant enzyme Trypanosoma brucei brucei azasterol
2.1.1.41 0.00243
-
 native enzyme Trypanosoma brucei brucei azasterol