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Literature summary for 2.1.1.41 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
Search for more literature for 2.1.1.41

Application

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

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
22,26-azasterol
-
 Trypanosoma brucei brucei
22,26-azasterol
-
 Trypanosoma brucei rhodesiense
azasterol
-
 Trypanosoma brucei brucei
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
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
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
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
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
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
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
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

Organism UniProt Comment Textmining
Trypanosoma brucei brucei Q45KX5
-
-
Trypanosoma brucei brucei 427 Q45KX5
-
-
Trypanosoma brucei rhodesiense
-
-
-
Trypanosoma brucei rhodesiense STIB900
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
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]

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

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

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