Literature summary for 1.14.14.154 extracted from

Lepesheva, G.I.; Hargrove, T.Y.; Anderson, S.; Kleshchenko, Y.; Furtak, V.; Wawrzak, Z.; Villalta, F.; Waterman, M.R.
Structural insights into inhibition of sterol 14alpha-demethylase in the human pathogen Trypanosoma cruzi (2010), J. Biol. Chem., 285, 25582-25590.

Search for more literature for 1.14.14.154

Cloned(Commentary)

Cloned (Comment)	Organism
expression of C-terminally His-tagged wild-type and mutant enzymes	Trypanosoma cruzi

Crystallization (Commentary)

Crystallization (Comment)	Organism
purified recombinant C-terminally His-tagged enzyme, for crystallization purposes, the N-terminal transmembrane domain upstream of Pro32 is replaced with MAKKTSSKGKL- in the construct used for co-crystallization with fluconazole and (R)-4'-chloro-N-(1-(2,4-dichlorophenyl)-2-(1H-imid-azol-1-yl)ethyl)biphenyl-4-carboxamide, and with MAKKT-(5'-ATGGTCAAGAAAACG-3') in the complex with posaconazole, hanging drop vapour diffusion method, 25°C, from 0.260 mM cytochrome P450 solution in 20 mM potassium phosphate buffer, pH 7.2, containing 200 mM NaCl, 0.1 mM EDTA,10% glycerol, and 0.048mMn-tridecyl-beta-D-maltoside preincubated with 1.2fold molar excess of posaconazole, or (R)-4'-chloro-N-(1-(2,4-dichlorophenyl)-2-(1H-imid-azol-1-yl)ethyl)biphenyl-4-carboxamide, and 2-fold molar excess of fluconazole against an equal volume of well solution containing 0.2 M potassium formate, pH 7.2, or 0.2 M sodium formate, pH 7.4, in the case of (R)-4'-chloro-N-(1-(2,4-dichlorophenyl)-2-(1H-imid-azol-1-yl)ethyl)biphenyl-4-carboxamide, and 15% w/v PEG 3550, X-ray diffraction structure determination and analysis, modelling	Trypanosoma cruzi

Crystallization (Comment)

Organism

purified recombinant C-terminally His-tagged enzyme, for crystallization purposes, the N-terminal transmembrane domain upstream of Pro32 is replaced with MAKKTSSKGKL- in the construct used for co-crystallization with fluconazole and (R)-4'-chloro-N-(1-(2,4-dichlorophenyl)-2-(1H-imid-azol-1-yl)ethyl)biphenyl-4-carboxamide, and with MAKKT-(5'-ATGGTCAAGAAAACG-3') in the complex with posaconazole, hanging drop vapour diffusion method, 25°C, from 0.260 mM cytochrome P450 solution in 20 mM potassium phosphate buffer, pH 7.2, containing 200 mM NaCl, 0.1 mM EDTA,10% glycerol, and 0.048mMn-tridecyl-beta-D-maltoside preincubated with 1.2fold molar excess of posaconazole, or (R)-4'-chloro-N-(1-(2,4-dichlorophenyl)-2-(1H-imid-azol-1-yl)ethyl)biphenyl-4-carboxamide, and 2-fold molar excess of fluconazole against an equal volume of well solution containing 0.2 M potassium formate, pH 7.2, or 0.2 M sodium formate, pH 7.4, in the case of (R)-4'-chloro-N-(1-(2,4-dichlorophenyl)-2-(1H-imid-azol-1-yl)ethyl)biphenyl-4-carboxamide, and 15% w/v PEG 3550, X-ray diffraction structure determination and analysis, modelling

Trypanosoma cruzi

Inhibitors

Inhibitors	Comment	Organism
(R)-4'-chloro-N-(1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethyl)biphenyl-4-carboxamide	VNF, complexes CYP51, binding structure, overview	Trypanosoma cruzi
fluconazole	complexes CYP51, binding structure, overview	Trypanosoma cruzi
posaconazole	complexes CYP51, binding structure, overview	Trypanosoma cruzi

Organism

Organism	UniProt	Comment	Textmining
Trypanosoma cruzi	Q7Z1V1	gene CYP51	-

Purification (Commentary)

Purification (Comment)	Organism
recombinant C-terminally His-tagged wild-type and mutant enzymes by nickel affinity chromatography and gel filtration	Trypanosoma cruzi

Synonyms

Synonyms	Comment	Organism
14DM	-	Trypanosoma cruzi
CYP51	-	Trypanosoma cruzi
sterol 14alpha-demethylase	-	Trypanosoma cruzi
TC14DM	-	Trypanosoma cruzi