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Sterol 14-alpha demethylase
A protein that is a translation product of any of the 2 copies of the CYP51 gene in Trypanosoma cruzi strain CL Brener. [PRO:DNx, UniProtKB:Q7Z1V1]
Synonyms
Tc14DM;
EC 1.14.14.154;
Cytochrome P450 51;
Lanosterol 14-alpha demethylase
Research
Bioassay Publications (8)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (12.50) | 29.6817 |
2010's | 4 (50.00) | 24.3611 |
2020's | 3 (37.50) | 2.80 |
Compounds (10)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
fluconazole | Trypanosoma cruzi strain CL Brener | Kd | 0.2575 | 3 | 4 |
ketoconazole | Trypanosoma cruzi strain CL Brener | Kd | 1.1600 | 1 | 2 |
posaconazole | Trypanosoma cruzi strain CL Brener | Kd | 0.0390 | 2 | 2 |
Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.European journal of medicinal chemistry, , Apr-10, Volume: 149, 2018
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.Journal of medicinal chemistry, , Feb-12, Volume: 58, Issue:3, 2015
Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth.Chemistry & biology, , Volume: 14, Issue:11, 2007
Examination of multiple Trypanosoma cruzi targets in a new drug discovery approach for Chagas disease.Bioorganic & medicinal chemistry, , 03-15, Volume: 58, 2022
A new chemotype with promise against Trypanosoma cruzi.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 30, Issue:1, 2020
Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.European journal of medicinal chemistry, , Apr-10, Volume: 149, 2018
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013