CYP51 as drug targets for fungi and protozoan parasites: past, present and future

GI Lepesheva, L Friggeri, MR Waterman - Parasitology, 2018 - cambridge.org
The efficiency of treatment of human infections with the unicellular eukaryotic pathogens
such as fungi and protozoa remains deeply unsatisfactory. For example, the mortality rates …

Free Radical Metabolites in the Mode of Action of Chemotherapeutic Agents and Phagocytic Cells on Trypanosoma cruzi

R Docampo, SNJ Moreno - Reviews of infectious diseases, 1984 - academic.oup.com
There are a number of biologic oxidations in Trypanosoma cruzi that generate O2-and/or
H2O2. In addition, intracellular reduction followed by autoxidation yielding O2-and H2O2 …

Design, Synthesis, and Biological Evaluation of Aryloxyethyl Thiocyanate Derivatives against Trypanosoma cruzi

E Elhalem, BN Bailey, R Docampo… - Journal of medicinal …, 2002 - ACS Publications
As a continuation of our project aimed at the search for new and safe chemotherapeutic and
chemoprophylactic agents against American trypanosomiasis (Chagas' disease), several …

Current status of Chagas disease chemotherapy

PMM Guedes, GK Silva, FRS Gutierrez… - Expert review of anti …, 2011 - Taylor & Francis
Chagas disease affects 7.7 million people and 28 million people are at risk of acquiring the
disease in 15 endemic countries of Latin America. Benznidazole and nifurtimox are drugs …

Structural insights into inhibition of sterol 14α-demethylase in the human pathogen Trypanosoma cruzi

GI Lepesheva, TY Hargrove, S Anderson… - Journal of Biological …, 2010 - ASBMB
Trypanosoma cruzi causes Chagas disease (American trypanosomiasis), which threatens
the lives of millions of people and remains incurable in its chronic stage. The antifungal drug …

[HTML][HTML] Recent developments in sterol 14-demethylase inhibitors for Chagas disease

FS Buckner, JA Urbina - International Journal for Parasitology: Drugs and …, 2012 - Elsevier
The protozoan parasite, Trypanosoma cruzi, causes the most prevalent parasitic infection in
the American continent. It gives rise to life-long infection in humans and results in severe …

Sterol 14alpha-demethylase (CYP51) as a therapeutic target for human trypanosomiasis and leishmaniasis

G I. Lepesheva, M R. Waterman - Current topics in medicinal …, 2011 - benthamdirect.com
Pathogenic protozoa threaten lives of several hundred million people throughout the world
and are responsible for large numbers of deaths globally. The parasites are transmitted to …

Sterol 14α-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth

GI Lepesheva, RD Ott, TY Hargrove, YY Kleshchenko… - Chemistry & biology, 2007 - cell.com
Summary Sterol 14α-demethylases (CYP51) serve as primary targets for antifungal drugs,
and specific inhibition of CYP51s in protozoan parasites Trypanosoma brucei (TB) and …

Targeting Trypanosoma cruzi sterol 14α-demethylase (CYP51)

GI Lepesheva, F Villalta, MR Waterman - Advances in parasitology, 2011 - Elsevier
There are at least two obvious features that must be considered upon targeting specific
metabolic pathways/enzymes for drug development: the pathway must be essential and the …

Ultrastructural alterations induced by two ergosterol biosynthesis inhibitors, ketoconazole and terbinafine, on epimastigotes and amastigotes of Trypanosoma …

K Lazardi, JA Urbina, W De Souza - Antimicrobial agents and …, 1990 - Am Soc Microbiol
We report the ultrastructural alterations induced during the proliferative stages of
Trypanosoma (Schizotrypanum) cruzi, the causative agent of Chagas' disease, by two …