A5047289790- Trypanosoma species research and implications
- Research on Leishmaniasis Studies
- Biochemical and Molecular Research
- Amoebic Infections and Treatments
- Lipid Membrane Structure and Behavior
- Clostridium difficile and Clostridium perfringens research
- Cellular transport and secretion
- HIV/AIDS drug development and treatment
- Carbohydrate Chemistry and Synthesis
- Photosynthetic Processes and Mechanisms
- Synthesis and Biological Evaluation
- Parasitic Infections and Diagnostics
Novartis (United States)
2019-2024
California State University, East Bay
2021
Millions who live in Latin America and sub-Saharan Africa are at risk of trypanosomatid infections, which cause Chagas disease human African trypanosomiasis (HAT). Improved HAT treatments available, but therapies rely on two nitroheterocycles, suffer from lengthy drug regimens safety concerns that frequent treatment discontinuation. We performed phenotypic screening against trypanosomes identified a class cyanotriazoles (CTs) with potent trypanocidal activity both vitro mouse models HAT....
Diarrhoeal disease caused by Cryptosporidium is a major cause of morbidity and mortality in young malnourished children from low- middle-income countries, with no vaccine or effective treatment. Here we describe the discovery EDI048, PI(4)K inhibitor, designed to be active at infection site gastrointestinal tract undergo rapid metabolism liver. By using mutational analysis crystal structure, show that EDI048 binds highly conserved amino acid residues ATP-binding site. orally efficacious an...
Human African Trypanosomiasis (HAT) is a vector-borne disease caused by kinetoplastid parasites of the Trypanosoma genus. The proceeds in two stages, with hemolymphatic blood stage and meningo-encephalic brain stage. In latter stage, parasite causes irreversible damage to leading sleep cycle disruption fatal if untreated. An orally bioavailable treatment highly desirable. this study, we present brain-penetrant, parasite-selective 20S proteasome inhibitor that was rapidly optimized from an...
ABSTRACT The kinetochore is a macromolecular structure that assembles on the centromeres of chromosomes and provides major attachment point for spindle microtubules during mitosis. In Trypanosoma brucei proteins make up are highly divergent, with inner comprising at least 20 distinct essential (KKT1-20) include four protein kinases, CLK1 (KKT10), CLK2 (KKT19), KKT2 KKT3. We performed phenotypic screen T. bloodstream forms Novartis kinase-focused inhibitor library, which identified number...
unc-11 is the only C. elegans ortholog of mammalian PICALM/AP180, paralogs that play an important role in Clathrin-Mediated Endocytosis (CME) and recycling a subset SNAREs, vesicle-associated membrane proteins (VAMPs). In this publication we report creation new allele endogenously-tagged with GFP just upstream stop codon. Moreover, demonstrate UNC-11::GFP fusion protein functions like wild type expression pattern similar to UNC-11 antibody staining described previously.