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Tag: Belen Cassera

Cripowellins Pause Plasmodium falciparum Intraerythrocytic Development at the Ring Stage

Donna Huber on March 13, 2023

  Cripowellins from Crinum erubescens are known pesticidal and have potent antiplasmodial activity. To gain mechanistic insights to this class of natural products, studies to determine the timing of action of cripowellins within the asexual intraerythrocytic cycle of Plasmodium falciparum were performed and led to the observation that this class of natural products induced reversible cytostasis in the ring …

In Vitro Diagnostic Assay to Detect SARS-CoV-2-Neutralizing Antibody in Patient Sera Using Engineered ACE-2 Mini-Protein

Donna Huber on December 18, 2022

The recent development and mass administration of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) vaccines allowed for disease control, reducing hospitalizations and mortality. Most of these vaccines target the SARS-CoV-2 Spike (S) protein antigens, culminating with the production of neutralizing antibodies (NAbs) that disrupt the attachment of the virus to ACE2 receptors on the host …

Cephalotane-type C20 diterpenoids from Cephalotaxus fortunei var. alpina

Donna Huber on November 4, 2022

Seventeen new cephalotane-type diterpenoids, fortalides A-Q (1-17), along with five known analogues, were isolated from the seeds of Cephalotaxus fortunei var. alpina. Their structures were determined by extensive spectroscopic methods, as well as electronic circular dichroism (ECD) and X-ray crystallographic data analyses. Some isolates exhibited unusual structural features that were first found in cephalotane-type diterpenoids, such as the …

Alkyne modified purines for assessment of activation of Plasmodium vivax hypnozoites and growth of pre-erythrocytic and erythrocytic stages in Plasmodium spp

Donna Huber on April 18, 2022

Malaria is a major global health problem which predominantly afflicts developing countries. Although many antimalarial therapies are currently available, the protozoan parasite causing this disease, Plasmodium spp., continues to evade eradication efforts. One biological phenomenon hampering eradication efforts is the parasite's ability to arrest development, transform into a drug-insensitive form, and then resume growth post-therapy. …

Enantiopure Benzofuran-2-carboxamides of 1-Aryltetrahydro-β-carbolines Are Potent Antimalarials In Vitro

Donna Huber on February 24, 2022

The tetrahydro-β-carboline scaffold has proven fertile ground for the discovery of antimalarial agents (e.g., MMV008138 (1) and cipargamin (2)). Similarity searching of a publicly disclosed collection of antimalarial hits for molecules resembling 1 drew our attention to N2-acyl tetrahydro-β-carboline GNF-Pf-5009 ((±)-3b). Compound purchase, "analog by catalog", and independent synthesis of hits indicated the benzofuran-2-yl amide portion was …

Malaria Box-Inspired Discovery of N-Aminoalkyl-β-carboline-3-carboxamides, a Novel Orally Active Class of Antimalarials

Donna Huber on February 23, 2022

Virtual ligand screening of a publicly available database of antimalarial hits using a pharmacophore derived from antimalarial MMV008138 identified TCMDC-140230, a tetrahydro-β-carboline amide, as worthy of exploration. All four stereoisomers of this structure were synthesized, but none potently inhibited growth of the malaria parasite Plasmodium falciparum. Interestingly, 7e, a minor byproduct of these syntheses, proved to be …

Antimalarial Natural Products

Donna Huber on January 1, 2022

Natural products have made a crucial and unique contribution to human health, and this is especially true in the case of malaria, where the natural products quinine and artemisinin and their derivatives and analogues, have saved millions of lives. The need for new drugs to treat malaria is still urgent, since the most dangerous malaria …

Researchers to test drug candidates to treat malaria

Donna Huber on September 15, 2021

by Donna Huber Belen Cassera is leading a research team that will test two new drugs for the treatment of malaria. The team's work will be funded by a $3.7 million grant from the National Institutes of Health. (Photo credit: Amy Ware) Though malaria was eliminated from the U.S. 70 years ago, the mosquito-borne disease …

Cassera named summer 2021 Innovation Fellow

Donna Huber on August 9, 2021

by Ashley Crain Belen Cassera (Submitted photo) Associate professor Belen Cassera is one step closer to introducing her research to the marketplace. Having spent the summer as UGA’s newest Innovation Fellow, Cassera has learned a lot about how to bring parasitic disease therapeutics arising from her research to market. “In fall 2019, I was among the 18 chosen women …

Belen Cassera named parasitology section editor for Current Clinical Microbiology Reports

Donna Huber on July 8, 2021

Last summer, biochemistry associate professor and Center for Tropical and Emerging Global Diseases member Belen Cassera was named the parasitology section editor for Current Clinical Microbiology Reports and has produced her first issue of reviews. Before former Editor-in-Chief Alan Hudson from Wayne State University School of Medicine stepped down, he recruited Cassera based on a …