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Tag: Dennis Kyle

Unlocking the potential of ommatins as sustainable photosensitizers for photodynamic therapy

Donna Huber on July 17, 2026

Photodynamic therapy (PDT) has demonstrated efficacy in cancer treatment, with recent advancements concentrating on photosensitizers that generate high levels of reactive oxygen species (ROS) upon light irradiation while exhibiting minimal dark toxicity. In this study, we explored the photophysical properties of ommatins, specifically xanthommatin (Xa), decarboxylated xanthommatin (Dc-Xa), and protected uncyclized xanthommatin (Uc-Xa), and assessed …

Structure-Guided Optimization of Novel Inhibitors of Plasmodium Lysyl-tRNA Synthetase with Multistage Activity against Malaria Parasites

Donna Huber on June 2, 2026

A fused dihydropyrrolidino-pyrimidine hit with low lipophilicity and excellent ligand efficiency was identified in a biochemical screen of the Global Health Chemical Diversity Library (GHCDL) against Plasmodium lysyl-tRNA synthetase (KRS). Structure-guided lead optimization delivered analogues with potent parasite growth inhibition, excellent biochemical and cellular selectivity (>1000-fold), and oral efficacy in the malaria NOD-scid-IL2Rγnull (SCID) mouse model. Structural …

Characterization of β-Carboline Derivatives Reveals a High Barrier to Resistance and Potent Activity against Ring-Stage and DHA-Induced Dormant Plasmodium falciparum

Donna Huber on October 17, 2025

Malaria, caused by Plasmodium falciparum, remains a major global health challenge, with an estimated 263 million new infections and 597,000 deaths annually. Increasing resistance to current antimalarial drugs underscores the urgent need for new therapeutics that target novel pathways in the parasite. We previously reported a novel class of β-carboline antimalarials, exemplified by PRC1584, which demonstrated …

In the News: Dennis Kyle

Donna Huber on July 3, 2025

Brain-eating amoebas are rare. But hot weather increases the risk (Washington Post) Brain-eating amoeba: Who is most often infected? (Rochester First) (CBS42) (The Hill)

Discovery and optimization of a novel carboxamide scaffold with selective antimalarial activity

Donna Huber on March 28, 2025

Artemisinin combination therapies (ACTs) are critical components of malaria control worldwide. Alarmingly, ACTs have begun to fail, owing to the rise in artemisinin resistance. Thus, there is an urgent need for an expanded set of novel antimalarials to generate new combination therapies. Herein, we have identified a 1,2,4-triazole-containing carboxamide scaffold that, through scaffold hopping efforts, …

Type I interferons induce guanylate-binding proteins and lysosomal defense in hepatocytes to control malaria

Donna Huber on March 25, 2025

Plasmodium parasites undergo development and replication within hepatocytes before infecting erythrocytes and initiating clinical malaria. Although type I interferons (IFNs) are known to hinder Plasmodium infection within the liver, the underlying mechanisms remain unclear. Here, we describe two IFN-I-driven hepatocyte antimicrobial programs controlling liver-stage malaria. First, oxidative defense by NADPH oxidases 2 and 4 triggers …

Screening the Global Health Priority Box against Plasmodium berghei liver stage parasites using an inexpensive luciferase detection protocol

Donna Huber on November 23, 2024

Background: Malaria, a disease caused by parasites of the genus Plasmodium, continues to impact many regions globally. The rise in resistance to artemisinin-based anti-malarial drugs highlights the need for new treatments. Ideally, new anti-malarials will kill the asymptomatic liver stages as well as the symptomatic blood stages. While blood stage screening assays are routine and efficient, …

In the news: Dennis Kyle

Donna Huber on July 8, 2024

  Dennis Kyle is the Director of CTEGD and the GRA Eminent Scholar in Antiparasitic Drug Discovery in the Departments of Cellular Biology and Infectious Diseases. Brain-eating amoeba: Will the warming climate bring more cases? (MSN)

Optimization of diastereomeric dihydropyridines as antimalarials

Donna Huber on June 18, 2024

The increase in research funding for the development of antimalarials since 2000 has led to a surge of new chemotypes with potent antimalarial activity. High-throughput screens have delivered several thousand new active compounds in several hundred series, including the 4,7-diphenyl-1,4,5,6,7,8-hexahydroquinolines, hereafter termed dihydropyridines (DHPs). We optimized the DHPs for antimalarial activity. Structure-activity relationship studies focusing …