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Accelerating Antimalarial Drug Discovery with a New High-Throughput Screen for Fast-Killing Compounds.
ACS Infect Dis
December 2024
Department of Molecular Infection Dynamics, Institute of Tropical Medicine (NEKKEN), Nagasaki University, Nagasaki 852-8523, Japan.
The urgent need for rapidly acting compounds in the development of antimalarial drugs underscores the significance of such compounds in overcoming resistance issues and improving patient adherence to antimalarial treatments. The present study introduces a high-throughput screening (HTS) approach using 1536-well plates, employing lactate dehydrogenase (PfLDH) combined with nitroreductase (NTR) and fluorescent probes to evaluate inhibition of the growth of the asexual blood stage of malaria parasites. This method was adapted to efficiently assess the speed of action profiling (SAP) in a 384-well plate format, streamlining the traditionally time-consuming screening process.
View Article and Find Full Text PDFHigh-resolution acoustic ejection mass spectrometry for high-throughput library screening.
SLAS Technol
December 2024
SCIEX. Concord, ON. Canada.
An approach is described for high-throughput quality assessment of drug candidate libraries using high-resolution acoustic ejection mass spectrometry (AEMS). Sample introduction from 1536-well plates is demonstrated for this application using 2.5 nL acoustically dispensed sample droplets into an Open Port Interface (OPI) with pneumatically assisted electrospray ionization at a rate of one second per sample.
View Article and Find Full Text PDFUnlocking Intracellular Protein Delivery by Harnessing Polymersomes Synthesized at Microliter Volumes using Photo-PISA.
Adv Mater
December 2024
Department of Materials, Department of Bioengineering, and Institute of Biomedical Engineering, Imperial College London, London, SW7 2AZ, UK.
Efficient delivery of therapeutic proteins and vaccine antigens to intracellular targets is challenging due to generally poor cell membrane permeation and endolysosomal entrapment causing degradation. Herein, these challenges are addressed by developing an oxygen-tolerant photoinitiated polymerization-induced self-assembly (Photo-PISA) process, allowing for the microliter-scale (10 µL) synthesis of protein-loaded polymersomes directly in 1536-well plates. High-resolution techniques capable of analysis at a single particle level are employed to analyze protein encapsulation and release mechanisms.
View Article and Find Full Text PDFUsing Reporter Gene Assays to Screen and Identify Chemical Compounds that Modulate Estrogen Receptor Activity.
Curr Protoc
October 2024
National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland.
Estrogen receptor alpha (ERα) is a nuclear receptor that is expressed mainly in the breast, uterus, and ovary, among several other organs. ERα plays important roles in reproduction, mammary gland formation, and glucose homeostasis. Disruption of ERα may result in adverse outcomes, such as cancer, impaired fertility, and abnormal fetal growth.
View Article and Find Full Text PDFSimultaneous screening for selective SARS-CoV-2, Lassa, and Machupo virus entry inhibitors.
SLAS Discov
September 2024
Department of Molecular Medicine, Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, 130 Scripps Way, Jupiter, FL 33458, United States. Electronic address:
Article Synopsis
- Emerging highly pathogenic viruses, such as SARS-CoV-2, Lassa virus, and Machupo virus, pose significant risks to global health, prompting initiatives like the establishment of Antiviral Drug Discovery centers by NIAID.
- Researchers developed paired entry assays to screen approximately 650,000 compounds using a dual pseudotyped virus infection system, achieving an extensive ultra-high throughput screening with over 2.4 million wells tested.
- The screening identified a total of 1812, 1506, and 2586 unique hits for LASV, MACV, and SARS2, respectively, and confirmed several promising compounds with low cytotoxicity and strong antiviral activity, with some compounds showing IC
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