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Real-time Cytotoxicity Assays in Human Whole Blood

Real-time Cytotoxicity Assays in Human Whole Blood

Published on: November 7, 2014

Novel trends in high-throughput screening.

Lorenz M Mayr¹, Dejan Bojanic

¹Novartis Institutes for BioMedical Research, Center of Proteomic Chemistry, Protease Platform, Novartis Campus, CH-4002 Basel, Switzerland. Lorenz.Mayr@novartis.com

Current Opinion in Pharmacology

|September 25, 2009

Summary

This summary is machine-generated.

High-throughput screening (HTS) has evolved from increasing capacity to focusing on quality and physiological relevance. Future HTS will emphasize rigorous characterization and tailored strategies for drug discovery.

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Area of Science:

Biochemistry
Pharmacology
Drug Discovery

Background:

High-throughput screening (HTS) is a cornerstone of drug discovery, evolving significantly since the 1990s.
Initially focused on quantitative increases in screening capacity, HTS now prioritizes qualitative improvements in assay content and relevance.

Purpose of the Study:

To review the evolution of HTS over the past decade.
To propose future directions for HTS in biomedical research and pharmaceutical R&D.

Main Methods:

Analysis of technological and process changes in HTS.
Discussion of trends in assay development, chemical characterization, and screening strategies.

Main Results:

A predicted slowdown in extreme miniaturization, with balanced use of various well plate formats.
Increased emphasis on rigorous assay validation, chemical characterization, and orthogonal readout technologies.
Greater adoption of flexible screening approaches (full deck, focused, iterative) and target identification strategies.

Conclusions:

HTS is at a critical juncture, balancing throughput with physiological relevance for enhanced drug discovery productivity.
Future HTS will be more project-specific, customized, and integrated into overall drug discovery pipelines.
Advances in biophysical methodologies and chemical diversity will drive more effective hit identification and validation.