Impact of high-throughput screening in biomedical research

  title={Impact of high-throughput screening in biomedical research},
  author={Ricardo Macarr{\'o}n and Martyn N. Banks and Dejan Bojanic and David J. Burns and Dragan A. Cirovic and Tina Garyantes and Darren V. S. Green and Robert P. Hertzberg and William P. Janzen and Jeff W. Paslay and Ulrich Schopfer and G. Sitta Sittampalam},
  journal={Nature Reviews Drug Discovery},
High-throughput screening (HTS) has been postulated in several quarters to be a contributory factor to the decline in productivity in the pharmaceutical industry. Moreover, it has been blamed for stifling the creativity that drug discovery demands. In this article, we aim to dispel these myths and present the case for the use of HTS as part of a proven scientific tool kit, the wider use of which is essential for the discovery of new chemotypes. 

High‐throughput screening (HTS) for the identification of novel antiviral scaffolds

  • M. Jadhav
  • Biology
    Clinical pharmacology in drug development
  • 2014
High-throughput screening (HTS) is an atomized technology for rapidly analyzing the activity of hundreds and thousands of chemical compounds and how it can assist in finding antiviral drugs in the twenty-first century is shed.

Screening-based translation of public research encounters painful problems.

  • J. Baell
  • Chemistry
    ACS medicinal chemistry letters
  • 2015
Whether identified through high throughput screening or in silico screening, and whether target-based or phenotypic, sets of hits will contain chemical con artists. Such pan-assay interference

High-Throughput Screening: What are we missing?

By reflecting on the hits and misses of HTS in this editorial, three personal perspectives on how screening efforts can be made more fruitful are offered.

Resurgence of Phenotypic Screening for Discovering Drug Leads

Phenotypic screenings became the methods of choice for drug discovery for decades because of the ease of application, simplicity and rapid findings of such methods.

Challenges in Secondary Analysis of High Throughput Screening Data

This work examines statistical and computational considerations for secondary analysis of publicly available high throughput screening data with respect to metadata, data quality, and completeness and develops methods and best practices that can help to ameliorate these issues.

High-Throughput Cell Toxicity Assays.

Methods employed in the AstraZeneca HTS laboratory to carry out very large scale cell toxicity screening are described, which demonstrates the ability to measure toxicity of compounds on a large scale.



High-Throughput Screening: Update on Practices and Success

High-throughput screening is becoming fully integrated within drug discovery, both upstream and downstream, which includes increasing use of cell-based assays and high-content screening (HCS) technologies to achieve more physiologically relevant results and to find higher quality leads.

Process Validation and Screen Reproducibility in High-Throughput Screening

This article describes how GlaxoSmithKline (GSK) has addressed the need of a true validation of the HTS process before embarking in full HTS campaigns, and presents a variety of reproducibility indexes that are either innovative or have been adapted from generic medical diagnostic screening strategies.

A guide to drug discovery: Hit and lead generation: beyond high-throughput screening

The identification of small-molecule modulators of protein function, and the process of transforming these into high-content lead series, are key activities in modern drug discovery and demand a departure from the linear process of identification, evaluation and refinement activities towards a more integrated parallel process.

Drug repositioning: identifying and developing new uses for existing drugs

Repositioning existing drugs for new indications could deliver the productivity increases that the industry needs while shifting the locus of production to biotechnology companies.

The influence of lead discovery strategies on the properties of drug candidates

Analysis of the physicochemical properties of a large database of hits and corresponding leads identified in the past decade shows that this undesirable phenomenon can be traced back to the nature of high-throughput screening hits and hit-to-lead optimization practices.

Enhancements of screening collections to address areas of unmet medical need: an industry perspective.

Industrial-Style Screening Meets Academic Biology

A $100-million-a-year-effort to find chemicals for exploring cellular processes and drug discovery is about to move into production; skeptics say it is struggling to meet its goals.

The A, B, Cs of G-protein-coupled receptor pharmacology in assay development for HTS

This review provides an overview of the binding and functional techniques available for high-throughput screening, with particular attention on how assay application and configuration can be maximised to ensure their successful identification of relevant chemical matter and thereby optimising project success.

Drug discovery in jeopardy.

Despite striking advances in the biomedical sciences, the flow of new drugs has slowed to a trickle, impairing therapeutic advances as well as the commercial success of drug companies. Reduced

Key aspects of the Novartis compound collection enhancement project for the compilation of a comprehensive chemogenomics drug discovery screening collection.

The NIBR compound collection enrichment and enhancement project integrates corporate internal combinatorial compound synthesis and external compound acquisition activities in order to build up a comprehensive screening collection for a modern drug discovery organization.