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Pharmaceutical Discovery, Jun 1, 2005 
Compound Management: Integrating Chemistry, Biology and Technology in the Modern Drug Discovery Environment
Michael J. Sofia, Jay M. Stevenson, John Houston

Cover Story

Compound Management: Integrating Chemistry, Biology and Technology in the Modern Drug Discovery Environment
By Michael J. Sofia , Jay M. Stevenson , John Houston
The compound assets developed over many years of drug discovery effort are some of the most valuable assets of a drug discovery organization. Through the process of biological screening, these compounds comprise the future leads that eventually will become drug candidates. Therefore, it is critical that these compounds be managed effectively and are widely accessible by the scientific staff. This review will describe the role of the compound management function within the drug discovery environment and provide an overview of technologies that are critical to effectively manage and distribute compounds.

Microarrays on the Spot

Microarray Probes That Mask Differential Expression
By Wendell Jones
This column discusses types of malperforming probes, illustrates their impact on identifying differentially expressed genes and describes a simple method for handling them when performing data analysis of Affymetrix microarrays.

Articles

Drug Discovery Technology & Development
By Jodi Harris
The 10th anniversary of this important industry conference aims to provide life scientists with ways to accelerate the drug discovery and development process, expand clinical pipelines of promising drugs, explore new markets and reduce attrition of compounds due to safety and efficacy issues.

Application Note

Correlation of Spot Density with DNA Quantity Using AlphaQuant" Molecular Ladders
By Robert E. Harding , Craig Smith , Katrina Loomis
DNA analysis is a cornerstone of molecular biology, and electrophoresis of DNA in agarose gels is among the most commonly used techniques to accomplish it. Internal standards can be incorporated into DNA agarose gel experiments to maximize the quantitative information acquired in the experiment. DNA ladders typically are employed to determine the molecular size (number of base pairs) of double-stranded DNA (dsDNA).

Automation of a Double-Sink PAMPA Permeability Assay on the Biomek® FX Laboratory Automation Workstation
By Yu Suen , Konstantin Tsinman , Zhu Zhu , Graham Threadgill
Early drug discovery ADME assays, such as fast Caco-2 screens, can help in rejecting test compounds that lack good pharmaceutical profiles. A cost-effective, high-throughput method — parallel artificial membrane permeability analysis — that uses a phospholipid artificial membrane that models passive transport of epithelial cells, is becoming increasingly popular.

A Mass Spectrometry-based Technique for Lead Discovery
By Can C. Özbal , William A. Lamarr , Colin J.H. Brenan
Mass spectrometry-based screening can be applied to a wide range of targets, including targets that use substrates such as lipids, fatty acids, phospholipids, steroids, prostaglandins and other compounds not generally amenable to conventional screening techniques.

Measurement of Oxidative Stress using Kinetic High-content Screening
By Vivek C. Abraham , Jeffrey R. Haskins
We have developed a high-content bioassay that enables fully automated measurement of oxidative stress in individual cells in microplate format. Here we report the automation of this bioassay, which quantitatively measures cytotoxicity in terms of the rate and magnitude of intracellular generation of reactive oxygen species.

Automated Analysis of Proteins Using the LabChip 90 System
By Sherri Biondi , Adrian Winoto , Jim Mikkelsen , Bahram Fathollahi
Presently, a need exists in protein laboratories for rapid sample analysis in a format that enables quantitative decision-making. As experimentation becomes more complex and broader in scope, whether it involves testing expression in multiple cell lines, growth conditions or constructs, it becomes infeasible to compare, analyze and make decisions based on data from gel images alone. Automated processes and direct data reporting enable life scientists to view and manipulate protein sizing, concentration and purity data in order to make the most informed decisions possible in high-throughput experimentation. Questions related to purity, process optimization, expression level and solubility must be answered quickly and accurately in order to move target proteins on to functional assays, crystallography or final production in a much more efficient and timely manner.

Panorama" Mouse/Rat Tissue Extract Protein Array Kit: A New Tool for Protein Expression Analysis
By Eliezer Kopf , Annette Haward , Dorit Zharhary
The Panorama" Mouse/Rat Tissue Extract Protein Array Kit is a convenient and robust tool for accurate determination of protein distribution and expression. The array contains 62 extracts from 10 mouse and 12 rat tissues spotted on a nitrocellulose-coated slide, and is a reliable platform for rapid evaluation of protein expression.

Retooling the Structure Discovery Pipeline via Parallel Processing and Upstream Access to Crystallization Data
By Andrew May
This note describes an innovative model for protein structure determination that significantly reduces the time, experimental burden and upstream cost associated with growing diffraction-quality crystals.

News Hits

Company News
By Jodi Harris