Articles Devoted to Combinatorial Chemistry and High Throughput Screening
Compilations of literature in combinatorial chemistry, high throughput screening, solid phase organic synthesis, solid phase peptide synthesis and drug discovery. All these articles are freely available on the internet.
Combinatorial Chemistry and Contemporary Pharmacology
John S. Lazo and Peter Wipf
Departments of Pharmacology and Chemistry, The Fiske Drug Discovery Laboratory and The Combinatorial Chemistry Center, University of Pittsburgh, Pittsburgh, Pennsylvania Abstract
Both solid- and liquid-phase combinatorial chemistry have emerged as powerful tools for identifying pharmacologically active compounds and optimizing the biological activity of a lead compound. Complementary high-throughput in vitro assays are essential for compound evaluation. Cell-based assays that use optical endpoints permit investigation of a wide variety of functional properties of these compounds including specific intracellular biochemical pathways, protein-protein interactions, and the subcellular localization of targets. Integration of combinatorial chemistry with contemporary pharmacology now represents an important factor in drug discovery and development. Full Text (PDF)
Combinatorial Chemistry: A Guide for Librarians
Philip Barnett
Science/Engineering Library, City College of New York (CUNY) Abstract
In the 1980s a need to synthesize many chemical compounds rapidly and inexpensively spawned a new branch of chemistry known as combinatorial chemistry. While the techniques of this rapidly growing field are used primarily to find new candidate drugs, combinatorial chemistry is also finding other applications in various fields such as semiconductors, catalysts, and polymers. This guide for librarians explains the basics of combinatorial chemistry and elucidates the key information sources needed by combinatorial chemists. Full Text (HTML)
A review of high-throughput screening approaches for drug discovery
Jason W. Armstrong
Application Notes Abstract
High-throughput screening (HTS) is an approach to drug discovery that has gained widespread popularity over the last three or four years. HTS is the process of assaying a large number of potential effectors of biological activity against targets (a biological event). The methods of HTS are applied to the screening of combinatorial chemistry, genomics, protein, and peptide libraries. The goal of HTS is to accelerate drug discovery by screening large libraries often composed of hundreds of thousands of compounds (drug candidates) at a rate that may exceed 20,000 compounds per week. This paper will focus on assay adaptations, robotic equipment, and implementation strategies that allow HTS programs to be successful. Ultra high-throughput screening (UHTS) issues (testing of 100,000 compounds/day) will also be discussed. Full Text (PDF)
Combinatorial Chemistry. Making More Drugs.
William Wells
Access Excellence @ the National Health Museum Abstract
Combinatorial chemistry promises better drugs, new superconductors and an artificial nose, all with a one-thousand-fold increase in productivity. Who could resist? Full Text (HTML)
Imaging Mass Spectrometry and Combinatorial Chemistry
Nicholas Winograd, Robert M. Braun
Penn State University, University Park, PA Abstract
This article describes how spatially resolved time-of-flight mass spectrometry potentially offers chemical analysis at the rate of 10 compounds per second, and how it is amenable to microarray formats. Full Text (PDF)
