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Journal of Biomolecular Screening
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High-Capacity Screening of Arylalkylamine N-Acetyltransferase Inhibitors using a High-Performance Liquid Chromatography System

Gilles Ferry

Division de Pharmacologie Mol6culaire et Cellulaire, Institut de Recherches Servier, Croissy-sur-Seine, France

Jean A. Boutin

Division de Pharmacologie Mol6culaire et Cellulaire, Institut de Recherches Servier, Croissy-sur-Seine, France

Systematic screening is a natural development of any pharmacological program. Most enzyme inhibitor screens use indirect or "aspecific" methods, such as colorimetric or fluorimetric ones. These screening methods cause quite a few false-positive and false-negative hits. In order to limit these as much as possible, we developed a methodology using a high-performance liquid chromatography (HPLC) system for the medium throughput screening of serotonin N-acetyltransferase inhibitors. The core of this screening system is (1) the dramatic shortening of the analytical time down to 100 s per run by using a high-performance analytical column (Turbo), and (2) the use of absorption as opposed to radioactivity for detection of the product of the reaction (N-acetylserotonin). This system permits the analysis of about 1,000 compounds per day to be performed with a single HPLC system. This enzymatic system was taken as an example, because the methodology can be extended to many other enzymes, particularly transferases, phosphatases, and kinases.

Journal of Biomolecular Screening, Vol. 5, No. 5, 361-368 (2000)
DOI: 10.1177/108705710000500508
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