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Issue 8, 2006
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Microtiter plate based chemistry and in situ screening: a useful approach for rapid inhibitor discovery

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Abstract

The use of libraries extracted from nature or constructed by combinatorial chemistry, have been widely appreciated in the drug discovery area. In this perspective, we present our contribution to the field of enzyme inhibitor discovery using a useful approach that allows diversification of a common core in a microtiter plate followed by in situ screening. Our method relies on an organic reaction that is highly selective, high yielding, amenable to the microscale and preferably can be performed in water. The core can be a designed molecule based on the structural and mechanistic information of the target, a compound with a weak binding affinity, or a natural product. Several reactions were found useful for this approach and were applied to the rapid discovery of potent inhibitors of representative enzymes.

Graphical abstract: Microtiter plate based chemistry and in situ screening: a useful approach for rapid inhibitor discovery

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Publication details

The article was received on 03 Feb 2006 and first published on 22 Mar 2006


Article type: Perspective
DOI: 10.1039/B600055J
Citation: Org. Biomol. Chem., 2006,4, 1446-1457
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    Microtiter plate based chemistry and in situ screening: a useful approach for rapid inhibitor discovery

    A. Brik, C. Wu and C. Wong, Org. Biomol. Chem., 2006, 4, 1446
    DOI: 10.1039/B600055J

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