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Methods Mol Biol. 2012;841:179-207. doi: 10.1007/978-1-61779-520-6_8.

The role of enzymology in a structure-based drug discovery program: bacterial DNA gyrase.

Author information

1
Trius Therapeutics, San Diego, CA, USA. mcunningham@triusrx.com

Abstract

The capability to accurately, rapidly, and reproducibly determine the affinity of a ligand for a target protein or enzyme is a vital component for a successful structure-based drug design effort. In order to successfully drive a structure-based drug design (SBDD) project forward, multiple distinct assays, each with particular strengths and weaknesses, need to be employed. Using bacterial DNA gyrase as an example, a range of assays are described that will fully support an SBDD program.

PMID:
22222453
DOI:
10.1007/978-1-61779-520-6_8
[Indexed for MEDLINE]

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