The role of enzymology in a structure-based drug discovery program: bacterial DNA gyrase.
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.
Trius Therapeutics, San Diego, CA, USA. mcunningham@triusrx.com
Mark L
ML
Cunningham
D001419:Bacteria / Q000201:enzymology*; D018360:Crystallography, X-Ray; D027081:DNA Gyrase / Q000737:chemistry* / Q000378:metabolism*; D015195:Drug Design; D055808:Drug Discovery; D008958:Models, Molecular; D015394:Molecular Structure; D059005:Topoisomerase II Inhibitors
D059005:Topoisomerase II Inhibitors; D027081:DNA Gyrase