Method for High Throughput Thermodynamic Screening of Ligands

The optimization of lead compounds as viable drug candidates involves the optimization of their binding affinity towards the selected target, most notably the achievement of high affinity and specificity. JHU scientists have devised a method of rapidly screening ligands on the basis of their binding affinity and binding enthalpy by carrying out binding assays at a minimum of two temperatures. This technique permits the selection for further optimization of lead ligands that bind to the target molecules with favorable enthalpies. Those ligands will exhibit higher solubilities in aqueous solution than ligands selected by conventional means, and may exhibit lower susceptibilities to resistant mutations. Proposed Use (Set) The present invention is a method that may be used as a standalone technique to optimize drug design, or may be adapted to, for example, known high throughput screening technologies. This invention is additionally an apparatus for carrying out the described method.

Patent (Set) Issued Patent US 6,242,190

Patents:
US 6,242,190

Inventor(s): Freire, Ernesto

Type of Offer: Licensing



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