ActiveSite's proprietary technology platform is a novel
approach to fragment-based drug discovery, especially applicable to enzymes
such as proteases that have proven to be recalcitrant targets in drug
discovery.
This technology enables ActiveSite
to detect the interaction of drug-like small molecules (from its unique,
internally developed library) with the active site of target enzymes without
the use of NMR, crystallization or in
silico methodology typically used by other fragment-based approaches.
Although the technology is applicable to all
enzymes, the company has focused on proteases owing to their well-known
intractability to HTS, that has mostly limited drug-development for this
important class of targets to peptidomimetic approaches that often results in
molecules with poor drug-like properties.
ActiveSite's approach offers a rapidly deployable alternative for
identifying non-peptidic, small molecule, drug-like inhibitors of proteases,
and other enzymes, as exemplified by its plasma kallikrein inhibitor program.
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