Critical Outcome Technologies Inc. Discovers Novel Scaffolds For Inhibiting HIV Integrase
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Critical Outcome Technologies Inc. (COTI) announced positive results from the first phase of its HIV integrase inhibitor discovery program. These results provide novel intellectual property to the Company and further validation of the CHEMSAS® drug discovery technology.
The significance of these results is that the majority of currently marketed and developmental stage HIV Integrase inhibitors have a very similar way of interacting with and inhibiting the enzyme through a diketo acid type moiety. COTI has used its proprietary technology, CHEMSAS®, to discover several novel small molecule scaffolds that have an entirely new binding mode and interaction with the active site of the viral enzyme.
COTI has completed the synthesis and initial confirmatory in vitro testing of the first three novel scaffolds from this program. All three scaffolds demonstrated good inhibitory activity in a biochemical HIV integrase assay at nanomolar concentrations. On the basis of these results, COTI has filed composition of matter patents and intends to proceed with the next phase of this project that consists of optimizing a small series of potential lead candidates based on these scaffolds.
“These encouraging results provide further validation of our CHEMSAS® technology and its ability to rapidly identify innovative small molecules for difficult drug targets. The discovery of new HIV integrase inhibiting scaffolds having an entirely novel mode of interacting with the enzyme has been challenging for HIV researchers, which makes these early results quite gratifying,” said Dr Wayne Danter, COTI’s President and CSO.
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