Critical Outcome Technologies Discovers Novel Scaffolds for Inhibiting HIV Integrase
News May 24, 2010
Critical Outcome Technologies Inc. has 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.
As previously announced, these novel scaffolds are part of a co-development program with a major pharmaceutical partner. The co-development partner is now conducting and funding agreed upon in vitro experiments in their evaluation of the compounds. Once these experiments have been completed and the results have been received by COTI, the co-development partner will have an exclusive time period to negotiate a licensing agreement with COTI for the compounds.
Chinese researchers have developed interfacially polymerized porous polymer particles for low- abundance glycopeptide separation. These polymer particles - with hydrophilic-hydrophobic heterostructured nanopores - can separate low-abundance glycopeptides from complex biological samples with high-abundance background molecules efficiently.