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Identification of a small molecule HIV-1 inhibitor that targets the capsid hexamer.


ABSTRACT: The HIV-1 CA protein is an attractive therapeutic target for the development of new antivirals. An inter-protomer pocket within the hexamer configuration of the CA, which is a binding site for key host dependency factors, is an especially appealing region for small molecule targeting. Using a field-based pharmacophore derived from an inhibitor known to interact with this region, coupled to biochemical and biological assessment, we have identified a new compound that inhibits HIV-1 infection and that targets the assembled CA hexamer.

SUBMITTER: Xu JP 

PROVIDER: S-EPMC4728034 | biostudies-literature | 2016 Feb

REPOSITORIES: biostudies-literature

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Identification of a small molecule HIV-1 inhibitor that targets the capsid hexamer.

Xu Jimmy P JP   Branson Jeffrey D JD   Lawrence Rae R   Cocklin Simon S  

Bioorganic & medicinal chemistry letters 20151225 3


The HIV-1 CA protein is an attractive therapeutic target for the development of new antivirals. An inter-protomer pocket within the hexamer configuration of the CA, which is a binding site for key host dependency factors, is an especially appealing region for small molecule targeting. Using a field-based pharmacophore derived from an inhibitor known to interact with this region, coupled to biochemical and biological assessment, we have identified a new compound that inhibits HIV-1 infection and  ...[more]

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