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Drug Development

Inhibitor design wraps packing defects in HIV-1 proteins

Published in Blood Weekly, October 28th, 2004

An inhibitor design wraps packing defects in HIV-1 proteins.

According to recent research from the United States, "Two viral proteins, HIV-1 protease and HIV-1 integrase, have been targeted for inhibitor design to prevent assembly and maturation of HIV-1 virions.

"The enzymatic mechanism of these proteins involves side-chain groups that serve as general acids or bases. Furthermore, catalytic activity requires that water be removed from the microenvironment surrounding the chemical reaction site or be constrained to serve as an activated nucleophile."

"We identify previously unrecognized structural features that promote water...

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