Elucidation of the structure of retroviral proteases: a reminiscence.
Determinations of only a very few protein structures had consequences comparable to the impact exerted by the structure of the protease encoded by HIV-1, published just over 25 years ago. The structure of this relatively small protein and its cousins from other retroviruses provided a clear target for a spectacularly successful structure-assisted drug design effort that offered new hope for controlling the then-escalating AIDS epidemic. This reminiscence is limited primarily to work conducted at the National Cancer Institute, and is not meant to be a comprehensive history of the field, but is rather an attempt to provide a very personal account of how the structures of this most thoroughly studied crystallographic target were determined.
['Jaskolski|Mariusz|M|', 'Miller|Maria|M|', 'Mohana Rao|J K|JK|', 'Gustchina|Alla|A|', 'Wlodawer|Alexander|A|']
D018360:Crystallography, X-Ray D055808:Drug Discovery D015658:HIV Infections D016333:HIV Protease D017320:HIV Protease Inhibitors D015497:HIV-1 D049673:History, 20th Century D049674:History, 21st Century D006801:Humans D008958:Models, Molecular D054547:National Cancer Institute (U.S.) D020836:Protein Structure, Quaternary D014481:United States
protease drug design HIV crystal structures inhibitors