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3'-Tetrahydrofuranylglycine as a Novel, Unnatural Amino Acid Surrogate for Asparagine in the Design of Inhibitors of the HIV Protease.


ABSTRACT: The blockade of the HIV protease has become a major target in the search for an effective therapy for AIDS.1 While many reports of potent HIV-1 inhibitors have appeared recently, the compound Ro 31-8959 remains the least selective for the HIV-1 and HIV-2 proteases.2 This property may result in reduced susceptibility to resistance since these represent the genetically most divergent strains of HIV presently known to exist.

SUBMITTER: Thompson WJ 

PROVIDER: S-EPMC6196357 | biostudies-literature | 1993 Jan

REPOSITORIES: biostudies-literature

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3'-Tetrahydrofuranylglycine as a Novel, Unnatural Amino Acid Surrogate for Asparagine in the Design of Inhibitors of the HIV Protease.

Thompson Wayne J WJ   Ghosh Arun K AK   Holloway M Katharine MK   Lee Hee Yoon HY   Munson Peter M PM   Schwering John E JE   Wai Jenny J   Darke Paul L PL   Zugay Joan J   Emini Emilio A EA   Schleif William A WA   Huff Joel R JR   Anderson Paul S PS  

Journal of the American Chemical Society 19930101 2


The blockade of the HIV protease has become a major target in the search for an effective therapy for AIDS.<sup>1</sup> While many reports of potent HIV-1 inhibitors have appeared recently, the compound Ro 31-8959 remains the least selective for the HIV-1 and HIV-2 proteases.<sup>2</sup> This property may result in reduced susceptibility to resistance since these represent the genetically most divergent strains of HIV presently known to exist. ...[more]

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