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- W1999308385 abstract "Abstract In this retrospective, personal review covering our research from the late 1980s until 2007, we outline nearly two‐decade worth of our own work on several aspartic protease inhibitors including those affecting renin, HIV‐1 protease, plasmepsins, β‐secretase, and HTLV‐I protease and we report on aspartic protease inhibitors as potential drugs to treat hypertension, AIDS, malaria, Alzheimer's disease and adult T‐cell leukemia, HTLV‐I associated myelopathy / tropical spastic paraparesis, and various, respectively, associated diseases. Herein, we describe our methods for rational substrate‐based drug design of peptidomimetics that potently inhibit the activity of renin, HIV‐1 protease, plasmepsins, β‐secretase, and HTLV‐I protease accordingly, using an appropriately selected inhibitory residue that contained a hydroxymethylcarbonyl isostere. Although this non‐hydrolyzable isostere mimics the transition state that is formed during protein cleavage of a substrate, the isostere‐containing inhibitor is not cleaved. We highlight our optimization studies in which we used various techniques and tools such as truncation studies, natural and non‐natural amino acid substitution studies, various moieties to promote chemical and pharmacological stability, X‐ray crystallography, computer‐assisted docking and dynamic simulations, quantitative structure‐activity relationship studies, and various other methods that this review can barely mention." @default.
- W1999308385 created "2016-06-24" @default.
- W1999308385 creator A5002620609 @default.
- W1999308385 creator A5006557735 @default.
- W1999308385 creator A5062102336 @default.
- W1999308385 creator A5081126904 @default.
- W1999308385 date "2008-09-01" @default.
- W1999308385 modified "2023-10-13" @default.
- W1999308385 title "Design of Potent Aspartic Protease Inhibitors to Treat Various Diseases" @default.
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