HIV proteinase inhibitors

Hansson, T., Aqvist, J. Estimation of binding free energies for HIV proteinase inhibitors by molecular dynamics simulations. Prot. Eng. 8 (1995) 1137-1144... 

Hansson T and J Aqvist 1995. Estimation of Binding Free Energies for HIV Proteinase Inhibitors b Molecular Dynamics Simulations. Protein Engineering 8 1137-1144. 

Roberts NA, Martin JA, Kinchington D, Broadhurst AV, Craig JC, Duncan IB, Galpin SA, Handa BJ, Kay J, Krohn A, Lambert RW, Merrett JH, Mills JS, Parkes KEB, Redshaw S, Ritchie AJ, Taylor DL, Thomas GJ, Machin PJ. Rational design of peptide-based HIV proteinase inhibitors. 1990 248 358-361. 

Krohn A, Redshaw S, Ritchie JC, Graves BJ, Hatada MH. Novel binding mode of highly potent HIV proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere. J. Med. Chem. 1991 34 3340-3342. 

Williams PEO, Muirhead GJ, Madigan MJ, et al. Disposition and bioavailability of the HIV-proteinase inhibitor, Ro 31-8959, after single doses in healthy volunteers. Br J Clin Pharmacol 1992 34 155P-156P. 

Fig. 2. Fluorescence micrographs of C. albicans SC5314 adhering on epithelial Vero cells in the absence a and in the presence b of the HIV proteinase inhibitor ritonavir at a concentration of 200 (rm. 

HIV proteinase inhibitors may display a specific anti-Sap activity leading to a reduced number of C. albicans yeasts on epithelial cells. Therefore, development of specific aspartic proteinase inhibitors might be useful in the treatment of mucosal candidiasis. The precise function of Candida Saps in the adherence process is not known, but two hypotheses can be advanced (1) the Candida Saps could act as ligands to surface proteins of the specific host cells, which do... 

Korting HC, Schaller M, Eder G, Hamm G, Bohmer U, Hube B Effects of the human immunodeficiency vims (HIV) proteinase inhibitors Saquinavir and Indinavir on in vitro activities of secreted aspartyl proteinases of Candida albicans isolates from HIV-infected patients. Antimicrob Agents Chemother 1999 43 2038-2042. 

Roberts, N. A., et al. (1990) Rational design of peptide based HIV proteinase inhibitors. Science 248, 358-361. 

In 1985 Toh et recognized a sequence in the Rous sarcoma virus (RSV) genome that resembled that of the Asp-Thr-Gly motif of aspartic proteinases, and a similar sequence was subsequently identified in HIV. This led to the suggestion that retroviruses contained a dimer which resembled the putative dimeric ancestor of the pepsin-like aspartic proteinases.The analogy, supported by observations that an HTV proteinase was sensistive to pepstatin, led to interest in the development of HIV proteinase inhibitors. It was later noted that HIV requires a specific protease for the maturation of its components and therefore inhibition of this protease could represent a therapeutic approach to the treatment of AIDs. 

Novel binding mode of highly potent HIV-proteinase inhibitors incorporating... 

T. Hansson and J. Aqvist, Protein Eng., 8, 1137 (1995). Estimation of the Binding Free Energies for HIV Proteinase Inhibitors by Molecular Simulations. 

Billich, A., Charpiot, B., Ettmayer, R, Gstach, H., Lehr, R, and Scholz, D. Rreparation of 2,4-diamino-3-hydroxycarboxylic acid-derivative HIV proteinase inhibitors. ER615969, 1994, Sandoz Ltd., Switzerland Sandoz-Ratent-G.m.b.H. Sandoz-Erfindungen Verwaltungsgesellschaft m.b.H. 

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