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  • antiviral
  • In total we present six protease-inhibitor complexes at 1.8-2.3 A resolution, which have been structurally characterized with respect to their antiviral and inhibitory activities, in order to evaluate the effects of different fluoro-substitutions. (diva-portal.org)
  • Used in combination with other antiviral drugs in the treatment of HIV in both adults and children. (pharmacycode.com)
  • The correct processing of the precursor polyproteins by the aspartic protease is required for the assembly of infectious virions, thus making the aspartic protease an attractive target for antiviral therapy. (allindianpatents.com)
  • compounds
  • All the protease inhibitors were modeled after the compounds first developed for renin. (middlebury.edu)
  • The compounds of this invention are also renin inhibitors and thus are useful in treating hypertension. (patentgenius.com)
  • In this study, nine C-terminally duplicated HIV-1 protease inhibitors were cocrystallised with the enzyme, the crystal structures analysed at 1.8-2.3 Å resolution, and the inhibitory activity of the compounds characterized in order to evaluate the effects of the individual modifications. (diva-portal.org)
  • 15 compounds most similar in shape to the inhibitor were selected for testing in vitro . (biochemj.org)
  • clinical
  • This is an open label, single site, randomized clinical trial comparing PI-based ART to NNRTI-based ART for the prevention of malaria in HIV-infected children. (clinicaltrials.gov)
  • The clinical use of HIV 1 protease inhibitors (PIs) has led to dramatic improvements in HIV-related morbidity and mortality ( 1 ). (pubmedcentralcanada.ca)
  • Opportunistic infections and deaths have gone down among U.S. young people living with HIV in the combination antiretroviral therapy era, but death rates among this group remain significantly higher than the general population, according to a study published in Clinical Infectious Diseases . (thebodypro.com)
  • aspartic protease
  • The cleavage sequence is initiated by the aspartic protease BACE-1, which makes the enzyme a key target in the effort of finding a therapy that aim to slow down the progression of AD. (diva-portal.org)
  • One of the critical pathways in a retroviral life cycle is the processing of polyprotein precursors by aspartic protease. (allindianpatents.com)
  • enzymes
  • In order to make optimum use of the genes, HIV makes long nonfunctional polypeptide chains that are precursers to the actual proteins and enzymes. (middlebury.edu)
  • Despite the fact that these antiretrovirals are very useful, they have a common limitation, namely, the targeted enzymes in the HIV virus are able to mutate in such a way that the known drugs become less effective, or even ineffective against these mutant HIV viruses. (allindianpatents.com)
  • metabolism
  • However, the high fat diet does not overcome the inhibitor going through extensive metabolism in the liver by the hepatatic cytochrome P450 3A system. (middlebury.edu)
  • To design future HIV drugs that have have the least adverse metabolic effects, it is necessary to identify the disorders of glucose metabolism with PI therapy. (clinicaltrials.gov)
  • In the future, drugs for the treatment of HIV can be developed that avoid these disorders of glucose metabolism. (clinicaltrials.gov)
  • Finally, these drug-specific effects are considered within the context of HIV-specific effects on lipid metabolism as well as lifestyle factors that have contributed to a rapidly increasing incidence of similar metabolic syndromes in the general population. (edu.au)
  • Symmetric
  • The ortho- and meta-fluorinated P1/P1'-benzyloxy side groups proved to have the most cytopathogenic effects compared with the nonsubstituted analog and related C2-symmetric diol-based inhibitors. (diva-portal.org)
  • Synthesis of four C 2 -symmetric cyclic urea inhibitors revealed the importance of correct stereochemistry in rigid cyclic structures for activity. (diva-portal.org)
  • Changing the water-mimicking group from urea to sulfamide resulted in an unexpected non-symmetric binding mode as deduced from comparison of the X-ray crystal structure of a urea and a sulfamide inhibitor in complex with the protease. (diva-portal.org)
  • A small X-ray structure of a sulfamide inhibitor in absence of the protease established that thenon-symmetric conformation of the inhibitor was an inherent feature of the sulfamide scaffold and not induced by the protease. (diva-portal.org)
  • In an attempt to establish the structure activity relationship (SAR) of the sulfamide class of inhibitors, symmetric and non-symmetrically substituted sulfamide inhibitors were prepared. (diva-portal.org)
  • potency
  • The most promising inhibitors 4a and 4e displayed K i values of 1.0 nM and 0.7 nM respectively and EC 50 values in the MT4 cell-based assay of 0.17 µM and 0.33 µM respectively, a slight loss in potency compared to lead inhibitor 3 . (diva-portal.org)
  • treatment
  • In particular for HIV treatment, the HIV protease is an attractive target. (allindianpatents.com)
  • The use of protease inhibitors is increasing in HIV-infected children because this treatment has resulted in improved body weight, improved immune status and less hospitalizations. (clinicaltrials.gov)
  • Inclusion criteria for HIV infected children- a) The participants may be either antiretroviral treatment naive, or experienced. (clinicaltrials.gov)
  • The conclusions are based on a trend over time of higher CD4 cell counts at diagnosis and treatment start among those with newly acquired HIV. (thebodypro.com)
  • These counts increased from 325 cells/μL in 2006 to 379 cells/μL in 2012 for diagnosis, and from 178 cells/μL to 360 cells/μL during the same period for starting HIV treatment. (thebodypro.com)
  • infectious
  • HIV-1 protease is a pivotal enzyme in the later stages of the viral life cycle which is responsible for the processing and maturation of the virus particle into an infectious virion. (diva-portal.org)
  • By 2012, people living with HIV in New York City were diagnosed earlier and started antiretroviral therapy sooner than in 2006, an analysis published in The Journal of Infectious Diseases found. (thebodypro.com)
  • The National Institute of Allergy and Infectious Diseases (NIAID), part of the National Institutes of Health, is partnering with GlaxoSmithKline (GSK) to form a new initiative for developing broadly neutralizing antibodies that work against HIV. (thebodypro.com)