FK506-binding protein (FKBP) partitions a modified HIV protease inhibitor into blood cells and prolongs its lifetime in vivo

No abstract is available for this paper.

• Publication year

  2009

• Venue

  Proceedings of the National Academy of Sciences of the United States of America

• Publication date

  2009-02-03

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1073/pnas.0805375106PMID 19164520PMCID PMC2635806
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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  2008cited by this paper
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  2008cited by this paper
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• A Directed Approach for Engineering Conditional Protein Stability Using Biologically Silent Small Molecules*

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  2005cited by this paper
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  2005cited by this paper
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  2005influential reference
• Synthesis of poly(ethylene glycol)-based saquinavir prodrug conjugates and assessment of release and anti-HIV-1 bioactivity using a novel protease inhibition assay.

  2004cited by this paper
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  2004cited by this paper
• HIV drug resistance.

  2004cited by this paper
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  2004cited by this paper
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  2003cited by this paper
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  2003cited by this paper
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  2002influential reference
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  2002cited by this paper
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  2002cited by this paper
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  1999cited by this paper
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  1999cited by this paper
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  1998cited by this paper
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  1997cited by this paper
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  1997cited by this paper
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  1996cited by this paper
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  1996cited by this paper
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  1995cited by this paper
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  1993cited by this paper
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  1992cited by this paper
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  1991cited by this paper

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