Literature DB >> 16517158

A fast and robust 19F NMR-based method for finding new HIV-1 protease inhibitors.

Silvia Frutos1, Teresa Tarrago, Ernest Giralt.   

Abstract

The human immunodeficiency virus (HIV) which encodes, among other indispensable enzymes, an aspartic protease that is essential for viral maturation and replication. Numerous inhibitors of the protease have been developed. However, the eventual resistance of HIV-1 to these drugs implies a continuous battle to develop new inhibitors. Proposed herein is a robust, fast, and reliable method employing (19)F NMR for the evaluation of the inhibitory activity of new compounds against HIV-1 protease.

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Year:  2006        PMID: 16517158     DOI: 10.1016/j.bmcl.2006.02.031

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Perspectives on NMR in drug discovery: a technique comes of age.

Authors:  Maurizio Pellecchia; Ivano Bertini; David Cowburn; Claudio Dalvit; Ernest Giralt; Wolfgang Jahnke; Thomas L James; Steve W Homans; Horst Kessler; Claudio Luchinat; Bernd Meyer; Hartmut Oschkinat; Jeff Peng; Harald Schwalbe; Gregg Siegal
Journal:  Nat Rev Drug Discov       Date:  2008-09       Impact factor: 84.694

2.  Use of Fluorinated Functionality in Enzyme Inhibitor Development: Mechanistic and Analytical Advantages.

Authors:  David B Berkowitz; Kannan R Karukurichi; Roberto de la Salud-Bea; David L Nelson; Christopher D McCune
Journal:  J Fluor Chem       Date:  2008-09       Impact factor: 2.050

  2 in total

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