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p15gag Proteinase of Myeloblastosis Associated Virus: Specificity Studies with Substrate Based Inhibitors

  • P. Štrop
  • L. Pavlíčková
  • D. Štys
  • M. Souček
  • J. Urban
  • O. Hrušková
  • F. Kaprálek
  • P. Ječmen
  • J. Sedláček
  • V. Kostka
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 306)

Abstract

The key role of retrovirus-encoded proteinases in limited proteolysis of polyprotein precursors, a prerequisite of the formation of mature infectious virions, makes these enzymes attractive targets of specific inhibitors. A rational basis for the design of such inhibitors requires detailed knowledge of the proteinase-inhibitor interactions at the level of three-dimensional structures. Such data are available so far only for the HIV-1 proteinase whose crystal complexes with some inhibitors were subject of X-ray studies.1 The absence of such information on the myeloblastosis associated virus (MAV) proteinase, another retroviral aspartate proteinase, together with the need of finding a tight-binding yet hydrophilic inhibitor for both X-ray studies and titration of its active site, led us to investigate the interactions of the proteinase with various classes of custom-synthesized inhibitors.

Keywords

General Aspartic Proteinase Myeloblastosis Associate Virus Bulky Hydrophobic Side Chain Chymosin Inhibitor Small Hydrophobic Side Chain 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Plenum Press, New York 1991

Authors and Affiliations

  • P. Štrop
    • 1
  • L. Pavlíčková
    • 1
  • D. Štys
    • 1
  • M. Souček
    • 1
  • J. Urban
    • 1
  • O. Hrušková
    • 1
  • F. Kaprálek
    • 2
  • P. Ječmen
    • 2
  • J. Sedláček
    • 2
  • V. Kostka
    • 1
  1. 1.Institute of Organic Chemistry and BiochemistryCzechoslovak Academy of SciencePragueCzechoslovakia
  2. 2.Institute of Molecular GeneticsCzechoslovak Academy of SciencePragueCzechoslovakia

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