Literature DB >> 25458183

Design of inhibitors of thymidylate kinase from Variola virus as new selective drugs against smallpox.

Ana P Guimarães1, Felipe R de Souza2, Aline A Oliveira3, Arlan S Gonçalves4, Ricardo B de Alencastro5, Teodorico C Ramalho6, Tanos C C França7.   

Abstract

Recently we constructed a homology model of the enzyme thymidylate kinase from Variola virus (VarTMPK) and proposed it as a new target to the drug design against smallpox. In the present work, we used the antivirals cidofovir and acyclovir as reference compounds to choose eleven compounds as leads to the drug design of inhibitors for VarTMPK. Docking and molecular dynamics (MD) studies of the interactions of these compounds inside VarTMPK and human TMPK (HssTMPK) suggest that they compete for the binding region of the substrate and were used to propose the structures of ten new inhibitors for VarTMPK. Further docking and MD simulations of these compounds, inside VarTMPK and HssTMPK, suggest that nine among ten are potential selective inhibitors of VarTMPK.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Docking; Molecular dynamics; Smallpox; Thymidylate kinase; Variola virus

Mesh:

Substances:

Year:  2014        PMID: 25458183     DOI: 10.1016/j.ejmech.2014.09.099

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

1.  Poxviruses as Gene Therapy Vectors: Generating Poxviral Vectors Expressing Therapeutic Transgenes.

Authors:  Steven J Conrad; Jia Liu
Journal:  Methods Mol Biol       Date:  2019

2.  Genome Sequences of Akhmeta Virus, an Early Divergent Old World Orthopoxvirus.

Authors:  Jinxin Gao; Crystal Gigante; Ekaterine Khmaladze; Pengbo Liu; Shiyuyun Tang; Kimberly Wilkins; Kun Zhao; Whitni Davidson; Yoshinori Nakazawa; Giorgi Maghlakelidze; Marika Geleishvili; Maka Kokhreidze; Darin S Carroll; Ginny Emerson; Yu Li
Journal:  Viruses       Date:  2018-05-12       Impact factor: 5.048

Review 3.  Dangerous Pathogens as a Potential Problem for Public Health.

Authors:  Edyta Janik; Michal Ceremuga; Marcin Niemcewicz; Michal Bijak
Journal:  Medicina (Kaunas)       Date:  2020-11-06       Impact factor: 2.430

4.  Design of inhibitors of thymidylate kinase from Variola virus as new selective drugs against smallpox: part II.

Authors:  Danielle Rodrigues Garcia; Felipe Rodrigues de Souza; Ana Paula Guimarães; Teodorico Castro Ramalho; Alcino Palermo de Aguiar; Tanos Celmar Costa França
Journal:  J Biomol Struct Dyn       Date:  2019-01-02       Impact factor: 5.235

  4 in total

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