Literature DB >> 24440298

Virtual screening reveals allosteric inhibitors of the Toxoplasma gondii thymidylate synthase-dihydrofolate reductase.

Hitesh Sharma1, Mark J Landau2, Todd J Sullivan3, Vidya P Kumar1, Markus K Dahlgren3, William L Jorgensen3, Karen S Anderson4.   

Abstract

The parasite Toxoplasma gondii can lead to toxoplasmosis in those who are immunocompromised. To combat the infection, the enzyme responsible for nucleotide synthesis thymidylate synthase-dihydrofolate reductase (TS-DHFR) is a suitable drug target. We have used virtual screening to determine novel allosteric inhibitors at the interface between the two TS domains. Selected compounds from virtual screening inhibited TS activity. Thus, these results show that allosteric inhibition by small drug-like molecules can occur in T. gondii TS-DHFR and pave the way for new and potent species-specific inhibitors.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Dihydrofolate reductase; Thymidylate synthase; Toxoplasma gondii; Virtual screening

Mesh:

Substances:

Year:  2013        PMID: 24440298      PMCID: PMC3946055          DOI: 10.1016/j.bmcl.2013.12.039

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


  31 in total

1.  A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening.

Authors:  Susan L McGovern; Emilia Caselli; Nikolaus Grigorieff; Brian K Shoichet
Journal:  J Med Chem       Date:  2002-04-11       Impact factor: 7.446

2.  Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy.

Authors:  Richard A Friesner; Jay L Banks; Robert B Murphy; Thomas A Halgren; Jasna J Klicic; Daniel T Mainz; Matthew P Repasky; Eric H Knoll; Mee Shelley; Jason K Perry; David E Shaw; Perry Francis; Peter S Shenkin
Journal:  J Med Chem       Date:  2004-03-25       Impact factor: 7.446

3.  ZINC--a free database of commercially available compounds for virtual screening.

Authors:  John J Irwin; Brian K Shoichet
Journal:  J Chem Inf Model       Date:  2005 Jan-Feb       Impact factor: 4.956

4.  The SWISS-MODEL workspace: a web-based environment for protein structure homology modelling.

Authors:  Konstantin Arnold; Lorenza Bordoli; Jürgen Kopp; Torsten Schwede
Journal:  Bioinformatics       Date:  2005-11-13       Impact factor: 6.937

Review 5.  Screening in a spirit haunted world.

Authors:  Brian K Shoichet
Journal:  Drug Discov Today       Date:  2006-07       Impact factor: 7.851

6.  Identifying and characterizing binding sites and assessing druggability.

Authors:  Thomas A Halgren
Journal:  J Chem Inf Model       Date:  2009-02       Impact factor: 4.956

7.  Variants of human thymidylate synthase with loop 181-197 stabilized in the inactive conformation.

Authors:  Leslie L Lovelace; Saphronia R Johnson; Lydia M Gibson; Brittnaie J Bell; Sondra H Berger; Lukasz Lebioda
Journal:  Protein Sci       Date:  2009-08       Impact factor: 6.725

8.  Cooperative inhibition of human thymidylate synthase by mixtures of active site binding and allosteric inhibitors.

Authors:  Leslie L Lovelace; Lydia M Gibson; Lukasz Lebioda
Journal:  Biochemistry       Date:  2007-02-13       Impact factor: 3.162

9.  Human thymidylate synthase with loop 181-197 stabilized in an inactive conformation: ligand interactions, phosphorylation, and inhibition profiles.

Authors:  BeiBei Luo; Jayanthi Repalli; Al-Motassem Yousef; Saphronia R Johnson; Lukasz Lebioda; Sondra H Berger
Journal:  Protein Sci       Date:  2011-01       Impact factor: 6.725

10.  The SWISS-MODEL Repository and associated resources.

Authors:  Florian Kiefer; Konstantin Arnold; Michael Künzli; Lorenza Bordoli; Torsten Schwede
Journal:  Nucleic Acids Res       Date:  2008-10-18       Impact factor: 16.971

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  5 in total

1.  Allosteric Communication Disrupted by a Small Molecule Binding to the Imidazole Glycerol Phosphate Synthase Protein-Protein Interface.

Authors:  Ivan Rivalta; George P Lisi; Ning-Shiuan Snoeberger; Gregory Manley; J Patrick Loria; Victor S Batista
Journal:  Biochemistry       Date:  2016-11-11       Impact factor: 3.162

2.  Targeting the TS dimer interface in bifunctional Cryptosporidium hominis TS-DHFR from parasitic protozoa: Virtual screening identifies novel TS allosteric inhibitors.

Authors:  Victor G Ruiz; Daniel J Czyzyk; Vidya P Kumar; William L Jorgensen; Karen S Anderson
Journal:  Bioorg Med Chem Lett       Date:  2020-05-30       Impact factor: 2.823

Review 3.  Review of Experimental Compounds Demonstrating Anti-Toxoplasma Activity.

Authors:  Madalyn M McFarland; Sydney J Zach; Xiaofang Wang; Lakshmi-Prasad Potluri; Andrew J Neville; Jonathan L Vennerstrom; Paul H Davis
Journal:  Antimicrob Agents Chemother       Date:  2016-11-21       Impact factor: 5.191

4.  Biomolecular study of human thymidylate synthase conformer-selective inhibitors: New chemotherapeutic approach.

Authors:  Hala O El-Mesallamy; Hekmat M El Magdoub; James M Chapman; Nadia M Hamdy; Mona F Schaalan; Lamiaa N Hammad; Sondra H Berger
Journal:  PLoS One       Date:  2018-03-14       Impact factor: 3.240

Review 5.  Modeling enzyme-ligand binding in drug discovery.

Authors:  Janez Konc; Samo Lešnik; Dušanka Janežič
Journal:  J Cheminform       Date:  2015-10-06       Impact factor: 5.514

  5 in total

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