Literature DB >> 17167070

The Trypanosoma brucei cAMP phosphodiesterases TbrPDEB1 and TbrPDEB2: flagellar enzymes that are essential for parasite virulence.

Michael Oberholzer1, Gabriela Marti, Mario Baresic, Stefan Kunz, Andrew Hemphill, Thomas Seebeck.   

Abstract

Cyclic nucleotide specific phosphodiesterases (PDEs) are pivotal regulators of cellular signaling. They are also important drug targets. Besides catalytic activity and substrate specificity, their subcellular localization and interaction with other cell components are also functionally important. In contrast to the mammalian PDEs, the significance of PDEs in protozoal pathogens remains mostly unknown. The genome of Trypanosoma brucei, the causative agent of human sleeping sickness, codes for five different PDEs. Two of these, TbrPDEB1 and TbrPDEB2, are closely similar, cAMP-specific PDEs containing two GAF-domains in their N-terminal regions. Despite their similarity, these two PDEs exhibit different subcellular localizations. TbrPDEB1 is located in the flagellum, whereas TbrPDEB2 is distributed between flagellum and cytoplasm. RNAi against the two mRNAs revealed that the two enzymes can complement each other but that a simultaneous ablation of both leads to cell death in bloodstream form trypanosomes. RNAi against TbrPDEB1 and TbrPDEB2 also functions in vivo where it completely prevents infection and eliminates ongoing infections. Our data demonstrate that TbrPDEB1 and TbrPDEB2 are essential for virulence, making them valuable potential targets for new PDE-inhibitor based trypanocidal drugs. Furthermore, they are compatible with the notion that the flagellum of T. brucei is an important site of cAMP signaling.

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Year:  2006        PMID: 17167070     DOI: 10.1096/fj.06-6818com

Source DB:  PubMed          Journal:  FASEB J        ISSN: 0892-6638            Impact factor:   5.191


  63 in total

1.  Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness.

Authors:  Nicholas D Bland; Cuihua Wang; Craig Tallman; Alden E Gustafson; Zhouxi Wang; Trent D Ashton; Stefan O Ochiana; Gregory McAllister; Kristina Cotter; Anna P Fang; Lara Gechijian; Norman Garceau; Rajiv Gangurde; Ron Ortenberg; Mary Jo Ondrechen; Robert K Campbell; Michael P Pollastri
Journal:  J Med Chem       Date:  2011-11-08       Impact factor: 7.446

2.  Leveraging biotech's drug discovery expertise for neglected diseases.

Authors:  Joanna E Lowell; Christopher D Earl
Journal:  Nat Biotechnol       Date:  2009-04       Impact factor: 54.908

3.  Three-dimensional cellular architecture of the flagellar pocket and associated cytoskeleton in trypanosomes revealed by electron microscope tomography.

Authors:  Sylvain Lacomble; Sue Vaughan; Catarina Gadelha; Mary K Morphew; Michael K Shaw; J Richard McIntosh; Keith Gull
Journal:  J Cell Sci       Date:  2009-03-19       Impact factor: 5.285

4.  Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1).

Authors:  Emanuele Amata; Nicholas D Bland; Robert K Campbell; Michael P Pollastri
Journal:  Tetrahedron Lett       Date:  2015-05-20       Impact factor: 2.415

5.  Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 2. Tadalafil analogs.

Authors:  Stefan O Ochiana; Alden Gustafson; Nicholas D Bland; Cuihua Wang; Michael J Russo; Robert K Campbell; Michael P Pollastri
Journal:  Bioorg Med Chem Lett       Date:  2012-02-09       Impact factor: 2.823

6.  Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 1. Sildenafil analogs.

Authors:  Cuihua Wang; Trent D Ashton; Alden Gustafson; Nicholas D Bland; Stefan O Ochiana; Robert K Campbell; Michael P Pollastri
Journal:  Bioorg Med Chem Lett       Date:  2012-02-09       Impact factor: 2.823

7.  Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1).

Authors:  Jennifer L Woodring; Nicholas D Bland; Stefan O Ochiana; Robert K Campbell; Michael P Pollastri
Journal:  Bioorg Med Chem Lett       Date:  2013-08-21       Impact factor: 2.823

Review 8.  Motility and more: the flagellum of Trypanosoma brucei.

Authors:  Gerasimos Langousis; Kent L Hill
Journal:  Nat Rev Microbiol       Date:  2014-07       Impact factor: 60.633

Review 9.  The paraflagellar rod of kinetoplastid parasites: from structure to components and function.

Authors:  Neil Portman; Keith Gull
Journal:  Int J Parasitol       Date:  2009-10-30       Impact factor: 3.981

10.  A protein-protein interaction map of the Trypanosoma brucei paraflagellar rod.

Authors:  Sylvain Lacomble; Neil Portman; Keith Gull
Journal:  PLoS One       Date:  2009-11-03       Impact factor: 3.240

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