The synthesis and kinetic evaluation of aryl α-aminophosphonates as novel inhibitors of T. cruzi trans-sialidase

Autor: Andrew G. Watts, A. Carlos Frasch, Ricardo Resende, Jean M. H. van den Elsen, Susan J. Crennell, Patricia Marcé, Pedro M. Alzari, Zexin Chen

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2018, 158, pp.25-33. ⟨10.1016/j.ejmech.2018.08.089⟩
Chen, Z, Marce Villa, P, Resende, R, Alzari, P M, Frasch, A C, Van Den Elsen, J, Crennell, S & Watts, A 2018, ' The synthesis and kinetic evaluation of aryl α-aminophosphonates as novel inhibitors of T. cruzi trans-sialidase ', European Journal of Medicinal Chemistry, vol. 158, pp. 25-33 . https://doi.org/10.1016/j.ejmech.2018.08.089
European Journal of Medicinal Chemistry, 2018, 158, pp.25-33. ⟨10.1016/j.ejmech.2018.08.089⟩

The trans-sialidase protein expressed by Trypanosoma cruzi is an important enzyme in the life cycle of this human pathogenic parasite and is considered a promising target for the development of new drug treatments against Chagas' disease. Here we des

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41ddfe1a4a8535e8f8ad3c5e44d9ceac
https://doi.org/10.1016/j.ejmech.2018.08.089

Insights into antitrypanosomal drug mode-of-action from cytology-based profiling

Autor: Thomas, James A., Baker, Nicola, Hutchinson, Sebastian, Dominicus, Caia, Trenaman, Anna, Glover, Lucy, Alsford, Sam, Horn, David

Publikováno v: PLoS Neglected Tropical Diseases
PLoS Neglected Tropical Diseases, Public Library of Science, 2018, 12 (11), pp.e0006980. ⟨10.1371/journal.pntd.0006980⟩
PLoS Neglected Tropical Diseases, Vol 12, Iss 11, p e0006980 (2018)
PLoS Neglected Tropical Diseases, 2018, 12 (11), pp.e0006980. ⟨10.1371/journal.pntd.0006980⟩

Chemotherapy continues to have a major impact on reducing the burden of disease caused by trypanosomatids. Unfortunately though, the mode-of-action (MoA) of antitrypanosomal drugs typically remains unclear or only partially characterised. This is the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::31f45f186ae5f4e445bd3a805273919e
https://hal-pasteur.archives-ouvertes.fr/pasteur-03107158

Binding Mode and Selectivity of Steroids towards Glucose-6-phosphate Dehydrogenase from the Pathogen Trypanosoma cruzi

Autor: Andrea Medeiros, Francesca Moraca, Marcelo A. Comini, Maurizio Botta, Cecilia Ortíz, Niall M. Hamilton

Publikováno v: Molecules
Molecules, MDPI, 2016, 21 (3), pp.368. ⟨10.3390/molecules21030368⟩
Molecules, Vol 21, Iss 3, p 368 (2016)
Molecules; Volume 21; Issue 3; Pages: 368

International audience; Glucose-6-phosphate dehydrogenase (G6PDH) plays a housekeeping role in cell metabolism by generating reducing power (NADPH) and fueling the production of nucleotide precursors (ribose-5-phosphate). Based on its indispensabilit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc7187f5e0d7bb2d19af004bec389b80
https://hal-riip.archives-ouvertes.fr/pasteur-01499027/file/molecules-21-00368.pdf

Trypanosoma brucei aquaglyceroporin 2 is a high-affinity transporter for pentamidine and melaminophenyl arsenic drugs and the main genetic determinant of resistance to these drugs

Autor: Munday, Jane C., Eze, Anthonius A., Baker, Nicola, Glover, Lucy, Clucas, Caroline, Aguinaga Andres, David, Natto, Manal J., Teka, Ibrahim A., McDonald, Jennifer, Lee, Rebecca S., Graf, Fabrice E., Ludin, Philipp, Burchmore, Richard J. S., Turner, C. Michael R., Tait, Andy, MacLeod, Annette, Mäser, Pascal, Barrett, Michael P., Horn, David, De Koning, Harry P.

Publikováno v: Journal of Antimicrobial Chemotherapy
Journal of Antimicrobial Chemotherapy, Oxford University Press (OUP), 2014, 69 (3), pp.651-663. ⟨10.1093/jac/dkt442⟩

Objectives: Trypanosoma brucei drug transporters include the TbAT1/P2 aminopurine transporter and the high-affinity pentamidine transporter (HAPT1), but the genetic identity of HAPT1 is unknown. We recently reported that loss of T. brucei aquaglycero

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https://hal-pasteur.archives-ouvertes.fr/pasteur-03107152/file/dkt442.pdf

Polysomnography as a diagnosis and post-treatment follow-up tool in human African trypanosomiasis: a case study in an infant

Autor: Bébène Bandzouzi, Ghislain Mpandzou, Alain Buguet, Philippe Vincendeau, Raymond Cespuglio, Stéphane Ngampo, Bernard Bouteille

Publikováno v: Journal of the Neurological Sciences
Journal of the Neurological Sciences, Elsevier, 2011, 305 (1-2), pp.112-5. ⟨10.1016/j.jns.2011.03.002⟩

International audience; Gambian (Trypanosoma brucei gambiense) human African trypanosomiasis (HAT) evolves from the hemolymphatic stage 1, treated with pentamidine, to the meningoencephalitic stage 2, often treated with melarsoprol. This arseniate ma

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0dae214db3083148b8f6e1669d38efb9
https://hal-unilim.archives-ouvertes.fr/hal-00933524