Why does oxamniquine kill Schistosoma mansoni and not S. haematobium and S. japonicum?

Autor: Anastasia R. Rugel, Meghan A. Guzman, Alexander B. Taylor, Frédéric D. Chevalier, Reid S. Tarpley, Stanton F. McHardy, Xiaohang Cao, Stephen P. Holloway, Timothy J.C. Anderson, P. John Hart, Philip T. LoVerde

Publikováno v: International Journal for Parasitology: Drugs and Drug Resistance, Vol 13, Iss , Pp 8-15 (2020)

Human schistosomiasis is a disease which globally affects over 229 million people. Three major species affecting humans are Schistosoma mansoni, S. haematobium and S. japonicum. Previous treatment of S. mansoni includes the use of oxamniquine (OXA),

Externí odkaz: https://doaj.org/article/d86b55a8a7f64c9c9976e5f440e1e224

Hsp90 Inhibitors

Autor: Brian S.J. Blagg, Matthew Kyle Hadden, Reid S. Tarpley

Publikováno v: Burger's Medicinal Chemistry and Drug Discovery. :1-88

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4721c6641183760a4f628996cfe40303
https://doi.org/10.1002/0471266949.bmc212.pub2

An iterative process produces oxamniquine derivatives that kill the major species of schistosomes infecting humans

Autor: Sevan N. Alwan, Dmytro P Kovalskyy, Stanton F. McHardy, Stephen P. Holloway, Anastasia R. Rugel, Meghan A. Guzman, Tim J. Anderson, Frédéric D. Chevalier, Reid S. Tarpley, Philip T. LoVerde, Alexander B. Taylor, Xiaohang Cao

Publikováno v: PLoS Neglected Tropical Diseases, Vol 14, Iss 8, p e0008517 (2020)
PLoS Neglected Tropical Diseases

Currently there is only one method of treatment for human schistosomiasis, the drug praziquantel. Strong selective pressure has caused a serious concern for a rise in resistance to praziquantel leading to the necessity for additional pharmaceuticals,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9fe9f110fd5ba9ae4d28dbe5539075a5
https://doaj.org/article/63cb9a6c7eed407f9070e62dc9bc98ef

Structural and enzymatic insights into species-specific resistance to schistosome parasite drug therapy

Autor: Reid S. Tarpley, Chiara M. Polcaro, Stephen P. Holloway, Nathaniel E. Clark, P. John Hart, Alexander B. Taylor, Stanton F. McHardy, Donato Cioli, Enrica Donati, Philip T. LoVerde, Kenneth M. Roberts, Livia Pica-Mattoccia, Paul F. Fitzpatrick, Xiaohang Cao

Publikováno v: The Journal of biological chemistry
292 (2017): 11154–11164. doi:10.1074/jbc.M116.766527
info:cnr-pdr/source/autori:Taylor A.B. (a,c); Roberts K.M. (d); Cao X. (a); Clark N.E. (a); Holloway S.P. (a); Donati E. (e); Polcaro C.M. (e); Pica-Mattoccia L. (f); Tarpley R.S. (g); McHardy S.F. (g); Cioli D. (e); LoVerde P.T. (a,b); Fitzpatrick P.F. (a); Hart P.J. (a,c,h)/titolo:Structural and enzymatic insights into species-specific resistance to schistosome parasite drug therapy/doi:10.1074%2Fjbc.M116.766527/rivista:The Journal of biological chemistry (Print)/anno:2017/pagina_da:11154/pagina_a:11164/intervallo_pagine:11154–11164/volume:292

The antischistosomal prodrug oxamniquine is activated by a sulfotransferase (SULT) in the parasitic flatworm Schistosoma mansoni. Of the three main human schistosome species, only S. mansoni is sensitive to oxamniquine therapy despite the presence of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ca6f5cfc7a36fdcd4465f7051c1803c
https://doi.org/10.1074/jbc.m116.766527