Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei

Autor: Ali H Alghamdi, Jane C Munday, Gustavo Daniel Campagnaro, Dominik Gurvic, Fredrik Svensson, Chinyere E Okpara, Arvind Kumar, Juan Quintana, Maria Esther Martin Abril, Patrik Milić, Laura Watson, Daniel Paape, Luca Settimo, Anna Dimitriou, Joanna Wielinska, Graeme Smart, Laura F Anderson, Christopher M Woodley, Siu Pui Ying Kelly, Hasan MS Ibrahim, Fabian Hulpia, Mohammed I Al-Salabi, Anthonius A Eze, Teresa Sprenger, Ibrahim A Teka, Simon Gudin, Simone Weyand, Mark Field, Christophe Dardonville, Richard R Tidwell, Mark Carrington, Paul O'Neill, David W Boykin, Ulrich Zachariae, Harry P De Koning

Publikováno v: eLife, Vol 9 (2020)

Mutations in the Trypanosoma brucei aquaporin AQP2 are associated with resistance to pentamidine and melarsoprol. We show that TbAQP2 but not TbAQP3 was positively selected for increased pore size from a common ancestor aquaporin. We demonstrate that

Externí odkaz: https://doaj.org/article/04cf21046dd94dac9faba5a20eaa5348

Snakebite drug discovery: high-throughput screening to identify novel snake venom metalloproteinase toxin inhibitors

Autor: Rachel H. Clare, Charlotte A. Dawson, Adam Westhorpe, Laura-Oana Albulescu, Christopher M. Woodley, Nada Mosallam, Daniel J. W. Chong, Jeroen Kool, Neil G. Berry, Paul M. O’Neill, Nicholas R. Casewell

Publikováno v: Frontiers in Pharmacology, Vol 14 (2024)

Snakebite envenoming results in ∼100,000 deaths per year, with close to four times as many victims left with life-long sequelae. Current antivenom therapies have several limitations including high cost, variable cross-snake species efficacy and a r

Externí odkaz: https://doaj.org/article/c67978e66f4041d2bd395e92866c736a

Artemisinin inspired synthetic endoperoxide drug candidates: Design, synthesis, and mechanism of action studies

Autor: Christopher M Woodley, Patrícia S M Amado, Maria Lurdes Santos Cristiano, Paul M. O'Neill

Publikováno v: Repositório Científico de Acesso Aberto de Portugal
Repositório Científico de Acesso Aberto de Portugal (RCAAP)
instacron:RCAAP
MEDICINAL RESEARCH REVIEWS

Artemisinin combination therapies (ACTs) have been used as the first-line treatments against Plasmodium falciparum malaria for decades. Recent advances in chemical proteomics have shed light on the complex mechanism of action of semi-synthetic artemi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae7fa1bcb987e730238df66192d7d471
https://hdl.handle.net/10400.1/17140

Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei

Autor: Harry P. de Koning, Ibrahim A. Teka, Hasan M. S. Ibrahim, Christopher M Woodley, Simon Gudin, Patrik Mili, Arvind Kumar, Daniel Paape, Fredrik Svensson, Fabian Hulpia, Jane C. Munday, Mark Carrington, Mohammed I. Al-Salabi, Dominik Gurvic, Laura F Anderson, Christophe Dardonville, David W. Boykin, Chinyere E Okpara, Ali H. Alghamdi, Luca Settimo, Laura Watson, Maria Esther Martin Abril, Joanna Wielinska, Gustavo D. Campagnaro, Graeme Smart, Ulrich Zachariae, Anthonius A. Eze, Richard R. Tidwell, Anna Dimitriou, Siu Pui Ying Kelly, Paul M. O'Neill

Mutations in the Trypanosoma brucei aquaporin AQP2 are associated with resistance to pentamidine and melarsoprol. We show that TbAQP2 but not TbAQP3 was positively selected for increased pore size from a common ancestor aquaporin. We demonstrate that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e12a2c3019e9ca4c7a9a0aacc54e2b6b