Results 21 to 30 of about 4,262 (206)

Structure and drug resistance of the Plasmodium falciparum transporter PfCRT [PDF]

Nature, 2019
The emergence and spread of drug-resistant Plasmodium falciparum impedes global efforts to control and eliminate malaria. For decades, treatment of malaria has relied on chloroquine (CQ), a safe and affordable 4-aminoquinoline that was highly effective against intra-erythrocytic asexual blood-stage parasites, until resistance arose in Southeast Asia ...
Kim, Jonathan, Tan, Yong Zi, Wicht, Kathryn J, Erramilli, Satchal K, Dhingra, Satish K, Okombo, John, Vendome, Jeremie, Hagenah, Laura M, Giacometti, Sabrina I, Warren, Audrey L, Nosol, Kamil, Roepe, Paul D, Potter, Clinton S, Carragher, Bridget, Kossiakoff, Anthony A, Quick, Matthias, Fidock, David A, Mancia, Filippo   +17 more
openaire   +2 more sources

Mutations in the Plasmodium falciparum chloroquine resistance transporter, PfCRT, enlarge the parasite's food vacuole and alter drug sensitivities [PDF]

, 2015
Mutations in the Plasmodium falciparum chloroquine resistance transporter, PfCRT, are the major determinant of chloroquine resistance in this lethal human malaria parasite. Here, we describe P.
Staines, Henry M., Mu, Jianbing, Lee, Andrew H., Pulcini, Serena, Daley, Daniel A., Fidock, David A., Cooper, Roland A., Shafik, Sarah H., Altenhofen, Lindsey M., Krishna, Sanjeev, Martin, Rowena E., Painter, Heather J., Hoke, Matthew J., Llinás, Manuel, Moore, Catherine M., Bouyer, Guillaume, Ferguson, David J.P.   +16 more
core   +3 more sources

PfCRT-mutant PPQ parasites show increased susceptibility to aminopeptidase M17 inhibition.

, 2022
Dose–response plots illustrate susceptibility of PfCRT mutants to aminopeptidase inhibition. Half maximal inhibitory concentrations (IC50 and IC90) are presented as the mean ± SEM (N, n  =  4, 2) for (A) MMV1557817; (B) E-64; (C) ALLN; and (D) pepstatin,
John Okombo (561448), Tomas Yeo (10134672), Tarrick Qahash (14026400), Jade Bath (5955668), Imhoi Koo (1538677), Lindsey M. Orchard (5676110), Istvan Albert (634554), Sachel Mok (258479), Edward Owens (14026403), Manuel Llinás (14834), David A. Fidock (248990)   +10 more
core   +1 more source

Analysis of the Antimalarial Drug Resistance Protein Pfcrt Expressed in Yeast [PDF]

Journal of Biological Chemistry, 2002
Mutations in the novel membrane protein Pfcrt were recently found to be essential for chloroquine resistance (CQR) in Plasmodium falciparum, the parasite responsible for most lethal human malaria (Fidock, D. A., Nomura, T., Talley, A. K., Cooper, R. A., Dzekunov, S. M., Ferdig, M. T., Ursos, L. M., Sidhu, A. B., Naude, B., Deitsch, K. W., Su, X.
Hanbang, Zhang, Ellen M, Howard, Paul D, Roepe   +2 more
openaire   +2 more sources

Assessment of the molecular marker of Plasmodium falciparum chloroquine resistance (Pfcrt) in Senegal after several years of chloroquine withdrawal. [PDF]

, 2012
As a result of widespread antimalarial drug resistance, all African countries with endemic malaria have, in recent years, changed their malaria treatment policy.
Dieng, Yemou, Annie Abiola, Aminata Lo, Ndiaye, Daouda, Daouda Ndiaye, Yemou Dieng, Roger Tine, Faye, Babacar, Babacar Faye, Ndiaye, Magatte, Jean Louis Ndiaye, Lo, Aminata, Hallett, Rachel, Ndiaye, Jean Louis, Gaye, Oumar, Magatte Ndiaye, Rachel Hallett, Oumar Gaye, Michael Alifrangis, Tine, Roger, Alifrangis, Michael, Abiola, Annie   +21 more
core   +1 more source

Defining the role of PfCRT in Plasmodium falciparum chloroquine resistance [PDF]

Molecular Microbiology, 2005
SummaryRecent studies have highlighted the importance of a parasite protein referred to as the chloroquine resistance transporter (PfCRT) in the molecular basis of Plasmodium falciparum resistance to the quinoline antimalarials. PfCRT, an integral membrane protein with 10 predicted transmembrane domains, is a member of the drug/metabolite transporter ...
Bray, Patrick G., Martin, Rowena E., Tilley, Leann., Ward, Stephen A., Kirk, Kiaran., Fidock, David A.   +5 more
openaire   +2 more sources

Impact of Drug Exposure on Resistance Selection Following Artemether‐Lumefantrine Treatment for Malaria in Children With and Without HIV in Uganda

Clinical Pharmacology &Therapeutics, Volume 113, Issue 3, Page 660-669, March 2023., 2023
Artemisinin‐based combination therapies (ACTs) are the primary treatment for malaria. It is essential to characterize the pharmacokinetics (PKs) and pharmacodynamics (PDs) of ACTs in vulnerable populations at risk of suboptimal dosing. We developed a population PK/PD model using data from our previous study of artemether‐lumefantrine in HIV‐uninfected ...
Katherine Kay, Justin Goodwin, Hanna Ehrlich, Joyce Ou, Tracey Freeman, Kaicheng Wang, Fangyong Li, Martina Wade, Jonathan French, Liusheng Huang, Francesca Aweeka, Norah Mwebaza, Richard Kajubi, Matthew Riggs, Ana Ruiz‐Garcia, Sunil Parikh   +15 more
wiley   +1 more source

Drug Development Strategies for Malaria: With the Hope for New Antimalarial Drug Discovery—An Update

Advances in Medicine, Volume 2023, Issue 1, 2023., 2023
Malaria continued to be a deadly situation for the people of tropical and subtropical countries. Although there has been a marked reduction in new cases as well as mortality and morbidity rates in the last two decades, the reporting of malaria caused 247 million cases and 619000 deaths worldwide in 2021, according to the WHO (2022).
Swaroop Kumar Pandey, Uttpal Anand, Waseem A. Siddiqui, Renu Tripathi, Shunqing Liang   +4 more
wiley   +1 more source

In vitro selection of Plasmodium falciparum Pfcrt and Pfmdr1 variants by artemisinin [PDF]

Malaria Journal, 2016
Anti-malarial drugs are the major focus in the prevention and treatment of malaria. Artemisinin-based combination therapy (ACT) is the WHO recommended first-line treatment for Plasmodium falciparum malaria across the endemic world. Also ACT is increasingly relied upon in treating Plasmodium vivax malaria where chloroquine is failing.
Njokah, Muturi J., Kang’ethe, Joseph N., Kinyua, Johnson, Kariuki, Daniel, Kimani, Francis T.   +4 more
openaire   +2 more sources

Status of the Multidrug Resistance‐1 Gene of Plasmodium falciparum in Four Malaria Epidemiological Strata, Two Decades after the Abolition of Chloroquine as First‐Line Treatment for Uncomplicated Malaria in Cameroon

Journal of Tropical Medicine, Volume 2023, Issue 1, 2023., 2023
Drug‐resistant malaria parasites pose a threat to global malaria control efforts, and it is important to know the extent of these drug‐resistant mutations in each region to determine appropriate control measures. Chloroquine (CQ) was widely used in Cameroon for decades, but its declining clinical efficacy due to resistance prompted health authorities ...
David Denis Sofeu-Feugaing, Fabrice Nkengeh Ajonglefac, Marcel Nyuylam Moyeh, Tobias Obejum Apinjoh, Marianne Elodie Essende, Gilchrist Destin Talla Kouam, Stephen Mbigha Ghogomu, Jianbing Mu   +7 more
wiley   +1 more source