PfCRT mutations conferring piperaquine resistance in falciparum malaria shape the kinetics of quinoline drug binding and transport

The chloroquine resistance transporter (PfCRT) confers resistance to a wide range of quinoline and quinoline-like antimalarial drugs in Plasmodium falciparum, with local drug histories driving its evolution and, hence, the drug transport specificities. For example, the change in prescription practic...

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Veröffentlicht in:	PLoS pathogens 2023-06, Vol.19 (6), p.e1011436-e1011436
Hauptverfasser:	Gomez, Guillermo M, D'Arrigo, Giulia, Sanchez, Cecilia P, Berger, Fiona, Wade, Rebecca C, Lanzer, Michael
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino acid substitution Amino acids Analysis Antimalarial agents Antimalarials - chemistry Antiparasitic agents Binding Biology and Life Sciences Chloroquine Chloroquine - pharmacology Chloroquine - therapeutic use Control Drug resistance Drug Resistance - genetics Drug therapy Drugs Enzyme kinetics Evaluation Gene mutations Health aspects Hemoglobin Humans Identification and classification Kinetics Malaria Malaria, Falciparum - drug therapy Medicine and Health Sciences Molecular docking Molecular dynamics Mutation Parasites Physical Sciences Plasmodium falciparum Plasmodium falciparum - genetics Plasmodium falciparum - metabolism Prevention Protozoan Proteins - metabolism Quinoline Quinolines - pharmacology Quinolines - therapeutic use Research and Analysis Methods Risk factors Substrates Vector-borne diseases
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