[PDF][PDF] Mutations in the P. falciparum digestive vacuole transmembrane protein PfCRT and evidence for their role in chloroquine resistance

…, B Naudé, KW Deitsch, X Su, JC Wootton, PD Roepe… - Molecular cell, 2000 - cell.com
The determinant of verapamil-reversible chloroquine resistance (CQR) in a Plasmodium
falciparum genetic cross maps to a 36 kb segment of chromosome 7. This segment harbors a 13…

Novel, rapid, and inexpensive cell-based quantification of antimalarial drug efficacy

…, AD Kosar, E Davidson, PD Roepe - Antimicrobial agents …, 2004 - Am Soc Microbiol
We report on the development of a new SYBR Green I-based plate assay for analyzing the
activities of antimalarial drugs against intraerythrocytic Plasmodium falciparum. This assay is …

Alternative mutations at position 76 of the vacuolar transmembrane protein PfCRT are associated with chloroquine resistance and unique stereospecific quinine and …

…, J Mu, T Nomura, H Fujioka, DA Fidock, PD Roepe… - Molecular …, 2002 - ASPET
Chloroquine resistance (CQR) in Plasmodium falciparum is associated with multiple mutations
in the digestive vacuole membrane protein PfCRT. The chloroquine-sensitive (CQS) 106/…

Quinoline drug–heme interactions and implications for antimalarial cytostatic versus cytocidal activities

AP Gorka, A de Dios, PD Roepe - Journal of medicinal chemistry, 2013 - ACS Publications
D. at Georgetown University, Washington, DC, under Dr. Paul Roepe, where he investigated
the cytostatic and cytocidal mechanisms of quinoline drug resistance in Plasmodium …

Evolution of a unique Plasmodium falciparum chloroquine-resistance phenotype in association with pfcrt polymorphism in Papua New Guinea and South America

RK Mehlotra, H Fujioka, PD Roepe… - Proceedings of the …, 2001 - National Acad Sciences
The mechanistic basis for chloroquine resistance (CQR) in Plasmodium falciparum recently
has been linked to the polymorphic gene pfcrt. Alleles associated with CQR in natural …

Solution structures of antimalarial drug− heme complexes

…, LMB Ursos, D Sears, AC De Dios, PD Roepe - Biochemistry, 2002 - ACS Publications
Paramagnetic metal centers [such as Fe III found within ferriprotoporphyrin IX heme (FPIX)]
exert through space effects on the relaxation rate of nearby proton spins that depend critically …

Structure and drug resistance of the Plasmodium falciparum transporter PfCRT

…, SI Giacometti, AL Warren, K Nosol, PD Roepe… - Nature, 2019 - nature.com
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 …

4-N-, 4-S-, and 4-O-Chloroquine Analogues: Influence of Side Chain Length and Quinolyl Nitrogen pKa on Activity vs Chloroquine Resistant Malaria

…, AC De Dios, C Wolf, PD Roepe - Journal of medicinal …, 2008 - ACS Publications
Using predictions from heme−quinoline antimalarial complex structures, previous modifications
of chloroquine (CQ), and hypotheses for chloroquine resistance (CQR), we synthesize …

Drug resistance-associated pfCRT mutations confer decreased Plasmodium falciparum digestive vacuolar pH

…, S Dzekunov, ABS Sidhu, DA Fidock, PD Roepe - Molecular and …, 2004 - Elsevier
Elucidating the altered physiology of various chloroquine resistant (CQR) strains of Plasmodium
falciparum is essential for understanding the molecular basis of CQR. In this study, we …

[HTML][HTML] Chloroquine resistance modulated in vitro by expression levels of the Plasmodium falciparum chloroquine resistance transporter

…, ABS Sidhu, H Fujioka, PD Roepe… - Journal of Biological …, 2003 - ASBMB
Plasmodium falciparum malaria is increasingly difficult to treat and control due to the emergence
of parasite resistance to the major antimalarials, notably chloroquine. Recent work has …