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Synthesis, Structure-Activity Relationship, and Mode-of-Action Studies of Antimalarial Reversed Chloroquine Compounds

August 10, 2010 - 08:20 -- Kabogo Ndegwa
SJ Burgess, JX Kelly, S Shomloo, S Wittlin, R Brun, K Liebmann, DH Peyton
J. Med. Chem. August 4, 2010

We have previously shown that a "reversed chloroquine (RCQ)" molecule, composed of a chloroquine-like moiety and a resistance reversal-like moiety, can overcome chloroquine resistance in P. falciparum

Characterization of coproporphyrinogen III oxidase in Plasmodium falciparum cytosol

May 5, 2010 - 09:25 -- Patrick Sampao
Viswanathan Arun Nagaraj, Dasari Prasad, Rajavel Arumugam, Pundi N. Rangarajan, Govindarajan Padmanaban
Parasitology International, Volume 59, Issue 2, June 2010, Pages 121-127

In this study, a recombinant P. falciparum coproporphyrinogen III oxidase (rPfCPO) was produced in E. coli and confirmed to be active under aerobic conditions.

Short communication: Target proteins of the cytosolic thioredoxin in Plasmodium falciparum

May 5, 2010 - 08:55 -- Patrick Sampao
Shin-ichiro Kawazu, Hitoshi Takemae, Kanako Komaki-Yasuda, Shigeyuki Kano
Parasitology International, Volume 59, Issue 2, June 2010, Pages 298-302

We captured 4 enzymes in the glycolysis pathway (hexokinase, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), phosphoglycerate mutase and l-lactate dehydrogenase (LDH)) as Trx-targets, and we found that PfTrx-1 enhanced the activity of PfGAPDH and PfLDH.

Induction of cell death on Plasmodium falciparum asexual blood stages by Solanum nudum steroids

May 5, 2010 - 08:20 -- Patrick Sampao
Mary Luz López, Rossiane Vommaro, Mariano Zalis, Wanderley de Souza, Silvia Blair, Cesar Segura
Parasitology International, Volume 59, Issue 2, June 2010, Pages 217-225

Thus, the aim of this work was to determine the effects of S. nudum compounds on P. falciparum asexual blood stages and their association with cell death. We found that trophozoite and schizont stages were the most sensitive to SNs.

Natural regulatory T cells mediate the development of cerebral malaria by modifying the pro-inflammatory response

May 5, 2010 - 07:48 -- Patrick Sampao
Jing-jing Wu, Guang Chen, Jun Liu, Tao Wang, Wei Zheng, Ya-Ming Cao
Parasitology International, Volume 59, Issue 2, June 2010, Pages 232-241

Our data demonstrate that Tregs mediate the incidence and outcome of CM in P.bANKA-infected mice by modifying the pro-inflammatory response.

Interaction between Plasmodium falciparum Apical Membrane Antigen 1 and the Rhoptry Neck Protein Complex Defines a Key Step in the Erythrocyte Invasion Process of Malaria Parasites

May 3, 2010 - 14:12 -- Patrick Sampao
Dave R., Christopher A., et al.
The Journal of Biological Chemistry, 285, 14815-14822.

Here we show that the R1 peptide binds the PfAMA1 hydrophobic trough and demonstrate that binding to this region prevents its interaction with the PfRON complex. We show that this defined association between PfAMA1 and the PfRON complex occurs after reorientation and engagement of the actomyosin motor and argue that it precedes rhoptry release.


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