Specific Inhibitors of Plasmodium falciparum Thioredoxin Reductase as Potential Antimalarial Agents.

ChemInform ◽  
2006 ◽  
Vol 37 (30) ◽  
Author(s):  
A. D. Adricopulo ◽  
M. B. Akoachere ◽  
R. Krogh ◽  
C. Nickel ◽  
M. J. McLeish ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Thioredoxin Reductase ◽  
Antimalarial Agents ◽  
Specific Inhibitors

Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents

2006 ◽  
Vol 16 (8) ◽  
pp. 2283-2292 ◽  
Author(s):  
A.D. Andricopulo ◽  
M.B. Akoachere ◽  
R. Krogh ◽  
C. Nickel ◽  
M.J. McLeish ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Thioredoxin Reductase ◽  
Antimalarial Agents ◽  
Specific Inhibitors

The development of quinoloneesters as novel antimalarial agents targeting the Plasmodium falciparum bc1protein complex

MedChemComm ◽  
2012 ◽  
Vol 3 (1) ◽  
pp. 39-44 ◽  
Author(s):  
Robin Cowley ◽  
Suet Leung ◽  
Nicholas Fisher ◽  
Mohammed Al-Helal ◽  
Neil G. Berry ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Agents

scholarly journals Plasmodium falciparum Thioredoxin Reductase (PfTrxR) and Its Role as a Target for New Antimalarial Discovery

Molecules ◽  
2015 ◽  
Vol 20 (6) ◽  
pp. 11459-11473 ◽  
Author(s):  
Sara McCarty ◽  
Amanda Schellenberger ◽  
Douglas Goodwin ◽  
Ngolui Fuanta ◽  
Babu Tekwani ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Thioredoxin Reductase

A proteomic glimpse into the effect of antimalarial drugs on Plasmodium falciparum proteome towards highlighting possible therapeutic targets

2020 ◽  
Author(s):  
Majid Dousti ◽  
Raúl Manzano-Román ◽  
Sajad Rashidi ◽  
Gholamreza Barzegar ◽  
Niloofar Bavarsad Ahmadpour ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Calcium Binding ◽  
Drug Targets ◽  
Thioredoxin Reductase ◽  
Resistance Mechanisms ◽  
Antimalarial Drugs ◽  
Effective Vaccine ◽  
Apical Membrane Antigen 1 ◽  
Clinic Management ◽  
Altered Proteins

Abstract There is no effective vaccine against malaria; therefore, chemotherapy is to date only choice to fight against this infectious disease. However, there are growing evidences of drug-resistance mechanisms in malaria treatments. Therefore, the identification of new drug targets is an urgent need for the clinic management of the disease. Proteomic approaches offer the chance of determining the effects of antimalarial drugs on the proteome of Plasmodium parasites. Accordingly, we here review the effects of antimalarial drugs on Plasmodium falciparum proteome pointing out the relevance of several proteins as possible drug targets in malaria treatment. In addition, some of the P. falciparum stage-specific altered proteins and parasite-host interactions might play important roles in pathogenicity, survival, invasion, and metabolic pathways and thus serve as potential source of drug targets. In this review, we have identified several proteins including thioredoxin reductase, helicases, peptidyl-prolyl cis-trans isomerase, endoplasmic reticulum-resident calcium-binding protein, choline/ethanolamine phosphotransferase, purine nucleoside phosphorylase, apical membrane antigen 1, glutamate dehydrogenase, hypoxanthine guanine phosphoribosyl transferase, heat shock protein70x, knob-associated histidine-rich protein, and erythrocyte membrane protein 1 as promising antimalarial drugs targets. Overall, proteomic approaches are able to partially facilitate finding the possible drug targets. However, the integration of other ‘omics’ and specific pharmaceutical techniques with proteomics may increase the therapeutic properties of the critical proteins identified in P. falciparum proteome.

Recombinant putative glutathione reductase of Plasmodium falciparum exhibits thioredoxin reductase activity

1996 ◽  
Vol 80 (2) ◽  
pp. 215-219 ◽  
Author(s):  
Sylke Müller ◽  
Tim-Wolf Gilberger ◽  
Petra M. Färber ◽  
Katja Becker ◽  
R. Heiner Schirmer ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Glutathione Reductase ◽  
Reductase Activity ◽  
Thioredoxin Reductase

scholarly journals Artemisone and Artemiside Are Potent Panreactive Antimalarial Agents That Also Synergize Redox Imbalance in Plasmodium falciparum Transmissible Gametocyte Stages

2018 ◽  
Vol 62 (8) ◽  
Author(s):  
Dina Coertzen ◽  
Janette Reader ◽  
Mariëtte van der Watt ◽  
Sindisiwe H. Nondaba ◽  
Liezl Gibhard ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Control ◽  
Malaria Parasite ◽  
Redox Homeostasis ◽  
New Drugs ◽  
Content Type ◽  
Artemisinin Derivatives ◽  
Antimalarial Agents ◽  
Redox Partner ◽  
Emergence Of Resistance

ABSTRACT The emergence of resistance toward artemisinin combination therapies (ACTs) by the malaria parasite Plasmodium falciparum has the potential to severely compromise malaria control. Therefore, the development of new artemisinins in combination with new drugs that impart activities toward both intraerythrocytic proliferative asexual and transmissible gametocyte stages, in particular, those of resistant parasites, is urgently required. We define artemisinins as oxidant drugs through their ability to oxidize reduced flavin cofactors of flavin disulfide reductases critical for maintaining redox homeostasis in the malaria parasite. Here we compare the activities of 10-amino artemisinin derivatives toward the asexual and gametocyte stages of P. falciparum parasites. Of these, artemisone and artemiside inhibited asexual and gametocyte stages, particularly stage V gametocytes, in the low-nanomolar range. Further, treatment of both early and late gametocyte stages with artemisone or artemiside combined with the pro-oxidant redox partner methylene blue displayed notable synergism. These data suggest that modulation of redox homeostasis is likely an important druggable process, particularly in gametocytes, and this finding thereby enhances the prospect of using combinations of oxidant and redox drugs for malaria control.

scholarly journals Discovery of oxybisbenzoylamides as a new class of antimalarial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (6) ◽  
pp. 1173-1177 ◽  
Author(s):  
A. Pancotti ◽  
S. Parapini ◽  
M. Dell'Agli ◽  
L. Gambini ◽  
C. Galli ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
New Class ◽  
Antimalarial Agents ◽  
Dual Inhibitors

A new antimalarial pharmacophore has been obtained starting from previously described dual inhibitors of Plasmodium falciparum.

Crystal Structure of the Plasmodium falciparum Thioredoxin Reductase–Thioredoxin Complex

2013 ◽  
Vol 425 (18) ◽  
pp. 3446-3460 ◽  
Author(s):  
Karin Fritz-Wolf ◽  
Esther Jortzik ◽  
Michaela Stumpf ◽  
Janina Preuss ◽  
Rimma Iozef ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Plasmodium Falciparum ◽  
Thioredoxin Reductase
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