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antimalarial drugs

Artemisinin susceptibility in the malaria parasite Plasmodium falciparum: propellers, adaptor proteins and the need for cellular healing

May 12, 2021 - 12:39 -- Open Access
Author(s): 
Sutherland CJ, Henrici RC, Artavanis-Tsakonas K
Reference: 
FEMS Microbiol Rev. 2021 May 5;45(3):fuaa056

Studies of the susceptibility of Plasmodium falciparum to the artemisinin family of antimalarial drugs provide a complex picture of partial resistance (tolerance) associated with increased parasite survival in vitro and in vivo.

The integrity and stability of specimens under different storage conditions for glucose-6-phosphate dehydrogenase deficiency screening using WST-8

May 5, 2021 - 08:56 -- Open Access
Author(s): 
Chamchoy K, Praoparotai A, Pakparnich P, Sudsumrit S, Swangsri T, Chamnanchanunt S, Songdej D, Imwong M, Boonyuen U
Reference: 
Acta Trop. 2021 May;217:105864

Accurate measurement of glucose-6-phosphate dehydrogenase (G6PD) activity is critical for malaria treatment as misclassification of G6PD deficiency could cause serious harm to patients. G6PD activity should be assessed in blood samples on the day of collection. Otherwise, specimens should be stored under suitable conditions to prevent loss of G6PD activity.

NOT Open Access | Design, Synthesis, and Structural Analysis of Cladosporin-Based Inhibitors of Malaria Parasites

April 13, 2021 - 13:26 -- NOT Open Access
Author(s): 
Babbar P, Das P, Manickam Y, Mankad Y, Yadav S, Parvez S, Sharma A, Reddy DS
Reference: 
ACS Infect Dis. 2021 Apr 12

Here we have described a systematic structure activity relationship (SAR) of a set of compounds inspired from cladosporin, a tool compound that targets parasite (Plasmodium falciparum) lysyl tRNA synthetase (KRS). Four sets of analogues, synthesized based on point changes in the chemical scaffold of cladosporin and other logical modifications and hybridizations, were assessed using high throughput enzymatic and parasitic assays along with in vitro pharmacokinetics.

Violacein-Induced Chaperone System Collapse Underlies Multistage Antiplasmodial Activity

April 13, 2021 - 13:07 -- Open Access
Author(s): 
Tavella TA, da Silva NSM, Maranhão Costa FT, et al.
Reference: 
ACS Infect Dis. 2021 Apr 9;7(4):759-776

Antimalarial drugs with novel modes of action and wide therapeutic potential are needed to pave the way for malaria eradication. Violacein is a natural compound known for its biological activity against cancer cells and several pathogens, including the malaria parasite, Plasmodium falciparum (Pf). Herein, using chemical genomic profiling (CGP), we found that violacein affects protein homeostasis. Mechanistically, violacein binds Pf chaperones, PfHsp90 and PfHsp70-1, compromising the latter's ATPase and chaperone activities.

Hydroxychloroquine Controversies: Clinical Trials, Epistemology, and the Democratization of Science

November 19, 2020 - 13:23 -- Open Access
Author(s): 
Berlivet L, Löwy I
Reference: 
Med Anthropol Q. 2020 Nov 18

The claim that anti-malaria drugs, chloroquine and hydroxychloroquine, can cure COVID-19 became a focus of fierce political battles that pitted promoters of these pharmaceuticals, Presidents Bolsonaro and Trump among them, against "medical elites." At the center of these battles are different meanings of effectiveness in medicine, the complex role of randomized clinical trials (RCTs) in proving such effectiveness, the task of medical experts and the state in regulating pharmaceuticals, patients' activism, and the collective production of medical knowledge.

Inhibition of Plasmodium falciparum Lysyl-tRNA synthetase via an anaplastic lymphoma kinase inhibitor

November 19, 2020 - 13:15 -- Open Access
Author(s): 
Zhou J, Huang Z, Zheng L, Hei Z, Wang Z, Yu B, Jiang L, Wang J, Fang P
Reference: 
Nucleic Acids Res. 2020 Nov 18;48(20):11566-11576

Aminoacyl-tRNA synthetases are attractive targets for the development of antibacterial, antifungal, antiparasitic agents and for the treatment of other human diseases. Lysyl-tRNA synthetase (LysRS) from this family has been validated as a promising target for the development of antimalarial drugs. Here, we developed a high-throughput compatible assay and screened 1215 bioactive compounds to identify Plasmodium falciparum cytoplasmic LysRS (PfLysRS) inhibitor.

Targeting the CD146/Galectin-9 axis protects the integrity of the blood-brain barrier in experimental cerebral malaria

November 19, 2020 - 13:08 -- Open Access
Author(s): 
Duan H, Zhao S, Xiang J, Ju C, Chen X, Gramaglia I, Yan X
Reference: 
Cell Mol Immunol. 2020 Nov 17

Cerebral malaria (CM) is a life-threatening diffuse encephalopathy caused by Plasmodium falciparum, in which the destruction of the blood-brain barrier (BBB) is the main cause of death. However, increasing evidence has shown that antimalarial drugs, the current treatment for CM, do little to protect against CM-induced BBB damage. Therefore, a means to alleviate BBB dysfunction would be a promising adjuvant therapy for CM.

NOT Open Access | A proteomic glimpse into the effect of antimalarial drugs on Plasmodium falciparum proteome towards highlighting possible therapeutic targets

November 18, 2020 - 12:25 -- NOT Open Access
Author(s): 
Dousti M, Manzano-Román R, Rashidi S, Barzegar G, Ahmadpour NB, Mohammadi A, Hatam G
Reference: 
Pathog Dis. 2020 Nov 17:ftaa071

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.

Plasmodium berghei K13 Mutations Mediate In Vivo Artemisinin Resistance That Is Reversed by Proteasome Inhibition

November 11, 2020 - 14:33 -- Open Access
Author(s): 
Simwela NV, Stokes BH, Aghabi D, Bogyo M, Fidock DA, Waters AP
Reference: 
mBio. 2020 Nov 10;11(6):e02312-20

The recent emergence of Plasmodium falciparum parasite resistance to the first line antimalarial drug artemisinin is of particular concern. Artemisinin resistance is primarily driven by mutations in the P. falciparum K13 protein, which enhance survival of early ring-stage parasites treated with the artemisinin active metabolite dihydroartemisinin in vitro and associate with delayed parasite clearance in vivo However, association of K13 mutations with in vivo artemisinin resistance has been problematic due to the absence of a tractable model.

An Update on Development of Small-Molecule Plasmodial Kinase Inhibitors

November 11, 2020 - 14:13 -- Open Access
Author(s): 
Moolman C, Sluis RV, Beteck RM, Legoabe LJ
Reference: 
Molecules. 2020 Nov 7;25(21):E518

Malaria control relies heavily on the small number of existing antimalarial drugs. However, recurring antimalarial drug resistance necessitates the continual generation of new antimalarial drugs with novel modes of action. In order to shift the focus from only controlling this disease towards elimination and eradication, next-generation antimalarial agents need to address the gaps in the malaria drug arsenal.

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