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antimalarial drug

NOT Open Access | A role for the succinate dehydrogenase in the mode of action of the redox-active antimalarial drug, plasmodione

November 25, 2020 - 13:05 -- NOT Open Access
Author(s): 
Mounkoro P, Michel T, Golinelli-Cohen MP, Blandin S, Davioud-Charvet E, Meunier B
Reference: 
Free Radic Biol Med. 2020 Nov 21:S0891-5849(20)31608-7

Malaria, caused by protozoan parasites, is a major public health issue in subtropical countries. An arsenal of antimalarial treatments is available, however, resistance is spreading, calling for the development of new antimalarial compounds. The new lead antimalarial drug plasmodione is a redox-active compound that impairs the redox balance of parasites leading to cell death.

A Photoalkylative Fluorogenic Probe of Guttiferone A for Live Cell Imaging and Proteome Labeling in Plasmodium falciparum

November 14, 2020 - 16:31 -- Open Access
Author(s): 
Duval R, Cottet K, Blaud M, Merckx A, Houzé S, Grellier P, Lallemand MC, Michel S
Reference: 
Molecules. 2020 Nov 4;25(21):E5139

Guttiferone A (GA) 1, a polycyclic polyprenylated acylphloroglucinol (PPAP) isolated from the plant Symphonia globulifera (Clusiaceae), constitutes a novel hit in antimalarial drug discovery. PPAPs do not possess identified biochemical targets in malarial parasites up to now. Towards this aim, we designed and evaluated a natural product-derived photoactivatable probe AZC-GA 5, embedding a photoalkylative fluorogenic motif of the 7-azidocoumarin (AZC) type, devoted to studying the affinity proteins interacting with GA in Plasmodium falciparum.

Transmission of artemisinin-resistant malaria parasites to mosquitoes under antimalarial drug pressure

November 4, 2020 - 14:46 -- Open Access
Author(s): 
Witmer K, Dahalan FA, Baum J, et al.
Reference: 
Antimicrob Agents Chemother. 2020 Nov 2:AAC.00898-20

Resistance to artemisinin-based combination therapy (ACT) in the Plasmodium falciparum parasite is threatening to reverse recent gains in reducing global deaths from malaria. Whilst resistance manifests as delayed parasite clearance in patients the phenotype can only spread geographically via the sexual stages and mosquito transmission. In addition to their asexual killing properties, artemisinin and its derivatives sterilise sexual male gametocytes.

Artemisinin exposure at the ring or trophozoite stage impacts Plasmodium falciparum sexual conversion differently

October 22, 2020 - 15:52 -- Open Access
Author(s): 
Portugaliza HP, Miyazaki S, Geurten FJ, Pell C, Rosanas-Urgell A, Janse CJ, Cortés A
Reference: 
Elife. 2020 Oct 21;9:e60058

Malaria transmission is dependent on the formation of gametocytes in the human blood. The sexual conversion rate, the proportion of asexual parasites that convert into gametocytes at each multiplication cycle, is variable and reflects the relative parasite investment between transmission and maintaining the infection. The impact of environmental factors such as drugs on sexual conversion rates is not well understood.

NOT Open Access | Regioisomerization of antimalarial drug WR99210 explains the inactivity of a commercial stock

October 21, 2020 - 09:24 -- NOT Open Access
Author(s): 
Remcho TP, Guggilapu SD, Cruz P, Nardone GA, Heffernan G, O'Connor RD, Bewley CA, Wellems TE, Lane KD
Reference: 
Antimicrob Agents Chemother. 2020 Oct 19:AAC.01385-20

WR99210, a former antimalarial drug candidate now widely used for the selection of Plasmodium transfectants, selectively targets the parasite dihydrofolate reductase thymidine synthase bifunctional enzyme (DHFR-TS) but not human DHFR, which is not fused with TS. Accordingly, WR99210 and plasmids expressing human dhfr have become valued tools for the genetic modification of parasites in the laboratory.

Finding the Dose for Hydroxychloroquine Prophylaxis for COVID-19: The Desperate Search for Effectiveness

October 7, 2020 - 16:11 -- Open Access
Author(s): 
Al-Kofahi M, Jacobson P, Boulware DR, Matas A, Kandaswamy R, Jaber MM, Rajasingham R, Young JH, Nicol MR
Reference: 
Clin Pharmacol Ther. 2020 Oct;108(4):766-769

Hydroxychloroquine is an antimalarial drug being tested as a potential treatment for the novel coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2. Although the efficacy of hydroxychloroquine for COVID-19 remains uncertain, it may serve as a potential prophylactic agent especially in those at high risk, such as healthcare workers, household contacts of infected patients, and the immunocompromised.

A machine learning approach to define antimalarial drug action from heterogeneous cell-based screens

September 29, 2020 - 13:06 -- Open Access
Author(s): 
Ashdown GW, Dimon M, Fan M, Sánchez-Román Terán F, Witmer K, Gaboriau DCA, Armstrong Z, Ando DM, Baum J
Reference: 
Sci Adv. 2020 Sep 25;6(39):eaba9338

Drug resistance threatens the effective prevention and treatment of an ever-increasing range of human infections. This highlights an urgent need for new and improved drugs with novel mechanisms of action to avoid cross-resistance.

Anti-SARS-CoV-2 Potential of Artemisinins In Vitro

September 15, 2020 - 10:05 -- Open Access
Author(s): 
Cao R, Hu H, Li Y, Wang X, Xu M, Liu J, Zhang H, Yan Y, Zhao L, Li W, Zhang T, Xiao D, Guo X, Li Y, Yang J, Hu Z, Wang M, Zhong W
Reference: 
ACS Infect Dis. 2020 Sep 11;6(9):2524-2531

The discovery of novel drug candidates with anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) potential is critical for the control of the global COVID-19 pandemic. Artemisinin, an old antimalarial drug derived from Chinese herbs, has saved millions of lives. Artemisinins are a cluster of artemisinin-related drugs developed for the treatment of malaria and have been reported to have multiple pharmacological activities, including anticancer, antiviral, and immune modulation.

Global research on artemisinin and its derivatives: Perspectives from patents

September 5, 2020 - 15:40 -- Open Access
Author(s): 
Liu K, Zuo H, Li G, Yu H, Hu Y
Reference: 
Pharmacol Res. 2020 Sep;159:105048

The isolation of artemisinin in 1971 heralded the beginning of a new era in antimalarial drug therapy, and artemisinin-based combination therapies are currently the mainstay of malaria treatment worldwide. Artemisinin-related studies have been extensively and intensively executed in the last few decades. However, although many purely technological reviews have been completed in this field, studies on artemisinin from the perspective of patents are still very limited. In terms of the importance of patents for academic research and commercial development, this study aims to reveal the overall patent landscape of artemisinin in the temporal, spatial, and technological dimensions. This work may provide a useful reference for relevant decision-making by researchers, investors, and policymakers.

Design and tests of prospective property predictions for novel antimalarial 2-aminopropylaminoquinolones

August 25, 2020 - 08:56 -- Open Access
Author(s): 
Clark RD, Morris DN, Chinigo G, Lawless MS, Prudhomme J, Le Roch KG, Lafuente MJ, Ferrer S, Gamo FJ, Gadwood R, Woltosz WS
Reference: 
J Comput Aided Mol Des. 2020 Aug 24

There is a pressing need to improve the efficiency of drug development, and nowhere is that need more clear than in the case of neglected diseases like malaria. The peculiarities of pyrimidine metabolism in Plasmodium species make inhibition of dihydroorotate dehydrogenase (DHODH) an attractive target for antimalarial drug design. By applying a pair of complementary quantitative structure-activity relationships derived for inhibition of a truncated, soluble form of the enzyme from Plasmodium falciparum (s-PfDHODH) to data from a large-scale phenotypic screen against cultured parasites, we were able to identify a class of antimalarial leads that inhibit the enzyme and abolish parasite growth in blood culture.

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