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Journal articles on the topic 'Artemisinin, Syk Inhibitor, Artemisinin resistance'

Author: Grafiati

Published: 11 March 2023

Last updated: 31 July 2025

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1

Tsamesidis, Ioannis, Karine Reybier, Giuseppe Marchetti, et al. "Syk Kinase Inhibitors Synergize with Artemisinins by Enhancing Oxidative Stress in Plasmodium falciparum-Parasitized Erythrocytes." Antioxidants 9, no. 8 (2020): 753. http://dx.doi.org/10.3390/antiox9080753.

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Although artemisinin-based combination therapies (ACTs) treat Plasmodium falciparum malaria effectively throughout most of the world, the recent expansion of ACT-resistant strains in some countries of the Greater Mekong Subregion (GMS) further increased the interest in improving the effectiveness of treatment and counteracting resistance. Recognizing that (1) partially denatured hemoglobin containing reactive iron (hemichromes) is generated in parasitized red blood cells (pRBC) by oxidative stress, (2) redox-active hemichromes have the potential to enhance oxidative stress triggered by the par

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Marchetti, Giuseppe, Alessandro Dessì, Roberto Dallocchio, et al. "Syk Inhibitors: New Computational Insights into Their Intraerythrocytic Action in Plasmodium falciparum Malaria." International Journal of Molecular Sciences 21, no. 19 (2020): 7009. http://dx.doi.org/10.3390/ijms21197009.

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Resistance to antimalarial drugs has spread rapidly over the past few decades. The WHO recommends artemisinin-based combination therapies for the treatment of uncomplicated malaria, but unfortunately these approaches are losing their efficacy in large areas of Southeast Asia. In 2016, artemisinin resistance was confirmed in 5 countries of the Greater Mekong subregion. We focused our study on Syk inhibitors as antimalarial drugs. The Syk protein is present in human erythrocytes, and the membrane of protein band 3 is its major target following activation by oxidant stress. Tyr phosphorylation of

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Kimata-Ariga, Yoko, and Rena Morihisa. "Effect of Artemisinin on the Redox System of NADPH/FNR/Ferredoxin from Malaria Parasites." Antioxidants 11, no. 2 (2022): 273. http://dx.doi.org/10.3390/antiox11020273.

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FNR and ferredoxin constitute a redox cascade, which provides reducing power in the plastid of malaria parasites. Recently, mutation of ferredoxin (D97Y) was reported to be strongly related to the parasite’s resistance to the front-line antimalarial drug artemisinin. In order to gain insight into the mechanism for the resistance, we studied the effect of dihydroartemisinin (DHA), the active compound of artemisinin, on the redox cascade of NADPH/FNR/ferredoxin in in vitro reconstituted systems. DHA partially inhibited the diaphorase activity of FNR by decreasing the affinity of FNR for NADPH. T

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Yang, Chao, Lijun Ge, Xiyong Yu, Philip Lazarovici, and Wenhua Zheng. "Artemisinin Confers Cytoprotection toward Hydrogen Peroxide-Induced Cell Apoptosis in Retinal Pigment Epithelial Cells in Correlation with the Increased Acetylation of Histone H4 at Lysine 8." Molecules 29, no. 8 (2024): 1789. http://dx.doi.org/10.3390/molecules29081789.

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Increased oxidative stress is one of the critical pathologies inducing age-related macular degeneration (AMD), characterized by retinal pigment epithelial (RPE) cell damage and death. The unbalanced acetylation and deacetylation of histones have been implicated in AMD pathogenesis or hydrogen peroxide (H2O2)-induced cell damage. Therefore, strategies aimed at controlling the balance between acetylation and deacetylation may effectively protect RPE cells from oxidative damage. Artemisinin is an antimalarial lactone drug derived from Artemisia annua, with antioxidant activity known to modulate h

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Pratama, Mohammad Rizki Fadhil, and Tutus Gusdinar. "BETWEEN ARTEMISININ AND DERIVATIVES WITH NEURAMINIDASE: A DOCKING STUDY INSIGHT." Asian Journal of Pharmaceutical and Clinical Research 10, no. 8 (2017): 304. http://dx.doi.org/10.22159/ajpcr.2017.v10i8.18667.

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Objectives: This study aims to find the relationship between artemisinins and neuraminidase (NA) with molecular docking study and also to determine the most potent NA inhibitor from artemisinin and derivatives.Methods: All ligands were sketched and optimized using Gaussian 03W with Hartree-Fock method basis sets 6-311G. Molecular docking was performed using AutoDock 4.2.3 toward NA in complexes with oseltamivir as co-crystal ligand. The main parameters used were the free energy of binding (ΔG) and dissociation constant (Ki) as affinity marker.Results: Artesunate provided most negative free ΔG

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Lee, Dong-Hwan, Md Hasanuzzaman, Daeho Kwon, et al. "10-Phenyltriazoyl Artemisinin is a Novel P-glycoprotein Inhibitor that Suppresses the Overexpression and Function of P-glycoprotein." Current Pharmaceutical Design 24, no. 46 (2019): 5590–97. http://dx.doi.org/10.2174/1381612825666190222155700.

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Background: The effect of drugs on ATP-binding cassette transporters, especially permeabilityglycoprotein (P-gp), is an important consideration during new anti-cancer drug development. Objective: In this context, the effects of a newly synthesized artemisinin derivative, 10-(4-phenyl-1H-1,2,3- triazol)-artemisinin (5a), were evaluated on P-gp expression and function. Methods: Reverse transcript polymerase chain reaction and immunoblotting techniques were used to determine the effect of 5a on P-gp expression in LS174T cells. In addition, the ability of 5a to work as either a substrate or an inh

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von Bredow, Lukas, Thomas Martin Schäfer, Julian Hogenkamp, et al. "Synthesis, Antiplasmodial, and Antileukemia Activity of Dihydroartemisinin–HDAC Inhibitor Hybrids as Multitarget Drugs." Pharmaceuticals 15, no. 3 (2022): 333. http://dx.doi.org/10.3390/ph15030333.

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Artemisinin-based combination therapies (ACTs) are the gold standard for the treatment of malaria, but the efficacy is threatened by the development of parasite resistance. Histone deacetylase inhibitors (HDACis) are an emerging new class of potential antiplasmodial drugs. In this work, we present the design, synthesis, and biological evaluation of a mini library of dihydroartemisinin–HDACi hybrid molecules. The screening of the hybrid molecules for their activity against selected human HDAC isoforms, asexual blood stage P. falciparum parasites, and a panel of leukemia cell lines delivered imp

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Zhang, Jingyi, Zhenwei Zhang, Samuel Waxman, Linxiang Zhao, and Yongkui Jing. "Abstract 5991: Improved venetoclax therapy by a novel conjugate with artemisinin by NOXA-mediated reduction of Mcl-1 and cyclin D1 protein in myeloid leukemia cells." Cancer Research 84, no. 6_Supplement (2024): 5991. http://dx.doi.org/10.1158/1538-7445.am2024-5991.

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Abstract Evasion of apoptosis is crucial for the growth, survival and chemoresistance of myeloid leukemia. The Bcl-2 selective inhibitor venetoclax is the only apoptosis inducer approved for clinical use. Venetoclax in combination with hypomethylating agents or low-dose cytarabine has now become the standard care for elderly AML patients. However, a sizeable fraction of patients are either refractory to venetoclax combination therapy or ultimately relapse. High or induced expression of Mcl-1 and Bcl-xL mediates venetoclax resistance. Previously we reported that artemisinin enhances venetoclax

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Kirkman, Laura A., Wenhu Zhan, Joseph Visone, et al. "Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance." Proceedings of the National Academy of Sciences 115, no. 29 (2018): E6863—E6870. http://dx.doi.org/10.1073/pnas.1806109115.

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We describe noncovalent, reversible asparagine ethylenediamine (AsnEDA) inhibitors of the Plasmodium falciparum proteasome (Pf20S) β5 subunit that spare all active subunits of human constitutive and immuno-proteasomes. The compounds are active against erythrocytic, sexual, and liver-stage parasites, against parasites resistant to current antimalarials, and against P. falciparum strains from patients in Africa. The β5 inhibitors synergize with a β2 inhibitor in vitro and in mice and with artemisinin. P. falciparum selected for resistance to an AsnEDA β5 inhibitor surprisingly harbored a point m

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Mustière, Romain, Patrice Vanelle, and Nicolas Primas. "Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments." Molecules 25, no. 24 (2020): 5949. http://dx.doi.org/10.3390/molecules25245949.

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Recent progress in reducing malaria cases and ensuing deaths is threatened by factors like mutations that induce resistance to artemisinin derivatives. Multiple drugs are currently in clinical trials for malaria treatment, including some with novel mechanisms of action. One of these, MMV390048, is a plasmodial kinase inhibitor. This review lists the recently developed molecules which target plasmodial kinases. A systematic review of the literature was performed using CAPLUS and MEDLINE databases from 2005 to 2020. It covers a total of 60 articles and describes about one hundred compounds targe

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Pulcini, Serena, Henry M. Staines, Jon K. Pittman, et al. "Expression in Yeast Links Field Polymorphisms in PfATP6 to in Vitro Artemisinin Resistance and Identifies New Inhibitor Classes." Journal of Infectious Diseases 208, no. 3 (2013): 468–78. http://dx.doi.org/10.1093/infdis/jit171.

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Bao, Changlei, Qian He, Hui Wang, et al. "Artemisinin and Its Derivate Alleviate Pulmonary Hypertension and Vasoconstriction in Rodent Models." Oxidative Medicine and Cellular Longevity 2022 (June 17, 2022): 1–21. http://dx.doi.org/10.1155/2022/2782429.

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Background. Pulmonary arterial hypertension (PAH) is a complex pulmonary vasculature disease characterized by progressive obliteration of small pulmonary arteries and persistent increase in pulmonary vascular resistance, resulting in right heart failure and death if left untreated. Artemisinin (ARS) and its derivatives, which are common antimalarial drugs, have been found to possess a broad range of biological effects. Here, we sought to determine the therapeutic benefit and mechanism of ARS and its derivatives treatment in experimental pulmonary hypertension (PH) models. Methods. Isolated per

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Ukpe, Ajima, O. Onah Johnson, N. Wannang Noel, and Gurumtet Istifanus. "Synthesis and Antimalarial Evaluation of a Dihydroartemisinin - Histone Deacetylase Inhibitor Conjugate." Pharmaceutical and Chemical Journal 7, no. 4 (2020): 30–42. https://doi.org/10.5281/zenodo.13955220.

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Malaria is a tropical disease caused by several species of the <em>Plasmodium</em> genus with <em>P. falciparum</em> being the most prevalent and dangerous specie. Despite the plethora of antimalarial drugs available, there is still the pressing need to develop new agents to treat the disease; this is due to problems with existing medications such as toxicity and parasite resistance to previously effective drugs. Histone deacetylase enzyme catalyzes the removal of the acetyl group from histone lysine residues and has been shown to play a key role in the regulation of gene expression in the pla

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Biosca, Arnau, Miriam Ramírez, Alex Gomez-Gomez, et al. "Characterization of Domiphen Bromide as a New Fast-Acting Antiplasmodial Agent Inhibiting the Apicoplastidic Methyl Erythritol Phosphate Pathway." Pharmaceutics 14, no. 7 (2022): 1320. http://dx.doi.org/10.3390/pharmaceutics14071320.

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The evolution of resistance by the malaria parasite to artemisinin, the key component of the combination therapy strategies that are at the core of current antimalarial treatments, calls for the urgent identification of new fast-acting antimalarials. The apicoplast organelle is a preferred target of antimalarial drugs because it contains biochemical processes absent from the human host. Fosmidomycin is the only drug in clinical trials targeting the apicoplast, where it inhibits the methyl erythritol phosphate (MEP) pathway. Here, we characterized the antiplasmodial activity of domiphen bromide

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Malmquist, Nicholas A., Sandeep Sundriyal, Joachim Caron, et al. "Histone Methyltransferase Inhibitors Are Orally Bioavailable, Fast-Acting Molecules with Activity against Different Species Causing Malaria in Humans." Antimicrobial Agents and Chemotherapy 59, no. 2 (2014): 950–59. http://dx.doi.org/10.1128/aac.04419-14.

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ABSTRACTCurrent antimalarials are under continuous threat due to the relentless development of drug resistance by malaria parasites. We previously reported promisingin vitroparasite-killing activity with the histone methyltransferase inhibitor BIX-01294 and its analogue TM2-115. Here, we further characterize these diaminoquinazolines forin vitroandin vivoefficacy and pharmacokinetic properties to prioritize and direct compound development. BIX-01294 and TM2-115 displayed potentin vitroactivity, with 50% inhibitory concentrations (IC50s) of <50 nM against drug-sensitive laboratory strains an

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Kampoun, Tanyaluck, Pimpisid Koonyosying, Jetsada Ruangsuriya, et al. "Antagonistic antimalarial properties of a methoxyamino chalcone derivative and 3-hydroxypyridinones in combination with dihydroartemisinin against Plasmodium falciparum." PeerJ 11 (April 27, 2023): e15187. http://dx.doi.org/10.7717/peerj.15187.

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Background The spread of artemisinin (ART)-resistant Plasmodium falciparum threatens the control of malaria. Mutations in the propeller domains of P. falciparum Kelch13 (k13) are strongly associated with ART resistance. Ferredoxin (Fd), a component of the ferredoxin/NADP+ reductase (Fd/FNR) redox system, is essential for isoprenoid precursor synthesis in the plasmodial apicoplast, which is important for K13-dependent hemoglobin trafficking and ART activation. Therefore, Fd is an antimalarial drug target and fd mutations may modulate ART sensitivity. We hypothesized that loss of Fd/FNR function

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Langlais, David, Regina Cencic, Neda Moradin, et al. "Rocaglates as dual-targeting agents for experimental cerebral malaria." Proceedings of the National Academy of Sciences 115, no. 10 (2018): E2366—E2375. http://dx.doi.org/10.1073/pnas.1713000115.

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Cerebral malaria (CM) is a severe and rapidly progressing complication of infection by Plasmodium parasites that is associated with high rates of mortality and morbidity. Treatment options are currently few, and intervention with artemisinin (Art) has limited efficacy, a problem that is compounded by the emergence of resistance to Art in Plasmodium parasites. Rocaglates are a class of natural products derived from plants of the Aglaia genus that have been shown to interfere with eukaryotic initiation factor 4A (eIF4A), ultimately blocking initiation of protein synthesis. Here, we show that the

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Birrell, Geoffrey W., Matthew P. Challis, Amanda De Paoli, et al. "Multi-omic Characterization of the Mode of Action of a Potent New Antimalarial Compound, JPC-3210, Against Plasmodium falciparum." Molecular & Cellular Proteomics 19, no. 2 (2019): 308–25. http://dx.doi.org/10.1074/mcp.ra119.001797.

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The increasing incidence of antimalarial drug resistance to the first-line artemisinin combination therapies underpins an urgent need for new antimalarial drugs, ideally with a novel mode of action. The recently developed 2-aminomethylphenol, JPC-3210, (MMV 892646) is an erythrocytic schizonticide with potent in vitro antimalarial activity against multidrug-resistant Plasmodium falciparum lines, low cytotoxicity, potent in vivo efficacy against murine malaria, and favorable preclinical pharmacokinetics including a lengthy plasma elimination half-life. To investigate the impact of JPC-3210 on b

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Frasse, Philip, Daniel Goldberg, and Audrey Odom John. "#23: Investigation of Phosphomannomutase as an Antimalarial Drug Target." Journal of the Pediatric Infectious Diseases Society 10, Supplement_2 (2021): S10. http://dx.doi.org/10.1093/jpids/piab031.019.

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Abstract Background Malaria continues to pose an enormous economic and global health threat, killing over 200,000 people annually, primarily children under the age of 5. With the constant barrier of antimalarial resistance and the rise of delayed clearance by artemisinin, it is especially important to identify drug/target pairs that rapidly kill parasites. We study targetable metabolic pathways in the malaria parasite, Plasmodium falciparum, to guide such future drug development against this disease. In recent years, we have discovered that a large family of hydrolases, the Haloacid Dehalogena

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Chandra, Ramesh, Santosh Kumar, and Sunil Kumar Puri. "Buthionine sulfoximine increases the efficacy of arteether antimalarial activity in arteether-resistant Plasmodium vinckei by glutathione depletion." MalariaWorld Journal 6, no. 4 (2015): 1–7. https://doi.org/10.5281/zenodo.10870048.

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<strong>Background.</strong> L-buthionine (S,R)-sulfoximine (BSO) regulates the glutathione (GSH) level, which in turn exhibits remarkable regulation of several important aspects of cellular metabolism. We hypothesised that increasing the cellular levels of glutathione leads to an increased resistance to arteether, whereas decreasing these by using a GSH inhibitor increases the parasite sensitivity to arteether in the rodent malaria parasite <em>Plasmodium vinckei</em>. <strong>Materials and Methods.</strong> We tested in vivo effects of BSO on GSH and hemozoin formation in

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Li, Yitian. "Pyrvinium pamoate can overcome artemisinin’s resistance in anaplastic thyroid cancer." BMC Complementary Medicine and Therapies 21, no. 1 (2021). http://dx.doi.org/10.1186/s12906-021-03332-z.

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Abstract Background Anaplastic thyroid carcinoma is a highly lethal subtype of thyroid cancer without effective therapies. Drug resistance in anaplastic thyroid carcinoma poses a significant problem. Although artemisinin exerts antitumor effects, but its efficacy in anaplastic thyroid carcinoma is unknown. Methods We used RNA sequencing to identify differentially expressed genes. Next, we determined the cause of ART resistance by testing the expression and activity of β-catenin, and enhanced ART activity with a WNT signaling inhibitor. Results Artemisinin suppressed the growth of BHT-101 but n

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Tong, Jie Xin, Sarah E. L. Ang, Esther H. N. Tan, and Kevin S. W. Tan. "Viability Screen of LOPAC1280 Reveals Tyrosine Kinase Inhibitor Tyrphostin A9 as a Novel Partner Drug for Artesunate Combinations To Target the Plasmodium falciparum Ring Stage." Antimicrobial Agents and Chemotherapy 63, no. 4 (2019). http://dx.doi.org/10.1128/aac.02389-18.

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ABSTRACT The emergence of artemisinin-resistant Plasmodium falciparum poses a major threat to current frontline artemisinin combination therapies. Artemisinin resistance is widely associated with mutations in the P. falciparum Kelch13 (PfKelch13) propeller region, leading to delayed parasite clearance and increased survival of early-ring-stage parasites. There is therefore a need to discover novel drugs that are effective against artemisinin-resistant P. falciparum. In view of this, our study aimed to identify compounds from the Library of Pharmacologically Active Compounds1280 (LOPAC1280) tha

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Platon, Lucien, David A. Baker, and Didier Ménard. "Modified Plasmodium falciparum Ring-Stage Survival Assay with ML10 Kinase Inhibitor." Antimicrobial Agents and Chemotherapy, April 26, 2023. http://dx.doi.org/10.1128/aac.00017-23.

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The ring-stage survival assay is the reference assay to measure in vitro Plasmodium falciparum artemisinin partial resistance. The main challenge of the standard protocol is to generate 0-to-3-h postinvasion ring stages (the stage least susceptible to artemisinin) from schizonts obtained by sorbitol treatment and Percoll gradient.

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Simwela, Nelson V., Barbara H. Stokes, Dana Aghabi, Matt Bogyo, David A. Fidock, and Andrew P. Waters. "Plasmodium berghei K13 Mutations Mediate In Vivo Artemisinin Resistance That Is Reversed by Proteasome Inhibition." mBio 11, no. 6 (2020). http://dx.doi.org/10.1128/mbio.02312-20.

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ABSTRACT 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. Herein, we have employed CRISPR/Cas9 genom

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Zahari, Nurul Izzaty Najwa, Noor Fardziatun Ujal, and Nurhidanatasha Abu-Bakar. "Synergistic interaction of two antimalarial drugs, artemisinin and concanamycin A." Life Sciences, Medicine and Biomedicine 7, no. 1 (2023). http://dx.doi.org/10.28916/lsmb.7.1.2023.107.

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Artemisinin is a powerful drug that has been combined with other antimalarial drugs to combat malaria and it has been crucial to recent achievements in reducing malaria cases. However, the emergence of Plasmodium falciparum resistance against artemisinin has become a serious problem in malaria treatment. Our previous studies reported that artemisinin alkalinised the digestive vacuole of P. falciparum similarly to concanamycin A. Concanamycin A is a specific inhibitor of V-type H+-ATPase, a proton pump located on the membrane of the digestive vacuole. A study also showed that a low concentratio

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Mok, Sachel, Barbara H. Stokes, Nina F. Gnädig, et al. "Artemisinin-resistant K13 mutations rewire Plasmodium falciparum’s intra-erythrocytic metabolic program to enhance survival." Nature Communications 12, no. 1 (2021). http://dx.doi.org/10.1038/s41467-020-20805-w.

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AbstractThe emergence and spread of artemisinin resistance, driven by mutations in Plasmodium falciparum K13, has compromised antimalarial efficacy and threatens the global malaria elimination campaign. By applying systems-based quantitative transcriptomics, proteomics, and metabolomics to a panel of isogenic K13 mutant or wild-type P. falciparum lines, we provide evidence that K13 mutations alter multiple aspects of the parasite’s intra-erythrocytic developmental program. These changes impact cell-cycle periodicity, the unfolded protein response, protein degradation, vesicular trafficking, an

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Bouzón-Arnáiz, Inés, Yunuen Avalos-Padilla, Arnau Biosca, et al. "The protein aggregation inhibitor YAT2150 has potent antimalarial activity in Plasmodium falciparum in vitro cultures." BMC Biology 20, no. 1 (2022). http://dx.doi.org/10.1186/s12915-022-01374-4.

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Abstract Background By 2016, signs of emergence of Plasmodium falciparum resistance to artemisinin and partner drugs were detected in the Greater Mekong Subregion. Recently, the independent evolution of artemisinin resistance has also been reported in Africa and South America. This alarming scenario calls for the urgent development of new antimalarials with novel modes of action. We investigated the interference with protein aggregation, which is potentially toxic for the cell and occurs abundantly in all Plasmodium stages, as a hitherto unexplored drug target in the pathogen. Results Attempts

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Nandi, Deeptashree, Pradeep Singh Cheema, Aakriti Singal, Hina Bharti, and Alo Nag. "Artemisinin Mediates Its Tumor-Suppressive Activity in Hepatocellular Carcinoma Through Targeted Inhibition of FoxM1." Frontiers in Oncology 11 (November 24, 2021). http://dx.doi.org/10.3389/fonc.2021.751271.

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The aberrant up-regulation of the oncogenic transcription factor Forkhead box M1 (FoxM1) is associated with tumor development, progression and metastasis in a myriad of carcinomas, thus establishing it as an attractive target for anticancer drug development. FoxM1 overexpression in hepatocellular carcinoma is reflective of tumor aggressiveness and recurrence, poor prognosis and low survival in patients. In our study, we have identified the antimalarial natural product, Artemisinin, to efficiently curb FoxM1 expression and activity in hepatic cancer cells, thereby exhibiting potential anticance

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Chery-Karschney, Laura, Rapatbhorn Patrapuvich, Devaraja Gouda Mudeppa, et al. "Tartrolon E, a secondary metabolite of a marine symbiotic bacterium, is a potent inhibitor of asexual and sexual Plasmodium falciparum." Antimicrobial Agents and Chemotherapy, January 9, 2024. http://dx.doi.org/10.1128/aac.00684-23.

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ABSTRACT Due to the spread of resistance to front-line artemisinin derivatives worldwide, there is a need for new antimalarials. Tartrolon E (TrtE), a secondary metabolite of a symbiotic bacterium of marine bivalve mollusks, is a promising antimalarial because it inhibits the growth of sexual and asexual blood stages of Plasmodium falciparum at sub-nanomolar levels. The potency of TrtE warrants further investigation into its mechanism of action, cytotoxicity, and ease with which parasites may evolve resistance to it.

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Edgar, Rebecca C. S., Tess R. Malcolm, Ghizal Siddiqui, et al. "On-target, dual aminopeptidase inhibition provides cross-species antimalarial activity." mBio, May 8, 2024. http://dx.doi.org/10.1128/mbio.00966-24.

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ABSTRACT To combat the global burden of malaria, development of new drugs to replace or complement current therapies is urgently required. Here, we show that the compound MMV1557817 is a selective, nanomolar inhibitor of both Plasmodium falciparum and Plasmodium vivax aminopeptidases M1 and M17, leading to inhibition of end-stage hemoglobin digestion in asexual parasites. MMV1557817 can kill sexual-stage P. falciparum , is active against murine malaria, and does not show any shift in activity against a panel of parasites resistant to other antimalarials. MMV1557817 -resistant P. falciparum exh

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Sharma, Kiran. "A Comprehensive Review on the Antimicrobial Activity of the Genus Artemisia, Artemisinin, and its Derivatives." Current Topics in Medicinal Chemistry 25 (February 27, 2025). https://doi.org/10.2174/0115680266343676250122062731.

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Abstract: Artemisinin and its semisynthetic derivatives are a group of bioactive chemicals obtained mostly from the extracts of Artemisia species that exert a significant amount of antimalarial activity while remaining relatively safe and tolerable. However, their effectiveness is not limited to malaria; it extends to a variety of human infectious diseases. Mostly the mode of action includes the generation of free radicals by breaking the endoperoxide link in its molecular structure, which facilitates the eradication of microbial species. Artemisinins are found to inhibit bacterial, viral, pro

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Huang, Zhenghui, Ruoxi Li, Tongke Tang, et al. "A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1." Cell Discovery 6, no. 1 (2020). http://dx.doi.org/10.1038/s41421-020-00215-4.

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AbstractAlthough artemisinin combination therapies have succeeded in reducing the global burden of malaria, multidrug resistance of the deadliest malaria parasite, Plasmodium falciparum, is emerging worldwide. Innovative antimalarial drugs that kill all life-cycle stages of malaria parasites are urgently needed. Here, we report the discovery of the compound JX21108 with broad antiplasmodial activity against multiple life-cycle stages of malaria parasites. JX21108 was developed from chemical optimization of quisinostat, a histone deacetylase inhibitor. We identified P. falciparum histone deacet

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Sun, Guangshun, Siqi Zhao, Zhongguo Fan, et al. "CHSY1 promotes CD8+ T cell exhaustion through activation of succinate metabolism pathway leading to colorectal cancer liver metastasis based on CRISPR/Cas9 screening." Journal of Experimental & Clinical Cancer Research 42, no. 1 (2023). http://dx.doi.org/10.1186/s13046-023-02803-0.

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Abstract Background The most common site of metastasis in colorectal cancer (CRC) is the liver and liver metastases occur in more than 50% of patients during diagnosis or treatment. The occurrence of metastasis depends on a series of events known as the invasive-metastasis cascade. Currently, the underlying genes and pathways regulating metastasis initiation in the liver microenvironment are unknown. Methods We performed systematic CRISPR/Cas9 screening using an in vivo mouse model of CRC liver metastasis to identify key regulators of CRC metastasis. We present the full results of this screen,

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Suthram, Niranjan, Siladitya Padhi, Payal Jha, et al. "Elucidation of DNA Repair Function of PfBlm and Potentiation of Artemisinin Action by a Small-Molecule Inhibitor of RecQ Helicase." mSphere 5, no. 6 (2020). http://dx.doi.org/10.1128/msphere.00956-20.

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Malaria continues to be a serious threat to humankind not only because of the morbidity and mortality associated with the disease but also due to the huge economic burden that it imparts. Resistance to all available drugs and the unavailability of an effective vaccine cry for an urgent discovery of newer drug targets.

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Enninful, Kweku S., Samuel K. Kwofie, Mark Tetteh-Tsifoanya, et al. "Targeting the Plasmodium falciparum’s Thymidylate Monophosphate Kinase for the Identification of Novel Antimalarial Natural Compounds." Frontiers in Cellular and Infection Microbiology 12 (May 25, 2022). http://dx.doi.org/10.3389/fcimb.2022.868529.

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Recent reports of resistance to artemisinin-based combination drugs necessitate the need to discover novel antimalarial compounds. The present study was aimed at identifying novel antimalarial compounds from natural product libraries using computational methods. Plasmodium falciparum is highly dependent on the pyrimidine biosynthetic pathway, a de novo pathway responsible for the production of pyrimidines, and the parasite lacks the pyrimidine salvage enzymes. The P. falciparum thymidylate monophosphate kinase (PfTMPK) is an important protein necessary for rapid DNA replication; however, due t

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Hsu, Hao-Chi, Daqiang Li, Wenhu Zhan, et al. "Structures revealing mechanisms of resistance and collateral sensitivity of Plasmodium falciparum to proteasome inhibitors." Nature Communications 14, no. 1 (2023). http://dx.doi.org/10.1038/s41467-023-44077-2.

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AbstractThe proteasome of the malaria parasite Plasmodium falciparum (Pf20S) is an advantageous drug target because its inhibition kills P. falciparum in multiple stages of its life cycle and synergizes with artemisinins. We recently developed a macrocyclic peptide, TDI-8304, that is highly selective for Pf20S over human proteasomes and is potent in vitro and in vivo against P. falciparum. A mutation in the Pf20S β6 subunit, A117D, confers resistance to TDI-8304, yet enhances both enzyme inhibition and anti-parasite activity of a tripeptide vinyl sulfone β2 inhibitor, WLW-vs. Here we present t

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Mao, Linlin, Guodong Deng, Mengfan Li, Shih-Hsin Lu, Wei Jiang, and Xiying Yu. "Antitumour effects of artesunate via cell cycle checkpoint controls in human oesophageal squamous carcinoma cells." European Journal of Medical Research 29, no. 1 (2024). http://dx.doi.org/10.1186/s40001-024-01882-9.

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AbstractArtesunate (ART), an effective antimalarial semisynthetic derivative of artemisinin, exhibits antitumour properties, but the mechanism(s) involved remain elusive. In this study, we investigated the antitumour effects of ART on human oesophageal squamous cell carcinoma (ESCC) cell lines. Treatment of ESCC cell lines with ART resulted in the production of excessive reactive oxygen species (ROS) that induced DNA damage, reduced cell proliferation and inhibited clonogenicity via G1-S cell cycle arrest and/or apoptosis in vitro. The administration of ART to nude mice with ESCC cell xenograf

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de Souza, Guilherme Eduardo, Renata Vieira Bueno, Juliana Oliveira de Souza, et al. "Antiplasmodial profile of selected compounds from Malaria Box: in vitro evaluation, speed of action and drug combination studies." Malaria Journal 18, no. 1 (2019). http://dx.doi.org/10.1186/s12936-019-3069-3.

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Abstract Background Artemisinin-based combination therapy (ACT) is used as the first-line treatment of uncomplicated malaria caused by the Plasmodium falciparum parasite and chloroquine-resistant Plasmodium vivax parasites. Evidence of resistance to ACT has been reported in Cambodia, and without new and effective anti-malarial agents, malaria burden and mortality will rise. Methods The used MolPrint 2D fingerprints and the Tanimoto similarity index were used to perform a structural similarity search within the Malaria Box collection to select diverse molecular scaffolds that are different from

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