Relevant bibliographies by topics / Artemisinin, Syk Inhibitor, Artemisinin resistance

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  1. Journal articles
  2. Dissertations / Theses

Academic literature on the topic 'Artemisinin, Syk Inhibitor, Artemisinin resistance'

Author: Grafiati
Published: 11 March 2023
Last updated: 31 July 2025

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

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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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Dissertations / Theses on the topic "Artemisinin, Syk Inhibitor, Artemisinin resistance"

1

Carlo, Zuddas. "Surface antigenic changes in P.falciparum infected erythrocytes following treatment with Syk inhibitors and Artemisinin." Doctoral thesis, 2020. http://hdl.handle.net/11562/1018318.

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The human Plasmodium falciparum (P.falciparum) parasite, currently infects more than 200 million people annually, causing about 500 000 deaths a year and imposes considerable morbidity on the surviving population. Since 2001, the WHO has recommended Artemisinin based combination therapies (ACTs) as treatment of choice for falciparum malaria. However the WHO has observed foci of suspected artemisinin resistance in South- east Asia. Because strains of P. falciparum are rapidly emerging that are resistant to all known antimalarial drugs, including artemisinin, quinine, chloroquine, piperaquine, a
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