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chloroquine resistance

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https://www.readbyqxmd.com/read/28637004/autophagy-is-required-for-crizotinib-induced-apoptosis-in-met-amplified-gastric-cancer-cells
#1
Rebecca D Schroeder, Woonyoung Choi, David S Hong, David J McConkey
MET amplification has been clinically credentialed as a therapeutic target in gastric cancer, but the molecular mechanisms underlying sensitivity and resistance to MET inhibitors are still not well understood. Using whole-genome mRNA expression profiling, we identified autophagy as a top molecular pathway that was activated by the MET inhibitor crizotinib in drug-sensitive human gastric cancer cells, and functional studies confirmed that crizotinib increased autophagy levels in the drug-sensitive cells in a concentration-dependent manner...
June 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28635296/benzoxaborole-antimalarial-agents-part-5-lead-optimization-of-novel-amide-pyrazinyloxy-benzoxaboroles-and-identification-of-a-preclinical-candidate
#2
Yong-Kang Zhang, Jacob J Plattner, Eric E Easom, Robert Toms Jacobs, Denghui Guo, Yvonne R Freund, Pamela Berry, Vic Ciaravino, John C L Erve, Philip J Rosenthal, Brice Campo, Francisco-Javier Gamo, Laura M Sanz, Jianxin Cao
Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a molecule with satisfactory antimalarial activity, physicochemical properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effort discovered 46, which met our target candidate profile. Compound 46 had excellent activity against cultured Plasmodium falciparum, and in vivo against P. falciparum and P. berghei in infected mice. It exhibited good PK properties in mouse, rat and dog. It was highly active against other eleven P...
June 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28627629/reducing-autophagy-and-inducing-g1-phase-arrest-by-aloperine-enhances-radio-sensitivity-in-lung-cancer-cells
#3
Zhijie Xu, Yuanliang Yan, Shuangshuang Zeng, Long Qian, Shuang Dai, Lingfang Xiao, Lin Wang, Xue Yang, Yi Xiao, Zhicheng Gong
Aloperine (ALO), an isolated alkaloid from the leaves of Sophora alopecuroides (S. alopecuroides), has been suggested to exhibit anti-inflammatory and antitumor properties, and has been traditionally used to treat various diseases, including cancers. However, little is known about the effects of ALO on the radio-sensitivity of lung cancer cells. In the present study, we confirmed that agent ALO inhibits cell growth, promotes cell aopotosis and induces G1 phase arrest and consequently enhanced the radio-sensitivity in radio-resistant lung cancer cells A549/IR...
June 19, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28622697/vitamin-c-and-doxycycline-a-synthetic-lethal-combination-therapy-targeting-metabolic-flexibility-in-cancer-stem-cells-cscs
#4
Ernestina Marianna De Francesco, Gloria Bonuccelli, Marcello Maggiolini, Federica Sotgia, Michael P Lisanti
Here, we developed a new synthetic lethal strategy for further optimizing the eradication of cancer stem cells (CSCs). Briefly, we show that chronic treatment with the FDA-approved antibiotic Doxycycline effectively reduces cellular respiration, by targeting mitochondrial protein translation. The expression of four mitochondrial DNA encoded proteins (MT-ND3, MT-CO2, MT-ATP6 and MT-ATP8) is suppressed, by up to 35-fold. This high selection pressure metabolically synchronizes the surviving cancer cell sub-population towards a predominantly glycolytic phenotype, resulting in metabolic inflexibility...
June 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28619113/mechanisms-underlying-extensive-ser129-phosphorylation-in-%C3%AE-synuclein-aggregates
#5
Shigeki Arawaka, Hiroyasu Sato, Asuka Sasaki, Shingo Koyama, Takeo Kato
Parkinson's disease (PD) is characterized neuropathologically by intracellular aggregates of fibrillar α-synuclein, termed Lewy bodies (LBs). Approximately 90% of α-synuclein deposited as LBs is phosphorylated at Ser129 in brains with PD. In contrast, only 4% of total α-synuclein is phosphorylated at Ser129 in brains with normal individuals. It is unclear why extensive phosphorylation occurs in the pathological process of PD. To address this issue, we investigated a mechanism and role of Ser129-phosphorylation in regulating accumulation of α-synuclein...
June 15, 2017: Acta Neuropathologica Communications
https://www.readbyqxmd.com/read/28615849/in-vivo-antimalarial-activity-of-aqueous-leaf-and-bark-extracts-of-trema-orientalis-against-plasmodium-berghei-in-mice
#6
Oluwatoyosi Eniola Oyebola, Olajumoke Abimbola Morenikeji, Isaiah Oluwafemi Ademola
The control of malaria relies on the use of chemical antimalarial, but the development of resistance necessitates research into alternatives. Trema orientalis (L.) Blume is used in Nigerian folklore medicine for the treatment of malaria. This study investigates the in vivo antiplasmodial activity of aqueous leaf and bark extracts of T. orientalis in rodent model. Swiss Albino mice weighing 23-27 g were intraperitoneally infected with Plasmodium berghei. The lethal dose in mice was estimated to be greater than 5000 mg/kg based on toxicity signs and death...
June 2017: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
https://www.readbyqxmd.com/read/28615016/ex-vivo-susceptibility-and-genotyping-of-plasmodium-falciparum-isolates-from-pikine-senegal
#7
Aminata Mbaye, Amy Gaye, Baba Dieye, Yaye D Ndiaye, Amy K Bei, Muna Affara, Awa B Deme, Mamadou S Yade, Khadim Diongue, Ibrahima M Ndiaye, Tolla Ndiaye, Mouhamed Sy, Ngayo Sy, Ousmane Koita, Donald J Krogstad, Sarah Volkman, Davis Nwakanma, Daouda Ndiaye
BACKGROUND: The monitoring of Plasmodium falciparum sensitivity to anti-malarial drugs is a necessity for effective case management of malaria. This species is characterized by a strong resistance to anti-malarial drugs. In Senegal, the first cases of chloroquine resistance were reported in the Dakar region in 1988 with nearly 7% population prevalence, reaching 47% by 1990. It is in this context that sulfadoxine-pyrimethamine temporarily replaced chloroquine as first line treatment in 2003, pending the introduction of artemisinin-based combination therapy in 2006...
June 14, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28605993/in-vitro-sensitivity-to-antimalarial-drugs-and-polymorphisms-in-pfg377-gene-in-plasmodium-falciparum-field-isolates-from-mewat-india
#8
Vineeta Singh, Amit Kumar, Purva Gupta
The malaria infection is the interplay of several complex factors, among which drug resistance and gametocyte biology are the crucial ones. Measurements of the drug sensitivity assays and prevalence of gametocyte genes play a major role in malaria eradication programmes. The purpose of this study was to assess the current drug sensitivity profile in the field isolates and type the Pfg377 gene. In vitro drug sensitivity assay was used to assess the susceptibility of Plasmodium falciparum field isolates collected from Mewat (Haryana), located in Northern region of India to four anti-malarial drugs...
June 12, 2017: Pathogens and Global Health
https://www.readbyqxmd.com/read/28599504/combination-of-wogonin-and-sorafenib-effectively-kills-human-hepatocellular-carcinoma-cells-through-apoptosis-potentiation-and-autophagy-inhibition
#9
Li-Wen Rong, Rui-Xue Wang, Xue-Lian Zheng, Xu-Qin Feng, Lei Zhang, Lin Zhang, Yong Lin, Zhi-Ping Li, Xia Wang
The small molecule multi-kinase inhibitor sorafenib has become the standard systemic treatment for patients with advanced hepatocellular carcinoma (HCC) and renal cell carcinoma. Similar to other kinase inhibitors, drug resistance hinders its clinical use; thus, combination therapy to improve sorafenib sensitivity is a promising approach. The present study shows for the first time that the combination of sorafenib and wogonin exerts a significant potentiation of cytotoxicity in a number of human HCC cell lines in a dose-dependent manner...
June 2017: Oncology Letters
https://www.readbyqxmd.com/read/28599416/autophagy-inhibition-impairs-the-epithelial-mesenchymal-transition-and-enhances-cisplatin-sensitivity-in-nasopharyngeal-carcinoma
#10
Zhongwu Su, Guo Li, Chao Liu, Shuling Ren, Tengbo Deng, Shuiting Zhang, Yongquan Tian, Yong Liu, Yuanzheng Qiu
Drug resistance restricts the efficacy of cisplatin in the treatment of nasopharyngeal carcinoma (NPC). Increasing evidence indicates that autophagy and the epithelial-mesenchymal transition (EMT) participate in cancer progression and drug sensitivity. The aim of the present study was to investigate the function of autophagy and EMT in cisplatin treatment, and to reveal the underlying impact of autophagy on the EMT process in NPC. Transmission electron microscopy assays and western blot analyses confirmed that cisplatin activates autophagy in NPC cells...
June 2017: Oncology Letters
https://www.readbyqxmd.com/read/28597984/dual-inhibition-of-bdnf-trkb-and-autophagy-a-promising-therapeutic-approach-for-colorectal-cancer
#11
Clément Mazouffre, Sophie Geyl, Aurélie Perraud, Sabrina Blondy, Marie-Odile Jauberteau, Muriel Mathonnet, Mireille Verdier
Colorectal cancer (CRC) is the most common digestive cancer in the Western world. Despite effective therapies, resistance and/or recurrence frequently occur. The present study investigated the impact of two survival pathways-neurotrophic factors (TrkB/BDNF) and autophagy-on cell fate and tumour evolution. In vitro studies were performed on two CRC cell lines, SW480 (primary tumour) and SW620 (lymph node invasion), which were also used for subcutaneous xenografts on a nude mouse model. In addition, the presence of neurotrophic factors (NTs) and autophagy markers were assessed in tissue samples representative of different stages...
June 9, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28596841/targeting-endosomal-acidification-by-chloroquine-analogs-as-a-promising-strategy-for-the-treatment-of-emerging-viral-diseases
#12
REVIEW
Md Abdul Alim Al-Bari
Emerging viruses such as HIV, dengue, influenza A, SARS coronavirus, Ebola, and other viruses pose a significant threat to human health. Majority of these viruses are responsible for the outbreaks of pathogenic lethal infections. To date, there are no effective therapeutic strategies available for the prophylaxis and treatment of these infections. Chloroquine analogs have been used for decades as the primary and most successful drugs against malaria. Concomitant with the emergence of chloroquine-resistant Plasmodium strains and a subsequent decrease in the use as antimalarial drugs, other applications of the analogs have been investigated...
February 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28595540/apicoplast-import-protein-tic20-a-promising-therapeutic-molecular-target-for-plasmodium-falciparum-an-insilico-approach-for-therapeutic-intervention
#13
Pavan C P K Srimath-Tirumala-Peddinti, Sandeep Solmon Kusuma, Deepthi Nammi, Nageswara Rao Reddy Neelapu
Malaria is a lethal disease causing mortality to over millions each year. Drug resistance in the malarial parasite encouraged to discover effective antimalarial drug targets and drugs. An objective of this current study is to identify drug targets for malarial parasite. Genes unique, non-homologous to humans and essential for parasite are identified using BLASTn by comparing genomes between parasite and host. Further open BLASTp was used to filter the targets specific to Plasmodium species and later were subjected to gene property analysis to identify 65 potential targets...
June 5, 2017: Infectious Disorders Drug Targets
https://www.readbyqxmd.com/read/28594879/molecular-surveillance-of-plasmodium-falciparum-resistance-to-artemisinin-based-combination-therapies-in-the-democratic-republic-of-congo
#14
Dieudonné Makaba Mvumbi, Thierry Lengu Bobanga, Jean-Marie Ntumba Kayembe, Georges Lelo Mvumbi, Hippolyte Nani-Tuma Situakibanza, Françoise Benoit-Vical, Pierrette Melin, Patrick De Mol, Marie-Pierre Hayette
Malaria is a major public health problem in the Democratic Republic of Congo. Despite progress achieved over the past decade in the fight against malaria, further efforts have to be done such as in the surveillance and the containment of Plasmodium falciparum resistant strains. We investigated resistance to artemisinin-based combination therapies currently in use in Democratic Republic of Congo by surveying molecular polymorphisms in three genes: pfcrt, pfmdr1 and pfk13 to explore possible emergence of amodiaquine, lumefantrine or artemisinin resistance in Democratic Republic of Congo...
2017: PloS One
https://www.readbyqxmd.com/read/28592636/interleukin-6-protects-pancreatic-%C3%AE-cells-from-apoptosis-by-stimulation-of-autophagy
#15
Amelia K Linnemann, Joseph Blumer, Michelle R Marasco, Therese J Battiola, Heidi M Umhoefer, Jee Young Han, Dudley W Lamming, Dawn Belt Davis
IL-6 is a pleiotropic cytokine with complex roles in inflammation and metabolic disease. The role of IL-6 as a pro- or anti-inflammatory cytokine is still unclear. Within the pancreatic islet, IL-6 stimulates secretion of the prosurvival incretin hormone glucagon-like peptide 1 (GLP-1) by α cells and acts directly on β cells to stimulate insulin secretion in vitro Uncovering physiologic mechanisms promoting β-cell survival under conditions of inflammation and stress can identify important pathways for diabetes prevention and treatment...
June 7, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28589330/triple-combination-therapy-and-drug-cycling-tangential-strategies-for-countering-artemisinin-resistance
#16
REVIEW
Bhattacharjee Dipanjan, G Shivaprakash, O Balaji
PURPOSE OF REVIEW: This review attempts to understand the reasons for the successes and failures of the two novel strategies that have slowly begun to emerge as potential counters for anti-malarial drug resistance-"Triple Combination Therapy" and "Drug Cycling." RECENT FINDINGS: Recent reports have suggested that increasing the heterogeneity within the parasite's environment, both at an individual and the population level, may help raise the probabilistic barrier of development of resistance in the parasite...
July 2017: Current Infectious Disease Reports
https://www.readbyqxmd.com/read/28580606/combating-multi-drug-resistant-plasmodium-falciparum-malaria
#17
REVIEW
Aung Myint Thu, Aung Pyae Phyo, Jordi Landier, Daniel M Parker, François H Nosten
Over the past 50 years, P. falciparum has developed resistance against all antimalarial drugs used against it: chloroquine, sulphadoxine-pyrimethamine, quinine, piperaquine and mefloquine. More recently, resistance to the artemisinin derivatives and the resulting failure of artemisinin based combination therapy (ACT) are threatening all major gains made in malaria control. Each time resistance has developed over a progression, with delayed clearance of parasites emerging in a few regions, increasing in prevalence and geographic range, and then ultimately resulting in the complete failure of that antimalarial...
June 5, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28577368/inhibitors-of-ubiquitin-e3-ligase-as-potential-new-antimalarial-drug-leads
#18
Jagrati Jain, Surendra K Jain, Larry A Walker, Babu L Tekwani
BACKGROUND: Protein ubiquitylation is an important post-translational regulation, which has been shown to be necessary for life cycle progression and survival of Plasmodium falciparum. Ubiquitin is a highly conserved 76 amino acid polypeptide, which attaches covalently to target proteins through combined action of three classes of enzymes namely, the ubiquitin-activating enzyme (E1), ubiquitin-conjugating enzyme (E2) and ubiquitin-protein ligase (E3). Ubiquitin E1 and E2 are highly conserved within eukaryotes...
June 2, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28566625/effective-loading-of-platinum-chloroquine-into-pegylated-neutral-and-cationic-liposomes-as-a-drug-delivery-system-for-resistant-malaria-parasites
#19
Shaimaa Ibrahim, Tatsuaki Tagami, Tetsuya Ozeki
The trans platinum-chloroquine diphosphate dichloride (PtCQ) is a new type of antimalarial drug used to fight parasites resistant to traditional drugs. PtCQ is synthesized by mixing platinum and chloroquine diphosphate (CQ). This study examines two efficient methods for forming a nanodrug, PtCQ-loaded liposomes, for use as a potential antimalarial drug-delivery system: the thin drug-lipid film method to incorporate the drug into a liposomal membrane, and a remote-loading method to load the drug into the interior of a cationic liposome...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28553083/cisplatin-induces-protective-autophagy-through-activation-of-becn1-in-human-bladder-cancer-cells
#20
Ji-Fan Lin, Yi-Chia Lin, Te-Fu Tsai, Hung-En Chen, Kuang-Yu Chou, Thomas I-Sheng Hwang
PURPOSE: Cisplatin-based chemotherapy is the first line treatment for several cancers including bladder cancer (BC). Autophagy induction has been implied to contribute to cisplatin resistance in ovarian cancer; and a high basal level of autophagy has been demonstrated in human bladder tumors. Therefore, it is reasonable to speculate that autophagy may account for the failure of cisplatin single treatment in BC. This study investigated whether cisplatin induces autophagy and the mechanism involved using human BC cell lines...
2017: Drug Design, Development and Therapy
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