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Antiparasitic drugs

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https://www.readbyqxmd.com/read/28811376/in-vivo-loss-of-function-screens-identify-kpnb1-as-a-new-druggable-oncogene-in-epithelial-ovarian-cancer
#1
Michiko Kodama, Takahiro Kodama, Justin Y Newberg, Hiroyuki Katayama, Makoto Kobayashi, Samir M Hanash, Kosuke Yoshihara, Zhubo Wei, Jean C Tien, Roberto Rangel, Kae Hashimoto, Seiji Mabuchi, Kenjiro Sawada, Tadashi Kimura, Neal G Copeland, Nancy A Jenkins
Epithelial ovarian cancer (EOC) is a deadly cancer, and its prognosis has not been changed significantly during several decades. To seek new therapeutic targets for EOC, we performed an in vivo dropout screen in human tumor xenografts using a pooled shRNA library targeting thousands of druggable genes. Then, in follow-up studies, we performed a second screen using a genome-wide CRISPR/Cas9 library. These screens identified 10 high-confidence drug targets that included well-known oncogenes such as ERBB2 and RAF1, and novel oncogenes, notably KPNB1, which we investigated further...
August 15, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28811324/the-transcriptional-program-functional-heterogeneity-and-clinical-targeting-of-mast-cells
#2
REVIEW
Gökhan Cildir, Harshita Pant, Angel F Lopez, Vinay Tergaonkar
Mast cells are unique tissue-resident immune cells that express an array of receptors that can be activated by several extracellular cues, including antigen-immunoglobulin E (IgE) complexes, bacteria, viruses, cytokines, hormones, peptides, and drugs. Mast cells constitute a small population in tissues, but their extraordinary ability to respond rapidly by releasing granule-stored and newly made mediators underpins their importance in health and disease. In this review, we document the biology of mast cells and introduce new concepts and opinions regarding their role in human diseases beyond IgE-mediated allergic responses and antiparasitic functions...
August 15, 2017: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/28801098/synthesis-and-in-vitro-evaluation-of-ca-2-channel-blockers-1-4-dihydropyridines-analogues-against-trypanosoma-cruzi-and-leishmania-amazonensis-sar-analysis
#3
Luiz A E Pollo, Milene H de Moraes, Júlia Cisilotto, Tânia B Creczynski-Pasa, Maique W Biavatti, Mario Steindel, Louis P Sandjo
Drugs containing the1,4-dihydropyridine (DHP) core have recently attracted attention concerning their antiparasitic effect against various species of Leishmania and Trypanosoma. This approach named drugs repositioning led to interesting results, which have prompted us to prepare 21 DHP's analogues. The 1,4-DHP scaffold was decorated with different function groups at tree points including the nitrogen atom (NH and N-phenyl), the aryl group attached to C-4 (various substituted aryl residues) and the carbon atoms 2 and 6 (bearing Ph or Me groups)...
August 8, 2017: Parasitology International
https://www.readbyqxmd.com/read/28798383/novel-giardicidal-compounds-bearing-proton-pump-inhibitor-scaffold-proceeding-through-triosephosphate-isomerase-inactivation
#4
B Hernández-Ochoa, G Navarrete-Vázquez, C Nava-Zuazo, A Castillo-Villanueva, S T Méndez, A Torres-Arroyo, S Gómez-Manzo, J Marcial-Quino, M Ponce-Macotela, Y Rufino-González, M Martínez-Gordillo, G Palencia-Hernández, N Esturau-Escofet, E Calderon-Jaimes, J Oria-Hernández, H Reyes-Vivas
Giardiasis is a worldwide parasitic disease that affects mainly children and immunosuppressed people. Side effects and the emergence of resistance over current used drugs make imperative looking for new antiparasitics through discovering of new biological targets and designing of novel drugs. Recently, it has determined that gastric proton-pump inhibitors (PPI) have anti-giardiasic activity. The glycolytic enzyme, triosephosphate isomerase (GlTIM), is one of its potential targets. Therefore, we employed the scaffold of PPI to design new compounds aimed to increase their antigiardial capacity by inactivating GlTIM...
August 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28795594/the-battle-of-worldviews-a-case-study-of-liver-fluke-infection-in-khon-kaen-thailand
#5
Sara Samiphak, S Leonard Syme
Control efforts to reduce infection from the parasitic flatworm Opisthorchis viverrini have progressed through understanding the epidemiology of Opisthorchis viverrini, antiparasitic drug developments, technological innovations, health education promoting cooking of fish, and improved hygienic defecation. Yet the problem persists. The case study method was used to examine the fundamental cause of the liver fluke infection problem. Evidence shows that the liver fluke-infected population does not care about living a long life...
January 1, 2017: Journal of Evidence-based Complementary & Alternative Medicine
https://www.readbyqxmd.com/read/28793307/larrea-tridentata-a-novel-source-for-anti-parasitic-agents-active-against-entamoeba-histolytica-giardia-lamblia-and-naegleria-fowleri
#6
Bharat Bashyal, Linfeng Li, Trpta Bains, Anjan Debnath, Daniel V LaBarbera
Protozoan parasites infect and kill millions of people worldwide every year, particularly in developing countries where access to clean fresh water is limited. Among the most common are intestinal parasites, including Giardia lamblia and Entamoeba histolytica. These parasites wreak havoc on the epithelium lining the small intestines (G. lamblia) and colon (E. histolytica) causing giardiasis and amebiasis, respectively. In addition, there are less common but far more deadly pathogens such as Naegleria fowleri that thrive in warm waters and infect the central nervous systems of their victims via the nasal passages...
August 9, 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28789893/lead-selection-of-antiparasitic-compounds-from-a-focused-library-of-benzenesulfonyl-derivatives-of-heterocycles
#7
Romina J Pagliero, Marcel Kaiser, Reto Brun, Marcelo J Nieto, María R Mazzieri
A library of 89 synthetic benzenesulfonyl derivatives of heterocycles with drug-like properties was assayed for in vitro antiparasitic activity and the results were added to our previously reported derivatives for a comprehensive SAR evaluation. Four compounds showed an IC50 between 0.25 and 3μM against Leishmania donovani and low cytotoxicity. Compound G{16} (1-(2,3,5,6-tetramethylphenylsulfonyl)-2-methylindoline), was particularly interesting with an IC50 similar to the reference drug miltefosine. Seven compounds showed an IC50 below 6µM against Trypanosoma cruzi, and three of them (E{3}, E{9} and G{3}) were identified as lead scaffolds for further optimization based on their activity-toxicity profile...
July 31, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28782352/cornus-mas-a-review-on-traditional-uses-and-pharmacological-properties
#8
Fatemeh Hosseinpour-Jaghdani, Tahoora Shomali, Sajedeh Gholipour-Shahraki, Mohammad Rahimi-Madiseh, Mahmoud Rafieian-Kopaei
Medicinal plants that are used today have been known by people of ancient cultures around the world and have largely been considered due to their medicinal properties. Cornus mas L. (Cornelian cherry) is one of these medicinal plants with high level of antioxidant activity. Cornelian cherry is an attractive ornamental plant with delicious fruit having nutritional and therapeutic values. The main purpose of this paper is to present and summarize the pharmacological and therapeutic effects from researches done on Cornelian cherry in studies from 2000 to 2016...
March 31, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28760415/surface-glycans-a-therapeutic-opportunity-for-kinetoplastid-diseases
#9
REVIEW
Víctor M Castillo-Acosta, Jan Balzarini, Dolores González-Pacanowska
Trypanosomal diseases are in need of innovative therapies that exploit novel mechanisms of action. The cell surface of trypanosomatid parasites is characterized by a dense coat of glycoconjugates with important functions in host cell recognition, immune evasion, infectivity, and cell function. The nature of parasite surface glycans is highly dynamic and changes during differentiation and in response to different stimuli through the action of glycosyltransferases and glycosidases. Here we propose a new approach to antiparasitic drug discovery that involves the use of carbohydrate-binding agents that bind specifically to cell-surface glycans, giving rise to cytotoxic events and parasite death...
July 28, 2017: Trends in Parasitology
https://www.readbyqxmd.com/read/28755871/cyclohexene-fused-1-3-oxazines-with-selective-antibacterial-and-antiparasitic-action-and-low-cytotoxic-effects
#10
Maria R M de Brito, Walter J Peláez, Martín S Faillace, Gardenia C G Militão, Jackson R G S Almeida, Gustavo A Argüello, Zsolt Szakonyi, Ferenc Fülöp, Maria C Salvadori, Fernanda S Teixeira, Rivelilson M Freitas, Pedro L S Pinto, Ana C Mengarda, Marcos P N Silva, Ademar A Da Silva Filho, Josué de Moraes
Oxazine derivatives, a class of heterocyclic compounds, exhibit a variety of biological properties, such as anticonvulsant and antitumor activities. In this study, we evaluated the effect of two cyclohexene-fused 1,3-oxazines (cis‑1-benzyl-N-phenyl-1,4,4a,5,8,8a-hexahydro-3,1-benzoxazin-2-imine (1) and trans‑N-phenyl-1,4,4a,5,8,8a-hexahydro-3,1-benzoxazin-2-imine (2)) in cultures of Bacillus cereus, Enterococcus faecalis, Escherichia coli, Klebsiella pneumoniae, Salmonella enterica, Serratia marcescens, Shigella flexneri and Staphylococcus aureus by the Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC)...
July 26, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28751930/the-correlation-between-chemical-structures-and-antioxidant-prooxidant-and-antitrypanosomatid-properties-of-flavonoids
#11
João Luiz Baldim, Bianca Gonçalves Vasconcelos de Alcântara, Olívia da Silva Domingos, Marisi Gomes Soares, Ivo Santana Caldas, Rômulo Dias Novaes, Tiago Branquinho Oliveira, João Henrique Ghilardi Lago, Daniela Aparecida Chagas-Paula
Flavonoids have demonstrated in vivo and in vitro leishmanicidal, trypanocidal, antioxidant, and prooxidant properties. The chemotherapy of trypanosomiasis and leishmaniasis lacks efficacy, presents high toxicity, and is related to the development of drug resistance. Thus, a series of 40 flavonoids were investigated with the purpose of correlating these properties via structure and activity analyses based on integrated networks and QSAR models. The classical groups for the antioxidant activity of flavonoids were combined in order to explain the influence of antioxidant and prooxidant activities on the antiparasitic properties...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28750211/moxidectin-residues-in-tissues-of-lambs-submitted-to-three-endoparasite-control-programs
#12
Maria Angela Machado Fernandes, Susana Gilaverte, Michele Dell Bianchi, Claudio José Araujo da Silva, Marcelo Beltrão Molento, Felix Guillermo Reyes Reyes, Alda Lucia Gomes Monteiro
The indiscriminate and continuous use of anthelmintic drugs has promoted the selection of resistant parasites population, the presence of drug residues in food products, and heavy environmental contamination. The aim of the present study was to determine the presence of antiparasitic drug residues in 42-days old lamb serum and tissues, submitted to three endoparasite control programs: preventive treatment (PT) using moxidectin (MOX) at every 28days; selective treatment (FEC) using MOX when fecal egg count was greater than or equal to 700; and selective treatment (FMC), using MOX when FAMACHA/FMC score was 3 and above...
July 13, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28740612/3-hydroxykynurenine-a-tryptophan-metabolite-generated-during-the-infection-is-active-against-trypanosoma-cruzi
#13
Carolina P Knubel, Constanza Insfran, Fernando F Martinez, Cintia Diaz Lujan, Ricardo E Fretes, Martin G Theumer, Laura Cervi, Claudia C Motran
The antiparasitic activity of 3-hydroxykynurenine (3-HK), one of the major tryptophan catabolites of the kynurenine pathway, against both Trypanosoma cruzi evolutive forms that are important for human infection, trypomastigotes (Tps) and amastigotes (Am), possible targets in the parasite and the drug toxicity to mammalian cells have been investigated. 3-HK showed a potent activity against Am with IC50 values in the micromolar concentration range, while the IC50 values to cause Tps death was ∼6000-times higher, indicating that the replicative form present in the vertebrate hosts is much more susceptible to 3-HK than bloodstream Tps...
July 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28715108/ivermectin-activates-girk-channels-in-a-pip2-dependent-g%C3%AE-%C3%AE-independent-manner-and-an-amino-acid-residue-at-the-slide-helix-governs-the-activation
#14
I-Shan Chen, Michihiro Tateyama, Yuko Fukata, Motonari Uesugi, Yoshihiro Kubo
KEY POINTS: Ivermectin (IVM) is a widely used antiparasitic drug in humans and pets which activates glutamate-gated Cl(-) channel in parasites. It is known that IVM binds to the transmembrane domains (TMs) of several ligand-gated channels, such as Cys-loop receptors and P2X receptors. We found that the G-protein-gated inwardly rectifying K(+) (GIRK) channel, especially GIRK2, is activated by IVM directly in a Gβγ -independent manner, but the activation is dependent on phosphatidylinositol-4,5-biphosphate (PIP2 )...
July 17, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28679535/small-molecule-based-inhibition-of-mek1-2-proteins-dampens-inflammatory-responses-to-malaria-reduces-parasite-load-and-mitigates-pathogenic-outcomes
#15
Xianzhu Wu, Kiran K Dayanand, Ramesh P Thylur, Christopher C Norbury, D Channe Gowda
Malaria infections cause several systemic and severe single- or multi-organ pathologies, killing hundreds of thousands of people annually. Considering the existing widespread resistance of malaria parasites to anti-parasitic drugs and their high propensity to develop drug resistance, alternative strategies are required to manage malaria infections. Because malaria is a host immune response-driven disease, one approach is based on gaining a detailed understanding of the molecular and cellular processes that modulate malaria-induced innate and adaptive immune responses...
August 18, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28671059/role-of-polyamines-in-parasite-cell-architecture-and-function
#16
Marcos A Vannier-Santos, Ana M Suarez-Fontes
In the absence of accessible, effective vaccines, the fight against parasitic disease relies mostly on chemotherapy. Nevertheless, the considerable side effects, high costs and growing number of refractory cases comprise substantial drawbacks. Thus, the search for new antiparasitic compounds remains a high priority. The polyamine biosynthesis, conversion and transport pathways offer different targets for selective chemotherapy. Polyamine analogues and other antagonists may provide tools in the search for new lead compounds...
July 3, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28666754/antiparasitic-activity-of-nerolidol-in-a-mouse-model-of-schistosomiasis
#17
Marcos P Silva, Rosimeire N de Oliveira, Ana C Mengarda, Daniel B Roquini, Silmara M Alegretti, Maria C Salvadori, Fernanda S Teixeira, Damião P de Sousa, Pedro L S Pinto, Josué de Moraes
Schistosomiasis is a major public health problem worldwide, especially in poor communities. Since praziquantel is currently the only drug available to treat schistosomiasis, there is an urgent need to identify new antischistosomal drugs. Nerolidol is a sesquiterpene present as an essential oil in several plants, and it has been approved by the US Food and Drug Administration. In this study, we evaluated the in vivo antischistosomal activity of nerolidol in a mouse model of schistosomiasis infected with either adult or juvenile stages of Schistosoma mansoni...
June 27, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28641558/bis-2-aminoimidazolines-and-bisguanidines-synthetic-approaches-antiparasitic-activity-and-dna-binding-properties
#18
Christophe Dardonville, J Jonathan Nué Martínez
BACKGROUND: Parasitic diseases caused by protozoan parasites of the genus Trypanosoma and Plasmodium cause some of the deadliest and disabling human infections in tropical and subtropical areas. Diphenyl-based bis(2-phenylimino)imidazolidines and bisguanidines are extremely potent antiparasitic agents against Trypanosoma brucei (etiological agent of African trypanosomiasis) and Plasmodium falciparum (etiological agent of severe malaria). Many of these compounds are also curative in mouse models of stage 1 African trypanosomiasis representing promising leads for the development of antitrypanosomal drugs...
June 22, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28624508/epidemiological-profile-of-cutaneous-larva-migrans-in-travelers-returning-to-france-between-2003-and-2015
#19
Doudou Sow, Ferelaha Soro, Emilie Javelle, Fabrice Simon, Philippe Parola, Philippe Gautret
BACKGROUND: Cutaneous larva migrans (CLM) is caused by the penetration and migration of canine or feline hookworm larvae into the skin, and frequently affects travelers from high-income countries returning from tropical and sub-tropical areas. Unfortunately, this pathology is neglected due to poor understanding among both physicians and travelers. This study describes the profile of cases reported in Marseille, France. PATIENTS AND METHODS: A retrospective study was performed in two specialized hospitals between 2003 and 2015...
June 15, 2017: Travel Medicine and Infectious Disease
https://www.readbyqxmd.com/read/28612332/cocaine-levamisole-induced-vasculitis-vasculopathy-syndrome
#20
REVIEW
Javier Marquez, Lina Aguirre, Carolina Muñoz, Andres Echeverri, Mauricio Restrepo, Luis F Pinto
PURPOSE OF REVIEW: To understand the clinical spectrum of cocaine-levamisole-induced vasculitis. Worldwide recreational drug consumption is high among the adult population from various social strata. The use of cocaine with levamisole, a frequently added antiparasitic diluent, favors the manifestations of vasculitic lesions, especially in the skin. RECENT FINDINGS: New insights into immunological mechanisms involved in the pathogenesis of the disease. There are still many unknown aspects in the pathogenesis of this disease, such as the immune system interaction with p-ANCAs and the release of inflammatory NETs (neutrophil extracellular traps), which are the origin of auto-antigens and tissue damage, manifesting as vasculitic purpura on the skin...
June 2017: Current Rheumatology Reports
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