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Amir Kumar Singh et al.
Nature communications, 9(1), 4515-4515 (2018-10-31)
Dysregulated ROR-γt-mediated IL-17 transcription is central to the pathogenesis of several inflammatory disorders, yet the molecular mechanisms that govern the transcription factor activity of ROR-γt in the regulation of IL-17 are not fully defined. Here we show that SUMO-conjugating enzyme
Juan D Unciti-Broceta et al.
PLoS pathogens, 11(6), e1004942-e1004942 (2015-06-26)
African trypanosomiasis is a deadly neglected disease caused by the extracellular parasite Trypanosoma brucei. Current therapies are characterized by high drug toxicity and increasing drug resistance mainly associated with loss-of-function mutations in the transporters involved in drug import. The introduction
Andrej Wagner et al.
International journal of molecular sciences, 15(11), 20134-20157 (2014-11-08)
Photodynamic therapy (PDT) is a palliative treatment option for unresectable hilar biliary tract cancer (BTC) showing a considerable benefit for survival and quality of life with few side effects. Currently, factors determining the cellular response of BTC cells towards PDT
Joost Schalkwijk et al.
Science translational medicine, 11(510) (2019-09-20)
Malaria eradication is critically dependent on new therapeutics that target resistant Plasmodium parasites and block transmission of the disease. Here, we report that pantothenamide bioisosteres were active against blood-stage Plasmodium falciparum parasites and also blocked transmission of sexual stages to
Mohamed Sham Shihabudeen et al.
Molecular and cellular endocrinology, 414, 19-28 (2015-07-19)
Adipose tissue secretes adipokines that regulate insulin sensitivity in adipocytes and other peripheral tissues critical to glucose metabolism. Insulin resistance is associated with severe alterations in adipokines characterized by release of increased pro-inflammatory cytokines and decreased anti-inflammatory cytokines from adipose
Samantha C W Chan et al.
European spine journal : official publication of the European Spine Society, the European Spinal Deformity Society, and the European Section of the Cervical Spine Research Society, 24(11), 2402-2410 (2015-07-29)
Mechanical loading is an important parameter that alters the homeostasis of the intervertebral disc (IVD). Studies have demonstrated the role of compression in altering the cellular metabolism, anabolic and catabolic events of the disc, but little is known how complex
Juan Alberto Castillo-Garit et al.
European journal of medicinal chemistry, 96, 238-244 (2015-04-18)
Two-dimensional bond-based bilinear indices and linear discriminant analysis are used in this report to perform a quantitative structure-activity relationship study to identify new trypanosomicidal compounds. A data set of 440 organic chemicals, 143 with antitrypanosomal activity and 297 having other
Timothy C Boire et al.
Acta biomaterialia, 24, 53-63 (2015-06-15)
Thermo-responsive shape memory polymers (SMPs) can be programmed to fit into small-bore incisions and recover their functional shape upon deployment in the body. This property is of significant interest for developing the next generation of minimally-invasive medical devices. To be
Fadi Abboodi et al.
Virology, 554, 9-16 (2020-12-16)
HPV-inactive head and neck and cervical cancers contain HPV DNA but do not express HPV E6/E7. HPV-positive primary head and neck tumors usually express E6/E7, however they may produce HPV-inactive metastases. These observations led to our hypothesis that HPV-inactive cancers
Maria R Dzamukova et al.
Scientific reports, 5, 10560-10560 (2015-05-16)
Fabrication of stimuli-triggered drug delivery vehicle s is an important milestone in treating cancer. Here we demonstrate the selective anticancer drug delivery into human cells with biocompatible 50-nm diameter halloysite nanotube carriers. Physically-adsorbed dextrin end stoppers secure the intercellular release
Qi Yan Ang et al.
Cell, 181(6), 1263-1275 (2020-05-22)
Very low-carbohydrate, high-fat ketogenic diets (KDs) induce a pronounced shift in metabolic fuel utilization that elevates circulating ketone bodies; however, the consequences of these compounds for host-microbiome interactions remain unknown. Here, we show that KDs alter the human and mouse
Hélène Chassin et al.
Nature communications, 10(1), 2013-2013 (2019-05-03)
Tight control over protein degradation is a fundamental requirement for cells to respond rapidly to various stimuli and adapt to a fluctuating environment. Here we develop a versatile, easy-to-handle library of destabilizing tags (degrons) for the precise regulation of protein
Daniel Vázquez-Sánchez et al.
Food science and technology international = Ciencia y tecnologia de los alimentos internacional, 21(8), 559-570 (2014-10-05)
The present study was aimed to evaluate the potential of essential oils to remove the foodborne pathogen Staphylococcus aureus from food-processing facilities. The effectiveness of 19 essential oils against planktonic cells of S. aureus was firstly assessed by minimal inhibitory
Marco Araújo et al.
International journal of pharmaceutics, 469(1), 140-145 (2014-04-29)
This work proposes melanin as a new nanocarrier for pH-responsive drug release. Melanin is an abundant natural polymer that can be easily extracted from cuttlefish as nanoparticles with a suitable size range for drug delivery. However, despite its high potentiality
Wen-Hao Guo et al.
Nature communications, 11(1), 4268-4268 (2020-08-28)
Current efforts in the proteolysis targeting chimera (PROTAC) field mostly focus on choosing an appropriate E3 ligase for the target protein, improving the binding affinities towards the target protein and the E3 ligase, and optimizing the PROTAC linker. However, due
Chris M Mallory et al.
Bioorganic & medicinal chemistry, 23(23), 7378-7385 (2015-11-07)
Two synthetic aziridinomitosenes (AZMs), Me-AZM and H-AZM, structurally related to mitomycin C (MC) were evaluated for their anticancer activity against six cancer cell lines (HeLa, Jurkat, T47D, HepG2, HL-60, and HuT-78) and tested for their DNA-modifying abilities in Jurkat cells.
Marcelo Fabiano Gomes Boriollo et al.
BMC complementary medicine and therapies, 20(1), 133-133 (2020-05-01)
Sedum praealtum has been used for a long time in traditional medicine as an analgesic and anti-inflammatory agent. Its beneficial effects have been known since ancient times, when Latinos used it to treat sore and swollen eyes. This research evaluated
Pedro Gonzalez-Menendez et al.
Endocrinology, 155(9), 3238-3250 (2014-06-17)
Cancer cells show different metabolic requirements from normal cells. In prostate cancer, particularly, glycolytic metabolism differs in androgen-responsive and nonresponsive cells. In addition, some natural compounds with antiproliferative activities are able to modify glucose entry into cells by either modulating
Ludmila A Kasatkina et al.
Biochemical pharmacology, 174, 113783-113783 (2019-12-28)
Neuroinflammation plays a prominent role in the onset of demyelinating diseases, major depressive disorder and delayed neurodegeneration. An open question remains whether pharmacological suppression of inflammation can effectively reduce the progression of these states. Bioactive lipid mediators such as N-acylethanolamines
Morris E Feldman et al.
PLoS biology, 7(2), e38-e38 (2009-02-13)
The mammalian target of rapamycin (mTOR) regulates cell growth and survival by integrating nutrient and hormonal signals. These signaling functions are distributed between at least two distinct mTOR protein complexes: mTORC1 and mTORC2. mTORC1 is sensitive to the selective inhibitor
Rachel R P Machado et al.
Tuberculosis (Edinburgh, Scotland), 95(6), 829-838 (2015-11-06)
Interferometry was used together with the conventional microplate resazurin assay to evaluate the antimycobacterial properties of essential oil (EO) from fruits of Pterodon emarginatus and also of rifampicin against Mycobacterium bovis. The aim of this work is not only to
Sanjib K Shrestha et al.
Scientific reports, 5, 17070-17070 (2015-11-26)
Azoles are antifungal drugs used to treat fungal infections such as candidiasis in humans. Their extensive use has led to the emergence of drug resistance, complicating antifungal therapy for yeast infections in critically ill patients. Combination therapy has become popular
Bijay Kumar Jha et al.
Parasitology research, 114(3), 1189-1195 (2015-01-08)
Acanthamoeba is an opportunistic protozoan parasite responsible for different diseases in humans, such as granulomatous amoebic encephalitis and amoebic keratitis. Tigecycline, a third-generation tetracycline antibiotic, has potential activity to treat most of the antibiotic resistant bacterial infections. The effects of
Ekaterina Schreiber-Brynzak et al.
Investigational new drugs, 33(4), 835-847 (2015-06-21)
Hypoxic and necrotic regions that accrue within solid tumors in vivo are known to be associated with metastasis formation, radio- and chemotherapy resistance, and drug metabolism. Therefore, integration of these tumor characteristics into in vitro drug screening models is advantageous
Michael Hellwig et al.
Journal of agricultural and food chemistry, 63(30), 6723-6730 (2015-07-18)
Maillard reaction products (MRPs) are taken up in substantial amounts with the daily diet, but the majority are not transported across the intestinal epithelium. The aim of this study was to obtain first insights into the stability of dietary MRPs
A K Krug et al.
Cell death & disease, 5, e1222-e1222 (2014-05-09)
Assessment of the network of toxicity pathways by Omics technologies and bioinformatic data processing paves the road toward a new toxicology for the twenty-first century. Especially, the upstream network of responses, taking place in toxicant-treated cells before a point of
Jiqing Zhang et al.
Molecular therapy : the journal of the American Society of Gene Therapy, 22(7), 1320-1332 (2014-04-04)
This study characterizes the ability of novel oncolytic rhabdoviruses (Maraba MG1) to boost natural killer (NK) cell activity. Our results demonstrate that MG1 activates NK cells via direct infection and maturation of conventional dendritic cells. Using NK depletion and conventional
Trong-Nhat Phan et al.
Molecules (Basel, Switzerland), 25(8) (2020-04-29)
Kinetoplastid parasites, including Leishmania and Trypanosoma spp., are life threatening pathogens with a worldwide distribution. Next-generation therapeutics for treatment are needed as current treatments have limitations, such as toxicity and drug resistance. In this study, we examined the activities of
Paul van den Berk et al.
Cell reports, 33(13), 108533-108533 (2020-12-31)
Altering ubiquitination by disruption of deubiquitinating enzymes (DUBs) affects hematopoietic stem cell (HSC) maintenance. However, comprehensive knowledge of DUB function during hematopoiesis in vivo is lacking. Here, we systematically inactivate DUBs in mouse hematopoietic progenitors using in vivo small hairpin RNA (shRNA)
Abdulsalam A M Alkhaldi et al.
Molecular pharmacology, 87(3), 451-464 (2014-12-21)
We have previously reported that curcumin analogs with a C7 linker bearing a C4-C5 olefinic linker with a single keto group at C3 (enone linker) display midnanomolar activity against the bloodstream form of Trypanosoma brucei. However, no clear indication of
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