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Showing 1-30 of 70 results for "I100" within Papers
Jiaqi Huang et al.
Journal of Cancer, 11(12), 3685-3692 (2020-04-15)
Accumulated extracellular adenosine suppresses antitumor immunity via adenosine 2A receptor (A2AR). Blockade of A2AR with DZD2269 can inhibit phosphorylation of cAMP response element-binding protein mediated by adenosine analogue in vitro and in vivo. Irradiation can cause the release of adenosine
William F Waas et al.
Biochemistry, 42(10), 2960-2970 (2003-03-12)
Extracellular regulated protein kinase 2 (ERK2) is a eukaryotic protein kinase whose activity is regulated by phorbol esters, serum, and growth factors, and displays enhanced activity in several human tumors. Despite its important biological function, its mechanism of catalysis and
Ken-ichi Otsuguro et al.
Neuropharmacology, 97, 160-170 (2015-06-13)
Adenosine kinase (AK) inhibitor is a potential candidate for controlling pain, but some AK inhibitors have problems of adverse effects such as motor impairment. ABT-702, a non-nucleoside AK inhibitor, shows analgesic effect in animal models of pain. Here, we investigated
A Peairs et al.
Clinical and experimental immunology, 156(3), 542-551 (2009-05-15)
Recent reports show that 5-amino-4-imidazole carboxamide riboside (AICAR), a pharmacological activator of AMP-activated protein kinase (AMPK), inhibits the lipopolysaccharide (LPS)-induced production of proinflammatory cytokines. MRL/MPJ-Fas(lpr) (MRL/lpr) mice show an intrinsic decreased threshold for the production of inflammatory mediators when stimulated.
Jing-Yu Lin et al.
Cell discovery, 6, 20-20 (2020-04-15)
Tissue regeneration, such as pancreatic islet tissue propagation in vitro, could serve as a promising strategy for diabetes therapy and personalised drug testing. However, such a strategy has not been realised yet. Propagation could be divided into two steps, in
Judith Giroud-Gerbetant et al.
Molecular metabolism, 30, 192-202 (2019-11-27)
A decay in intracellular NAD+ levels is one of the hallmarks of physiological decline in normal tissue functions. Accordingly, dietary supplementation with NAD+ precursors can prevent, alleviate, or even reverse multiple metabolic complications and age-related disorders in diverse model organisms.
Raghvendra K Dubey et al.
Hypertension (Dallas, Tex. : 1979), 66(6), 1207-1219 (2015-09-30)
The goal of this study was to determine whether and how adenosine affects the proliferation of human coronary artery smooth muscle cells (HCASMCs). In HCASMCs, 2-chloroadenosine (stable adenosine analogue), but not N(6)-cyclopentyladenosine, CGS21680, or N(6)-(3-iodobenzyl)-adenosine-5'-N-methyluronamide, inhibited HCASMC proliferation (A2B receptor
H Jia et al.
Oncogene, 34(27), 3568-3581 (2014-09-10)
The DNA damage response (DDR) helps to maintain genome integrity, suppress tumorigenesis and mediate the radiotherapeutic and chemotherapeutic effects on cancer. Here we report that p57Kip2, a cyclin-dependent kinase (CDK) inhibitor implicated in the development of tumor-prone Beckwith-Wiedemann syndrome, is
Zubing Cao et al.
Reproduction (Cambridge, England) (2019-03-15)
HASPIN kinase-catalyzed phosphorylation of histone H3 on threonine 3 (H3T3p) directs the activity and localization of chromosomal passenger complex (CPC) and spindle assembly checkpoint (SAC) to regulate chromosome condensation and segregation in both mitosis and meiosis. However, the function of
Catarina Miranda-Lourenço et al.
Neurobiology of disease, 145, 105043-105043 (2020-08-18)
Rett syndrome (RTT; OMIM#312750) is mainly caused by mutations in the X-linked MECP2 gene (methyl-CpG-binding protein 2 gene; OMIM*300005), which leads to impairments in the brain-derived neurotrophic factor (BDNF) signalling. The boost of BDNF mediated effects would be a significant
Jian Zhuge
Cell biology and toxicology, 25(3), 253-263 (2008-05-14)
5'-adenosine monophosphate (AMP)-activated protein kinase (AMPK) is a phylogenetically conserved serine/threonine protein kinase. AMPK may inhibit cell growth and proliferation and also regulates apoptosis. 5'-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR) is a cell-permeable AMPK activator. Activation of AMPK with AICAR has been shown to
Paula A Pousinha et al.
The Journal of pharmacology and experimental therapeutics, 332(1), 153-163 (2009-10-01)
Adenosine-induced modulation of neuromuscular transmission in young (3-4-week-old) rats was evaluated. Inhibition of adenosine kinase with iodotubercidin (ITU; 10 microM), which is known to induce adenosine release, enhanced the amplitude of evoked end-plate potentials (EPPs) recorded from innervated diaphragm muscle
Eun Jee Chung et al.
Scientific reports, 7(1), 17651-17651 (2017-12-17)
Age related macular degeneration is the leading cause of blindness in the developed world. Although its precise cause remains elusive, dysfunction of the retinal pigment epithelium (RPE) and dysregulation of complement have been implicated in its pathogenesis. The goal of
Clara Campàs et al.
Blood, 101(9), 3674-3680 (2003-01-11)
Acadesine, 5-aminoimidazole-4-carboxamide (AICA) riboside, induced apoptosis in B-cell chronic lymphocytic leukemia (B-CLL) cells in all samples tested (n = 70). The half-maximal effective concentration (EC(50)) for B-CLL cells was 380 +/- 60 microM (n = 5). The caspase inhibitor Z-VAD.fmk
Gabriel M Gordon et al.
Wound repair and regeneration : official publication of the Wound Healing Society [and] the European Tissue Repair Society, 24(1), 89-99 (2015-12-10)
The goal of this study was to develop and validate a simple but quantitative cell-based assay to identify compounds that might be used pharmaceutically to give tissue repair a more regenerative character. The cornea was used as the model, and
Anna De Antoni et al.
The Journal of cell biology, 199(2), 269-284 (2012-10-17)
By phosphorylating Thr3 of histone H3, Haspin promotes centromeric recruitment of the chromosome passenger complex (CPC) during mitosis. Aurora B kinase, a CPC subunit, sustains chromosome bi-orientation and the spindle assembly checkpoint (SAC). Here, we characterize the small molecule 5-iodotubercidin
Giuseppe Pignataro et al.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 27(1), 1-5 (2006-05-11)
Adenosine is an endogenous neuromodulator with anticonvulsive and neuroprotective activity. Adenosine levels are normally kept in the range of 20 to 200 nmol/L by low basal expression of its main metabolic enzyme, adenosine kinase (ADK). Dysfunction of the adenosinergic system
Cai Liang et al.
EMBO reports, 19(1), 43-56 (2017-11-16)
Sister-chromatid cohesion mediated by the cohesin complex is fundamental for precise chromosome segregation in mitosis. Through binding the cohesin subunit Pds5, Wapl releases the bulk of cohesin from chromosome arms in prophase, whereas centromeric cohesin is protected from Wapl until
Nikolaos E Efstathiou et al.
PloS one, 15(12), e0244307-e0244307 (2020-12-29)
Age-related macular degeneration (AMD) is the most prevalent form of irreversible blindness in the developed world. Aging, inflammation and complement dysregulation affecting the retinal pigment epithelium (RPE), are considered significant contributors in its pathogenesis and several evidences have linked tumor
Simon I R Lane et al.
Development (Cambridge, England), 144(19), 3475-3486 (2017-08-31)
Mouse oocytes carrying DNA damage arrest in meiosis I, thereby preventing creation of embryos with deleterious mutations. The arrest is dependent on activation of the spindle assembly checkpoint, which results in anaphase-promoting complex (APC) inhibition. However, little is understood about
The cytotoxic effect of purine riboside on COS-7 cells.
K Tkacz et al.
Advances in experimental medicine and biology, 486, 355-359 (2002-01-11)
Hai-Ying Shen et al.
Epilepsia, 51(3), 465-468 (2009-08-14)
Sudden unexpected death in epilepsy (SUDEP) is a significant cause of mortality in people with epilepsy. Two postulated causes for SUDEP, cardiac and respiratory depression, can both be explained by overstimulation of adenosine receptors. We hypothesized that SUDEP is a
Chiachen Chen et al.
Cellular signalling, 76, 109785-109785 (2020-09-24)
Aggressive form of neuroblastoma (NB) is a malignant childhood cancer derived from granule neuron precursors and sympatho-adrenal lineage with N-MYC amplification. An insulinoma associated-1 (INSM1) transcription factor has emerged as a NB biomarker that plays critical role in facilitating tumor
Munjal M Acharya et al.
Scientific reports, 7, 42885-42885 (2017-02-22)
Among the dangers to astronauts engaging in deep space missions such as a Mars expedition is exposure to radiations that put them at risk for severe cognitive dysfunction. These radiation-induced cognitive impairments are accompanied by functional and structural changes including
Rajat Mudgal et al.
FEBS letters, 594(4), 678-694 (2019-10-18)
Alphaviruses, including Chikungunya (CHIKV) and Venezuelan equine encephalitis virus (VEEV), are among the leading causes of recurrent epidemics all over the world. Alphaviral nonstructural protein 1 (nsP1) orchestrates the capping of nascent viral RNA via its S-adenosyl methionine-dependent N-7-methyltransferase (MTase)
Walied A Kamel et al.
Molecular cancer therapeutics, 16(1), 182-192 (2016-11-02)
Osteosarcoma is the most common type of primary bone tumor, novel therapeutic agents for which are urgently needed. To identify such agents, we screened a panel of approved drugs with a mouse model of osteosarcoma. The screen identified simvastatin, which
D Massillon et al.
The Biochemical journal, 299 ( Pt 1), 123-128 (1994-04-01)
Addition of micromolar concentrations of the adenosine derivative 5-iodotubercidin (Itu) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase [Flückiger-Isler and Walter (1993) Biochem. J. 292, 85-91]. We report here that Itu also
Vincenzo Marzolla et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 34(9), 12450-12465 (2020-07-31)
Mineralocorticoid receptor antagonists (MRAs) are recommended for the treatment of heart failure and hypertension, mainly due to their natriuretic and anti-fibrotic mode of action. Rodent studies have shown that MRAs can prevent adverse metabolic consequences of obesity but an elucidation
Suman Rao et al.
Cell chemical biology, 26(6), 818-829 (2019-04-16)
Covalent kinase inhibitors, which typically target cysteine residues, represent an important class of clinically relevant compounds. Approximately 215 kinases are known to have potentially targetable cysteines distributed across 18 spatially distinct locations proximal to the ATP-binding pocket. However, only 40
Hiroyuki Fujimori et al.
Biological & pharmaceutical bulletin, 25(3), 307-311 (2002-03-27)
To elucidate the biological significance of extracellular adenine compounds, the effects of adenosine (Ado) on cellular levels of adenine compounds, especially adenosine triphosphate (ATP), in PC12 cells were studied. Ado and inosine but not adenosine 5'-monophosphate, adenosine 5'-diphosphate, ATP, guanosine
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