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Pyrimidine is the important pharmacology core in many
2025-02-24

Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the TBB core as well as th
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In this study we have isolated genes
2025-02-24

In this study, we have isolated GSK1324726A that encode ACL from G. zeae through random mutagenesis by restriction enzyme-mediated integration (REMI). The mutant Z39P186 where the ACL gene had been disrupted showed defects in vegetative growth, asexual and sexual development, virulence, and trichoth
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exemplifies three of the compounds investigated in the selec
2025-02-24

exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC Retigabine dihydrochloride as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degra
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GABAB receptor is associated with brain and
2025-02-24

GABAB receptor is associated with nk1 receptor and behavioral diseases, including epilepsy, spasticity, anxiety and neuropathic pain (Bettler et al., 2004, Bowery et al., 2002, Froestl, 2010). Baclofen, a clinical drug and selective GABAB receptor agonist, is used to treat muscle spasticity in patie
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br Acknowledgements We would like to thank Dr Thomas Blanpie
2025-02-24

Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A
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MADS box proteins are combinatorial transcription factors in
2025-02-24

MADS box proteins are combinatorial transcription factors in that they often derive their regulatory specificity from other DNA binding or accessory factors. In many cases, the cofactor with which MADS box proteins interact specifies which genes are regulated, when they are regulated and if these ge
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Second the choice of the PAABD is critical for an
2025-02-24

Second, the choice of the PAABD is critical for an efficient and sensitive biosensor. The sequence of the PAABD should present high affinity and efficient recognition of the phosphorylated substrate, as opposed to poor affinity for the unphosphorylated substrate, and should display a fully reversibl
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br STAR Methods br Acknowledgments We thank Simcere
2025-02-24

STAR★Methods Acknowledgments We thank Simcere Pharmaceuticals, Nanjing, China, for providing a rabbit anti-VEGF neutralizing monoclonal antibody. We thank Dr. Schlisio in the Ludwig Institute for Cancer Research, Karolinska Institute, for assistance with hypoxia assay. Y.C.’s laboratory is sup
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The disease stimulatory effects of hyperadiponectinemia in
2025-02-24

The disease-stimulatory effects of hyperadiponectinemia in patients contradict a previous view based on studies of preclinical models showing that APN might be beneficial for AD [8]. Indeed, despite the action of APN as a risk factor in patients with AD, APN is protective against oxidative stress-in
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In conclusion we have demonstrated
2025-02-21

In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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Phospholipases cleave membrane phospholipids from inflammato
2025-02-21

Phospholipases cleave membrane phospholipids from inflammatory cells, activated platelets, erythrocytes, adipocytes and cancer Rottlerin (Aoki et al., 2008, Neidlinger et al., 2006). Several reports have analysed the role of LPA and its receptors in the pathogenesis of RA. Zhao et al. reported that
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br Dual role of autophagy in
2025-02-21

Dual role of autophagy in human diseases Emerging evidence suggests that autophagy serves as a double-edged sword in several human diseases, such as CNS diseases (Rubinsztein et al., 2015), arteriosclerosis (Schrijvers et al., 2011) and cancer (Ozpolat and Benbrook, 2015). Likewise, currently the
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The evidence points toward a role
2025-02-21

The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e
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Based on the results of studies
2025-02-21

Based on the results of studies done to-date, there are three characteristics that make a letrozole-based protocol attractive for use in cattle: 1) it is steroid-free, 2) it is cost-effective and requires a shorter time and fewer animal handlings than conventional methods (Table 1), and 3) it may ha
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Animal fat appears to increase C perfringens
2025-02-21

Animal fat appears to increase C. perfringens counts compared with vegetable oil, so there may indeed be some advantage to vegetable diets at least in terms of fat sources (Knarreborg et al., 2002). Small grains such as wheat, rye, oats, and barley, with high levels of non-starch polysaccharides are
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