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Several structural classes of ASK
2024-11-14
Several structural Imiloxan hydrochloride of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck an
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br HMGB proteins and chromatin structure The
2024-11-14
HMGB proteins and chromatin structure The multifaceted roles played by HMGB (formerly called HMG-1 and -2) proteins in modulating chromatin structure, gene transcriptional activity and cellular phenotype have been covered in a number of recent reviews and readers are referred to these for in-dept
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In humans the superior safety profile of
2024-11-14
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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In the MT SGL two
2024-11-13
In the MT-SGL, two regularization parameters need to be specified: λ1 and λ2. Using recent results on norm regularization (Banerjee et al., 2014), it is possible to express both parameters via a single parameter as follows: and (Meier et al., 2008, Banerjee et al., 2014), where and are computed as:
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To date defining the prognostic impact
2024-11-13
To date, defining the prognostic impact of molecular drivers of early-stage NSCLC has been challenging due to the relative rarity of these subsets and the redefinition of comparator arms over time as understanding of the molecular drivers of NSCLC evolved. Indeed, use of molecularly heterogeneous co
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Although several ARIs have reached various phases of clinica
2024-11-13
Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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The finding that OCT is expressed in the nucleus
2024-11-13
The finding that OCT3 is expressed in the nucleus accumbens (Gasser et al., 2009) suggests that inhibition of this transporter may underlie previously described effects of glucocorticoids on extracellular DA concentrations and indicates that DA clearance in this region is not mediated exclusively by
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Rising depolarization was observed during and decaying depol
2024-11-13
Rising depolarization was observed during and decaying depolarization after the photostimulation (Fig. 1D). The slow decrease of the firing rate after photostimulation is also a remarkable characteristic of the striatal neuron (Figs. 1E, 2 and 3), since the cortex pyramidal neurons (data not shown)
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Adiponectin also works on AdipoR inducing extracellular Ca i
2024-11-13
Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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br Conclusions br Funding br Acknowledgements and
2024-11-13
Conclusions Funding Acknowledgements and Disclosures We would like to thank veterinarian Angelina Williams and assistants Justin Courson, Ashutosh Jnawali, Mythri Puella, Santoshi Ramachandran, and Zhihui She for support during dissections. We also thank Drs. Vallabh Das, Deborah Otteson an
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The pathogenesis of d penicillamine induced
2024-11-13
The pathogenesis of d-penicillamine-induced MG is not clear. The repertoire of anti-AChR thapsigargin in d-penicillamine-induced MG has been shown to be similar to that in idiopathic MG in terms of AChR antigenic regions, suggesting a common immune mechanism (Tzartos et al., 1988). About 20% of d-
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br Acknowledgements MC and PD were
2024-11-13
Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b
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br Author contributions br Competing
2024-11-13
Author contributions Competing interests Transparency document Acknowledgments This research was funded by a TOP ZonMW grant (40-00812-98-10054) to R.O.E., a DFG grant (KR4391/1-1) and IZKF Erlangen grant (J36) to A.K. and supported in part by Centro de Investigación Biomédica en Red de
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ATP citrate lyase ACLY is a cytosolic enzyme
2024-11-13
ATP citrate lyase (ACLY) is a cytosolic enzyme that catalyzes the generation of acetyl-CoA from citrate [15]. Acetyl-CoA is the building block for the biosynthesis of fatty acids and cholesterol, and also serves as a substrate of the acetylation reaction of various molecules, including histones and
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Aromatization of the pyrrole ring after anion capturing usin
2024-11-13
Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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