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The fibroblast growth factor receptor FGFRs including
2021-12-09
The fibroblast growth factor receptor (FGFRs), including four highly conserved proteins (FGFR1-4), are important membrane sensors for extracellular signals [4]. By binding to their ligands, FGFRs are activated and can trigger various downstream intracellular signaling cascades, which is required for
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Pharmacological inhibition of PKR seems to be an
2021-12-09
Pharmacological inhibition of PKR seems to be an interesting strategy for revealing the role of PKR in oxytosis and ferroptosis. The oxindole/imidazole derivative C16 was identified by screening a library of 26 different ATP-binding site-directed inhibitors of varying structure that is more selectiv
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The cases of the Berlin and London patients also
2021-12-09
The cases of the Berlin and London patients also highlight our limits to defining an HIV cure. No signs of the virus have been found in numerous assays with multiple samples from diverse tissues that Timothy Brown has generously contributed to advance research over the past 12 years. In the case of
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br Resistance to targeted therapy
2021-12-08
Resistance to targeted therapy The idea of treating HER2 mutant tumors with specific therapies is relatively new and, as a consequence, little is known about the potential mechanisms of resistance to anti-HER2 agents in this setting. Primary resistance may be mediated by the presence of on-targe
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Several classes of small molecules that modulate CDK activit
2021-12-08
Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymat
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Also in this work we investigated the
2021-12-08
Also in this work, we investigated the correlated signaling pathways of GSK-3 inhibition in protecting bupivacaine-induced DRG neurotoxicity. Through western blot assay, we demonstrated that, SB216763 suppressed protein productions of p-GSK-3 α/β and Casp-3, but increased protein production of PKC,
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br Results br Discussion Cell contact mediated spread of HIV
2021-12-08
Results Discussion Cell-contact-mediated spread of HIV-1 has been estimated to be at least an order of magnitude more efficient compared to passive dissemination of particles through the extracellular milieu. Thus, this form of viral transmission can have significant effects on the pathogenesi
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braf inhibitors The facts mentioned above indicate that glyc
2021-12-08
The facts mentioned above indicate that glycine function in brain is tightly regulated or pathologically altered mostly by glycine transporters. Modification of cytosolic regions of transporters, which interconnect them with intracellular regulatory pathways, could be one of the ways to provoke brai
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In this study we present the synthesis and
2021-12-08
In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g
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The role of the ER
2021-12-08
The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of ARL 67156 trisodium salt levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might pr
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Taken together previous data suggest that ghrelin signaling
2021-12-08
Taken together, previous data suggest that ghrelin signaling is causally linked to alcohol use and may regulate alcohol seeking and consummatory behaviors [[66], [67], [68]]. As such, the ghrelin system may represent a therapeutic target for AUD. Here, we provide a narrative review of the existing
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We note that zinc speciation at
2021-12-08
We note that zinc speciation at and 2 mol. equiv. of myristate is already markedly different; this means that FFAZn2+ crosstalk is in operation under normal physiological conditions. At present, there are few data to allow tracking of the effects of such physiological crosstalk, although there are s
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br Introduction Atrial fibrillation is the most common
2021-12-08
Introduction Atrial fibrillation is the most common cardiac arrhythmia (Benjamin et al., 1998). Pulmonary vein (PV) sleeves contain a mixture of working myocardium and potential arrhythmogenic pacemaker Tadalafil behaving as an ectopic trigger of atrial fibrillation (Haissaguerre et al., 1998, C
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JMJD C is another JmjC domain
2021-12-07
JMJD1C is another JmjC domain protein discovered as a putative oncogene in shRNA screens in MLL-AF9-, HOXA9-, and AML1-ETO-driven AML 40, 41, 42. Depletion of JMJD1C decreased the frequency of LICs by inducing their differentiation and impaired the growth and establishment of leukemia in serial tran
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Given the major differences between the molecular regulation
2021-12-07
Given the major differences between the molecular regulation of the genes encoding HO-1 (HMOX1) in mice and humans, it is not appropriate to utilize mouse models for mechanistic analyses of human HMOX1[35]. In addition, it has been reported that drugs, such as statins, as well as stressors and the r
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