• What can we learn about

  2023-08-30

  

  What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito

• The acidification of endocytic compartments is closely relat

  2023-08-30

  

  The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe

• As cytosolic acetyl CoA levels in hepatocytes

  2023-08-30

  

  As cytosolic acetyl-CoA levels in hepatocytes descend, cellular production and concentration of cholesterol go down, a change that is known to be sensed by the Sterol response element binding protein (SREBP)/Cleavage-Activating Protein system, leading to SREBP escort to the Golgi apparatus, cleavage

• In this review we will present

  2023-08-30

  

  In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since

• Negative regulation of AR expression by NF B

  2023-08-30

  

  Negative regulation of AR expression by NFκB was also correlated with the ‘age-dependent desensitisation’ of androgen action in the rat liver (Supakar et al., 1995). In this case the binding site was mapped upstream of the gene to sequences −555 to −565 bp, that binds heterodimers of p65 and p50, as

• Interestingly we noticed that LPS exposure was

  2023-08-30

  

  Interestingly, we noticed that LPS exposure was associated with decreased phosphorylation of AMPK and increased phosphorylation of p70S6K1, suggesting that AMPK inactivation and the subsequent mTOR activation might be involved in the development of LPS-induced inflammation. On the other side, treatm

• Calcium entry through postsynaptic NMDARs activates intracel

  2023-08-30

  

  Calcium entry through postsynaptic NMDARs activates intracellular signaling cascades including Ca2+/calmodulin (CaM)-dependent protein kinase II (CaMKII) and calcineurin. The spatiotemporal abundance of this Ca2+/CaM complex determines the direction of synaptic plasticity, resulting in LTP (Malinow

• br Disclosure br Acknowledgments br Introduction

  2023-08-30

  

  Disclosure Acknowledgments Introduction Deeper understanding of the pathobiology of non-small cell lung cancer (NSCLC) has led to the development of small Bay 65-1942 HCl salt sale that target genetic mutations known to play critical roles in the progression to metastatic disease. Mutations

• Studies on both TCDD treated mice and AhR

  2023-08-30

  

  Studies on both TCDD treated mice and AhR null mice have also pointed to a role of AhR in hematopoiesis [65], [66]. Singh et al. showed that AhR is a negative regulator of HSC (hematopoietic stem cell) proliferation, while deletion of AhR leads to spleen enlargement in juvenile and adult mice [67].

• Elacridar br Mechanisms for regulation of intracellular

  2023-08-30

  

  Mechanisms for regulation of intracellular cholesterol homeostasis Cells maintain intracellular free cholesterol levels and distribution within stringent tolerances by several mechanisms [55]: (1) uptake of native LDL (the major extracellular carrier of cholesterol) by LDL receptors and modified

• TCEP br Detection and possible treatments for prostate cance

  2023-08-30

  

  Detection and possible treatments for prostate cancer PC can be diagnosed, by screening for prostate-specific antigen (PSA) and after diagnosis, treatments may include intense observation, radical prostatectomy, radiation, chemotherapy, hormone therapy or vaccination depending on the type and sta

• Endogenous adenosine systems have largely been implicated

  2023-08-29

  

  Endogenous adenosine systems have largely been implicated in drug actions by the demonstration that caffeine (non-selective A1R and A2AR antagonist) (see Section The issue of caffeine), in doses up to 7.5–10mg/kg, inhibits antinociception, and when this occurs, it g proteins is generally also seen

• Beauvericin synthesis br Conclusions The following are the s

  2023-08-29

  

  Conclusions The following are the supplementary data related to this article. Author contributions Conflict of interest Funding sources This work was supported by the Canadian Institutes of Health Research [grant: MOP-79470]. Introduction Sperm cells undergo a number of physical and

• Acetazolamide To understand the kinase selectivity profile

  2023-08-29

  

  To understand the kinase selectivity profile of this series, Acetazolamide , as a representative analog from this series, was profiled against 216 purified protein kinases representing the tyrosine and serine/threonine kinase families using an in-house Caliper EZ Reader mobility shift assay. Assays

• br Experimental section br Competing interests br Author s

  2023-08-29

  

  Experimental section Competing interests Author's contributions Acknowledgement This research is partially supported by a seed fund for the Center for Drug Discovery and Translational Research (LS) and a research grant by Fujifilm (VPS and LS). The Sponsors played no roles in study desig

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