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A candidate protein for the regulation
2024-08-19
A candidate protein for the regulation of AMPAR transport is CaMKII, a Ca2+-dependent kinase with diverse cellular functions. With respect to synaptic transmission, CaMKII is recognized as a key synaptic protein that is required to modify the number of synaptic AMPARs in response to LTP and LTD stim
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Epidermal growth factor EGF has been shown to increase the
2024-08-19
Epidermal growth factor (EGF) has been shown to increase the 12S-lipoxygenase mRNA level by about two-fold in human epidermoid carcinoma A431 cells [71]. This enzyme was shown to be of the platelet-type and associated with the microsomal fraction of the cells [71], [72]. A requirement for EGF recept
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(S)-Crizotinib br Depletion of serum amino acids
2024-08-19
Depletion of serum amino acids Currently, the only anticancer agents that directly target amino (S)-Crizotinib metabolism are bacterial l-asparaginases (from Escherichia coli and Erwinia chrysanthemi), which are FDA-approved for treatment of pediatric and adult ALL. A potential complication of u
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Interestingly intermittent high doses of AKT inhibitors have
2024-08-17
Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula
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As an alternative to chronic receptor blockade we have
2024-08-17
As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify ACET adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK facilitates the c
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During myeloid cell maturation expression of LO mRNA and
2024-08-17
During myeloid cell maturation, expression of 5-LO mRNA and protein is strongly induced (60–130-fold) by calcitriol (1,25(OH)2D3) and transforming growth factor-β (TGFβ) [6,7]. The upregulation of 5-LO mRNA transcription is mainly due to transcript elongation and mRNA maturation [8,9]. Interestingly
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br Conclusion br Conflicts of interest br
2024-08-17
Conclusion Conflicts of interest Introduction RNA interference is a specific post-transcriptional gene silencing mechanism within a cell via the transfection of microRNAs (miRNA), exogenous small interfering RNAs (siRNA) or small hairpin RNAs (shRNA) [1–3]. Transfection of shRNA can be done
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Fencilli et al reported derivatives of PHA which
2024-08-17
Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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br Aurora A Aurora B and
2024-08-17
Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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The Type A series contains of the confirmed
2024-08-17
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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In agreement with the role of ACLY
2024-08-17
In agreement with the role of ACLY in induced macrophage, we observe a drastically reduction of PGE2 levels when ACLY activity is inhibited. This is possible because PGE2 production requires arachidonic acid, which in turn is synthesized by elongation of dietary linoleic Gefitinib sale with acetyl-
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Previous studies have demonstrated ATR inhibition is effecti
2024-08-17
Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia Curcumol to enhance chemotherapy sensitivity [[16], [17], [18],[20], [21], [22]]. VE
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br Introduction In the past two decades
2024-08-17
Introduction In the past two decades, graphene and graphene based nanomaterials with unique physicochemical properties have attracted great attentions in many fields including biomedicine and biotechnology. Graphene oxide (GO) and its derivatives have shown promising potential as biological and c
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br Other Strategies for HIF
2024-08-16
Other Strategies for HIF-α Inhibition NSC-644221 is another HIF-α inhibitor acting at the translational level, independently of proteasomal degradation and VHL status, and is devoid of DNA damage-inducing properties [70]. NSC-644221 arrests Quinacrine hydrochloride hydrate in G2–M through a cell
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Ch 55 br Natriuretic peptides and neprilysin Left ventricula
2024-08-16
Natriuretic peptides and neprilysin Left ventricular systolic function, most commonly due to myocardial damage as a consequence of coronary artery disease, hypertension or both, and leading to sustained, pathological activation of the renin angiotensin Ch 55 system (RAAS) and sympathetic nervous
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