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A third motif involves the toggle
2024-04-29
A third motif involves the toggle switch and consists of the conserved FxxCWxP sequence in TM6 of class A GPCRs (Hofmann et al., 2009, Rosenbaum et al., 2009). Rotamerization of Trp in combination with a kink caused by Pro facilitates the outward movement of TM6 upon activation (Hofmann et al., 2009
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At the outset of targeting the two
2024-04-29
At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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br Material and methods br
2024-04-29
Material and methods Results Discussion Asparagine, arginine, leucine, methionine, and glutamine are the essential Lovastatin for cancer cells and intensively investigated for the development of selective targeted therapeutics. Among them, asparagine depleting bacterial enzyme asparaginase
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Of the cardiovascular studies involving ARBs reported
2024-04-28
Of the cardiovascular studies involving ARBs, 3 reported renal outcomes. In the Losartan Intervention For Endpoint study, albuminuria was observed less frequently in the losartan than in the atenolol arm (7% vs. 13%; p=0.002) (5). In the Candesartan Antihypertensive Survival Evaluation in Japan tria
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br AR signaling and urothelial cancer progression As shown
2024-04-28
AR signaling and urothelial cancer progression As shown in other types of malignancies, such as prostate cancer cells, it has been documented that androgens induce AR expression and its nuclear translocation as well as ARE promoter activity in urothelial cancer cells (Chen et al., 2003, Izumi et
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The mechanisms that control Ahr transcription are
2024-04-28
The mechanisms that control Ahr transcription are poorly understood, especially when considering cell type-specific regulation. A recent report suggested that the Ahr transcription might be directly promoted by RORγt [retinoic fluorescent probes receptor (RAR)-related orphan receptor γt] based on C
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Diabetes or inflammation is associated with up regulation
2024-04-28
Diabetes or inflammation is associated with up-regulation of A2AAR (Pang et al., 2010). High levels of A2AARs are found in macrophages and microglial cells that are poised, on activation, to abrogate the immune response (Trincavelli et al., 2008). In addition, hyperglycemia is associated with increa
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MicroRNA miRNA is an abundant group of small nucleotide nonc
2024-04-28
MicroRNA (miRNA) is an abundant group of small (22-nucleotide) noncoding RNA molecules that directly binds with 3′ untranslated region (UTR) of target messenger RNAs (mRNAs) to regulate gene expression, playing an important role in variety of biological processes including cell proliferation, apopto
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Our previous studies and others have identified that
2024-04-27
Our previous studies and others have identified that the inhalational anesthetic isoflurane induces neuronal apoptosis via [Ca2+]i overload through the opening of synaptic voltage-dependent calcium channels (VDCCs) and the excessive Ca2+ release from the endoplasmic reticulum (Zhao et al., 2011; Zha
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Plasma apelin levels predict the major cardiovascular event
2024-04-27
Plasma apelin levels predict the major cardiovascular event after percutaneous coronary intervention in patients with ST elevation myocardial infarction (STEMI), and adverse events are higher in patients with lower plasma apelin levels [75]. Apelin and its receptor are markedly upregulated in the he
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The PDZ domains of DLG interact with tumor
2024-04-27
The PDZ domains of DLG interact with tumor suppressor proteins, APC and PTEN, as well as with several viral oncoproteins such as the E6 protein present in oncogenic human papillomavirus (reviewed in [177]). It has been reported that overexpression of DLG in fibroblasts impairs the events in the G0/G
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br The lipoxygenase pathway in diseases
2024-04-27
The 12/15-lipoxygenase pathway in diseases of the nervous system Conclusions and future perspectives Arachidonic EPZ004777 australia and other polyunsaturated fatty acids, and their lipid metabolites, play very important roles in human health and disease. This review has outlined the function
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Introduction Epinephrine is an endocrine hormone mainly prod
2024-04-27
Introduction Epinephrine is an endocrine hormone mainly produced by adrenal medulla in response to stress (Tank and Lee Wong, 2015). This catecholamine exerts various major physiological effects, concerning notably the cardiovascular system, the respiratory system and the endocrine system, through
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Actin is capable of polymerizing spontaneously However this
2024-04-26
Actin is capable of polymerizing spontaneously. However, this process is relatively slow and kinetically unfavorable in cells. Formation of Sulbactam dimers and trimers, which can easily disassemble due to their instability, is a rate-determining step in actin polymerization [5], [6]. The shape and
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Five alternatively spliced isoforms of ATX have been describ
2024-04-26
Five alternatively-spliced isoforms of ATX have been described and all are catalytically active [16], [17]. The original ATX described in 1992 is termed ATXα, whereas the most abundant isoform is ATXβ and is the same isoform responsible for plasma lysoPLD activity [18]. Full length ATX is synthesize
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