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Data were collected using a Powerlab and Chart
2022-07-16
Data were collected using a Powerlab and Chart 5 software (ADInstruments, Bella Vista, NSW, Australia) and were analysed using GraphPad Prism 5 (GraphPad Software, San Diego, CA). Responses to ghrelin receptor agonists in phenylephrine, methoxamine, endothelin-1, U46619 and 60mM [K+] contracted vess
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br Mechanisms of gap junction internalization disaggregation
2022-07-16
Mechanisms of gap junction internalization: disaggregation, endocytosis and annular gap junctions It has been clearly shown that gap junction internalization can occur by a distinctive mechanism where one cell internalizes an entire gap junction via formation of double membrane structure termed a
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br STAR Methods br Introduction Secretase
2022-07-16
STAR★Methods Introduction γ-Secretase is a membrane-embedded proteolytic complex belonging to a diverse family of intramembrane-cleaving proteases and is composed of four integral membrane proteins: presenilin (PS), nicastrin (NCT), anterior pharynx-defective 1 (Aph-1), and presenilin enhancer
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Clinical trials of all GSIs
2022-07-16
Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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Similar to C lividipennis RDL Jiang et al
2022-07-16
Similar to C. lividipennis RDL (Jiang et al., 2015), we found that the intracellular loop variants of A. mellifera RDL had no effect on GABA EC50 (Table 1). Also, as with C. lividipennis, there was no significant difference in maximal GABA responses (Table 1). However, whereas the 31 amino acid inse
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Concanamycin A synthesis One effective approach to fine tuni
2022-07-16
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Concanamycin A synthesis scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3
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The current lack of effective treatments for primary or meta
2022-07-15
The current lack of effective treatments for primary or metastatic UM leaves a large therapeutic gap for patients and clinicians underscoring an urgent need for the identification of additional pharmacological targets for therapeutic intervention. As YAP-targeting strategies have remained elusive th
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One PKC target that controls cortical actin structure
2022-07-15
One PKC target that controls cortical hinokitiol sale structure is a well-known actin crosslinking protein, myristoylated alanine-rich C-kinase substrate (MARCKS). MARCKS cross-links actin and binds PIP2 and this binding activity is regulated by PKC phosphorylation [82]. Activation of PKC releases
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Endotoxin induced pulmonary hypertension is a reproducible f
2022-07-15
Endotoxin induced-pulmonary anatoxin a synthesis is a reproducible finding in various animal models Leeper-Woodford et al., 1991, Weitzberg et al., 1993 and is also a feature of human sepsis where it may affect right ventricular function (Vincent, 1998). Mechanisms such as vasoconstriction and leuk
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Structurally HMTs can be broadly categorized into three
2022-07-15
Structurally, HMTs can be broadly categorized into three functional enzymatic families, the SET (Suppressor of variegation, Enhancer of zeste, Trithorax)-domain- containing methyltransferases, the non-SET DOT1-like (DOT1L) lysine methyltransferases, the PRDM family, containing a PR (PRDI-BF1-RIZ1 ho
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A biochemical characterisation of this functionally
2022-07-15
A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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Our extensive preliminary data suggest that the loss of
2022-07-15
Our extensive preliminary data suggest that the loss of p300 (and resulting H3K27ac) is related to inorganic arsenic related diseases. Therefore, it may open a new avenue for alleviating the consequence of H3K27ac, for example, via boosting CBP enzymatic activity for at least partially compensating
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br Introduction Regulation of transcription is a critical
2022-07-15
Introduction Regulation of transcription is a critical event of the embryonic development and epigenetic mechanisms such as histone modifications and DNA methylation appear important in mediating temporal changes, and differences among cells/tissues, of temporary stabilized transcriptomes (Mas et
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Literature review suggests a strong presence of central hist
2022-07-15
Literature review suggests a strong presence of central histaminergic transmission in the 69 9 areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release of histamine in the brain [1
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Studies of early cell fate specification in the mouse embryo
2022-07-15
Studies of early cell fate specification in the mouse embryo have identified a role for differential Motin localization in controlling Hippo signaling [88]. At the 32-cell stage, mouse blastomeres are subdivided into inner cells, which form the inner cell mass (ICM), and outer cells, which form the
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