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br Perspectives and challenges Previously the main
2024-04-02

Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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Based on our previous work and the observation that SNX
2024-04-02

Based on our previous work [13] and the observation that SNX9 is a partner for ACK, we have investigated interactions involving the SH3 domain of SNX9, and identified for the first time synaptojanin-1 as an alternate partner. This SH3 domain can bind a single site in ACK1, but multiple sites in the
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Nowadays more than kinases have been identified of
2024-04-02

Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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TAK-632 australia br The role of apelin in
2024-04-02

The role of apelin in hypertension diseases The role of apelin and its receptor APJ in cardiovascular diseases has been described in numerous studies (Table 2) [36,37]. It has been revealed that exogenous apelin may lower blood pressure. Tatemoto et al. [6] have discovered that different forms of
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Another interesting aspect of neutralizing AP is the inhibit
2024-04-02

Another interesting aspect of neutralizing AP-1 is the inhibition of interactions between AP-1 and Smad proteins, which synergize to activate the TGF-β1-responsive genes involved in hypertrophic growth of the heart muscle and in the development of cardiac fibrosis. Through preventing AP-1 activation
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br Introduction Humans have consumed
2024-04-02

Introduction Humans have consumed mushrooms for centuries because of their high nutrient content and low lipid content, as well as their excellent flavor and texture [1]. Edible mushrooms possess notable medicinal properties and bioactivities, including antitumor, antiviral, antidiabetic, and ant
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2189 br Downstream signalling of AKT A
2024-04-01

Downstream signalling of AKT A consensus phosphorylation motif has been described for AKT substrates: R-X-R-X-X-S/T-B where X represents any amino 2189 and B represents bulky hydrophobic residues (Alessi, Caudwell, Andjelkovic, Hemmings, & Cohen, 1996). Numerous AKT substrates have been publishe
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br A novel therapeutic strategy based on the APN and
2024-04-01

A novel therapeutic strategy based on the APN and obesity paradoxes As shown above, the relationship of the serum APN concentration with health and disease states shows an inverted-U correlation, suggesting that moderate concentrations of serum APN are beneficial (Fig. 3). Given that both hypo- a
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Our initial approach to identify hits was two pronged
2024-04-01

Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI NCT-502 library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was inc
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Macrophage polarization is linked to activation of the
2024-04-01

Macrophage polarization is linked to activation of the ligand-dependent transcription factor PPARγ. Recently, Odegaard et al. demonstrated with a macrophage-specific deletion of PPARγ in mice that alternative macrophage activation is impaired [14]. We provided evidence that contact to apoptotic BMS
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Additionally regulation of GPCR heteromerization by specific
2024-04-01

Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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br Mechanisms of GPCR internalization Like
2024-04-01

Mechanisms of GPCR internalization Like for other types of receptors, prolonged agonist stimulation often leads to GPCR internalization, which can occur via different pathways ∗[2], [20], [21], [22], [23]. Of these pathways, clathrin-mediated LY294002 (CME) is the best characterized and arguably
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The presence of crown like structures and
2024-04-01

The presence of crown-like structures and inflammatory factors in the breast of obese patients is associated with considerable changes in intracellular signaling and a profound cellular dysfunction. Secreted pro-inflammatory factors can directly promote breast carcinogenesis as they have been report
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br Introduction Increasing number of mycosis infections has
2024-03-30

Introduction Increasing number of mycosis infections has been reported during the past several years because of the rise in the number of immuno-compromised individuals in subtropical and tropical countries with high mortality and morbidity [1], [2]. Trichophyton mentagrophytes, Trichophyton rubr
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br Materials and methods br Results br
2024-03-30

Materials and methods Results Discussion Our results revealed that LPS injection in rats impaired fear memory in the PA task. This results are in agreement with the most of previous studies reported that following acute [23,24,39,[45], [46], [47]] or chronic systemic Azithromycin Dihydrate
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