• crth2 antagonist A role for YAP in mediating resistance to E

  2025-01-27

  

  A role for YAP in mediating resistance to EGFR inhibition has also been described [28], [29]. In line with these evidences, we observed increased YAP activation in all the generated EGFR TKI–resistant cells, testified by decreased phosphorylation on the inhibitory serine 127, enhanced nuclear locali

• Docking studies were performed on the

  2025-01-27

  

  Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-83

• Song et al reported series of triazolylsalicylamide

  2025-01-27

  

  Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se

• br Acknowledgements br Introduction Double stranded DNA brea

  2025-01-27

  

  Acknowledgements Introduction Double-stranded DNA breaks (DSBs) are among the most deleterious DNA lesions that threaten genomic integrity. DSBs are generated not only by exogenous DNA-damaging agents but also by normal cellular processes such as V(D)J recombination, meiosis, and DNA replicati

• In this review we will present

  2025-01-27

  

  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

• CORT induced hippocampal damage has been

  2025-01-27

  

  CORT-induced hippocampal damage has been implicated in depression, aging and long-term glucocorticoid therapy. Therefore, finding a drug that can protect hippocampal neurons from the adverse effects of CORT could have significant clinical benefits. In this regard, we tested the potential protective

• br Conclusions br Acknowledgements We would like to

  2025-01-27

  

  Conclusions Acknowledgements We would like to thank the members of the Bergmann lab for fruitful discussions in the course of this work. This work was supported by the National Institute of General Medical Sciences (NIGMS) under award number R35 GM118330. The content is solely the responsibili

• SM-164 Although the role of apelin and APJ receptor in

  2025-01-27

  

  Although the role of apelin and APJ receptor in cardiovascular functions has been well-elucidated, little is known for the effect of the central apelinergic system on gastrointestinal (GI) functions. In mice, it has been found previously that central exogenous apelin-13 decreased gastric emptying (G

• To further evaluate the influence of

  2025-01-27

  

  To further evaluate the influence of 235 6 on allergy, Russel et al. initiated vancomycin treatment during pregnancy in mice and continued it for several weeks after birth. This resulted in exaggerated OVA-induced allergic inflammation, characterized by higher numbers of lung eosinophils, elevated c

• A has been reported to decrease

  2025-01-27

  

  Aβ has been reported to decrease insulin receptors and impair insulin signaling in neurons, preventing phosphorylation of Akt and glycogen synthase kinase 3β (GSK-3β), downstream of insulin signaling, and to increase phosphorylation of tau protein causing neurofibrillary tangles (Tokutake et al., 20

• br Adiponectin in prostate cancer PC was documented

  2025-01-26

  

  Adiponectin in prostate cancer PC was documented as the leading type of malignancy in males in the US with respect to both the estimated number of cases (22,800) and deaths (27,540) (Siegel et al., 2016). Studies have reported an association between low APN levels and the progression of PC (Micha

• As the close paralog of adiponectin

  2025-01-26

  

  As the close paralog of adiponectin, we hypothesized that CTRP9 could participate in regulation of reproduction. In order to evaluate whether Ctrp9 plays a role in the control of reproduction in tilapia, i.p. injection experiment was performed. HPG (Hypothalamic/pituitary/gonadal) axis plays a key r

• In fact serotonin is a major modulator

  2025-01-26

  

  In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc

• br Conclusions and clinical relevance Astrogliosis and

  2025-01-26

  

  Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic Luminescent ATP assay is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonist

• br Acknowledgements This work was supported

  2025-01-26

  

  Acknowledgements This work was supported by Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), Fundação de Amparo à Pesquisa do Estado do Rio Grande do Sul (FAPERGS) FINEP research grant “Rede Instituto Brasil

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