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To our knowledge BAY has
2025-01-26
To our knowledge, BAY 60-6583 has not progressed to clinical development and remains to be the only ADORA2B agonist that has been developed.33, 34 Further development of similar compounds would be beneficial in future fibrosis research. One of the limitations of our study is being limited to in vit
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Calphostin C synthesis The nAChR has been considered an inte
2025-01-26
The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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Since innate immune responses represent the
2025-01-26
Since innate immune responses represent the first defense against incoming infectious microorganisms, they are particularly engaged during the early stages of viral infections. Many innate defense mechanisms rely on the engagement of pattern recognition receptors (PRRs) which are conserved, germ lin
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However there are studies revealing the dark side
2025-01-26
However, there are studies revealing the “dark side” of autophagy at later stages in cancers, when oncogenes (mainly K-ras and B-raf) are activated and/or tumour suppressors such as PTEN and p53 are inactivated. These studies are based on the use of GEMM and deletions of essential autophagy genes (A
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The use of FTAI can overcome the negative impact of
2025-01-26
The use of FTAI can overcome the negative impact of low estrus detection efficiency, but implies effective synchrony of luteal function as well as synchronous growth and ovulation of a viable 98 9 follicle. Pregnancy rates obtained with FTAI may be comparable or better than those obtained after AI w
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br Physiology of the apelin pathway
2025-01-26
Physiology of the apelin pathway Role of apelin in heart disease Both apelin and apelin receptor null mice manifested moderate reduction in cardiac contractile function under basal conditions and their exercise capacity was markedly reduced (Table 1) [56]. Apelin has direct effects on the prop
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Plasma apelin levels predict the major cardiovascular event
2025-01-26
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 lack of benefit in terms of overall survival for
2025-01-24
The lack of benefit in terms of overall survival for antiangiogenic treatment was similar when antiangiogenic drug was used both as first and second-line therapy, and both in association with cytotoxic treatment or alone. Noteworthy, a trend for an inferior outcome was observed in the group of patie
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br Conclusions and perspectives In view of the
2025-01-24
Conclusions and perspectives In view of the evidences supporting that Atglistatin ATGL inhibitor MAS receptors mediate the effects of AT1 antagonists (Iwai et al., 2012, Ohshima et al., 2014, Pernomian et al., 2015, Schuchard et al., 2015), the prime targets from the perspectives on future direc
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The lactam emerged as lead candidate due
2025-01-24
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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T-5224 transcription factor inhibitor As one of emerging hig
2025-01-24
As one of emerging high-throughout methods, metabolomics detects metabolites which are ultimate response of biological systems to environmental changes [14]. Metabolomics uncovers metabolic alteration at the systems level. Comparison of global metabolic profiling reflects some unidentified biologica
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Previous studies to investigate the functions of AHR in
2025-01-24
Previous studies to investigate the functions of AHR in Treg Oseltamivir phosphate have employed a loss-of-function approach, using AHR complete-null mice, or a gain-of-function approach by ligand administration. However, these approaches may confound the interpretation of the results. For example,
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br Impact of global AHR deficiency on diet induced obesity
2025-01-24
Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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Human testicular peritubular cells HTPCs are also the
2025-01-24
Human testicular peritubular PEG2000 NHS bioconjugate (HTPCs) are also the only human testicular cell type that can be isolated, cultured and studied in vitro (Albrecht et al., 2006, Mayerhofer, 2013). Results from recent studies indicate that their roles go beyond sperm transport and include immun
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br Detection and possible treatments
2025-01-24
Detection and possible treatments for prostate cancer PC can be diagnosed, by screening for prostate-specific antigen (PSA) and after diagnosis, treatments may include intense observation, radical prostatectomy, radiation, chemotherapy, hormone therapy or vaccination depending on the type and sta
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