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ACE inhibition is often thought to play a
2022-11-08
ACE inhibition is often thought to play a central role in the mechanisms of blood pressure reduction in vivo, and most ACE inhibitory (ACEi) peptides were characterized based on in vitro ACE inhibition. A relationship between in vitro ACE inhibition and antihypertensive activity, however, is not app
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br Acknowledgements MC and PD were funded by
2022-11-08
Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b
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Given the recent discovery of regions of
2022-11-08
Given the recent discovery of regions of single-stranded DNA in the nuclei of hypoxic cells, the role for ATR in the response to hypoxic stress seems clearer . Zou and Elledge demonstrated that both Ddc 2 (the homolog of ATRIP) and ATRIP have a lower affinity for double-strand breaks than they do f
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A high throughput screening campaign led to the
2022-11-08
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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Several structural classes of ASK inhibitors
2022-11-08
Several structural Fmoc-Phe-OH receptor of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and
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br APJ expression in metabolic diseases Under physiological
2022-11-08
APJ expression in metabolic diseases Under physiological conditions, APJ is present in humans as well as in mouse tissues with high metabolic activity such as muscle and adipose tissue but not in the liver. Moreover, the presence and regulation of APJ in established adipocyte or muscle cell lines
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Aconitase clusters are prone to
2022-11-07
Aconitase clusters are prone to oxidations and are among the first to undergo a change in transition state during stages of electrophilic stress rendering them inactive [31]. Aconitase activity in LETO and OLETF did not differ at T0 suggesting that the early onset of insulin resistance may not be at
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Moreover a multiple regression analysis using the year
2022-11-07
Moreover, a multiple regression analysis using the 1-year MMSE score as a dependent variable was conducted. The result showed that serum football levels at admission did not affect the MMSE score 1 year later (β = 0.10, p = 0.639). Discussion In this study, serum Aβ42 levels were significantly
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br Results br Discussion Using primarily
2022-11-07
Results Discussion Using primarily an electrophysiological analysis of dysbindin-deficient hippocampal neurons in cultures and slices, we have uncovered a previously unreported role for dysbindin in enhancing CA3–CA1 AMPAR-mediated transmission. An earlier study, however, has reported a reduct
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Moreover mice exposed to high cholesterol diet have mildly a
2022-11-07
Moreover, mice exposed to high-cholesterol diet have mildly activated astrocytes, increased expression of ApoE and aquaporin-4 in the hippocampus, and altered levels of proteins associated with Aβ metabolism (Chen et al., 2016), which is related to a higher demand for cholesterol transport and the n
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br Conflicts of interest br Acknowledgements This
2022-11-07
Conflicts of interest Acknowledgements This work was sponsored by grants from Longyan University Scientific Research Fund for the Young Scholars (LQ2016010), Middle-aged and Young Teachers Education Research Projects of Fujian Province (JAT170569), Longyan University Scientific Research Fund f
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3mb br Liver specific AHR deficiency and
2022-11-07
Liver-specific AHR deficiency and energy balance In contrast to the amelioration of hepatic steatosis by global AHR deficiency, targeted knockout of Ahr in hepatocytes exacerbated it in B6 mice fed on a high-fat diet, without interfering with body weight gain [21]. This appeared to result from au
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br New AMPK activators Fenofibrate is a drug of the
2022-11-07
New AMPK activators Fenofibrate is a drug of the fibrate class used for the treatment of dyslipidemia [53] but is also an agent that could alleviate DN-induced alterations through AMPK activation (Fig. 2). Streptozotocin-induced diabetic rats treated with fenofibrate improved in not only renal fu
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The structures of these compounds were confirmed from
2022-11-07
The structures of these compounds were confirmed from their spectral and micro analytical data. Based on [M + H] 367, molecular formula of was established as CHON. The IR spectrum of showed melk inhibitor due to CO stretching at 1700 Cm & OH stretching at 3188 Cm indicating that compound contains o
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The role of DHT in early teleost embryogenesis is not
2022-11-07
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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