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br ABCA is a sterol
2024-10-18

ABCA2 is a sterol-responsive gene The first evidence to demonstrate that ABCA2 expression responded to sterol loading was provided in an experiment involving monocyte to macrophage differentiation in vitro. Upon sterol loading with enzymatically degraded LDL (eLDL), ABCA2 expression increased onl
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Phosphodiesterase inhibition increases the intracellular lev
2024-10-18

Phosphodiesterase inhibition increases the intracellular levels of cAMP to restore spontaneous contraction (Essayan, 2001, Qi and Kwan, 1996), acting downstream of adenylyl cyclase. Therefore, cardiac arrest induced by decreased intracellular cAMP levels could be reversed by phosphodiesterase inhibi
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Recently several groups including ours have started to use
2024-10-18

Recently, several groups, including ours, have started to use the C. elegans multi-dendritic PVD neurons as a model system to dissect the molecular mechanisms of dendrite development. During larval development, PVD elaborates complex and stereotyped dendritic arbors by sequentially adding primary (1
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A high throughput small molecule ACK
2024-10-18

A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found VUF 11207 fumarate to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) wo
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br Introduction In myasthenia gravis MG autoantibodies again
2024-10-18

Introduction In myasthenia gravis (MG), autoantibodies against the native AChR conformation cause loss of AChR at the neuromuscular junction and fatigable muscle weakness (Newsom-Davis et al., 1993). The AChR is a pentameric transmembrane protein, with two splice forms of the α-subunit, P3A− and
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Although ACE genetic variance does not influence the
2024-10-18

Although ACE genetic variance does not influence the level of bradykinin significantly, the bradykinin level tends to be affected by ACE inhibitor therapy used by patients. ACE inhibitor reduces the ACE activity that may lead to the accumulation of serum bradykinin. The level of bradykinin tends to
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nicotinic acetylcholine receptor Based on these findings the
2024-10-17

Based on these findings, the time point for manipulating autophagy may also determine its role, whereby autophagy induction performed before ischemia could play a protective role but have an opposite effect once ischemia/reperfusion has occurred. This hypothesis is further supported by the protectiv
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17-ODYA receptor In Rainey et al published the results of a
2024-10-17

In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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Although several different membrane estrogen receptors
2024-10-17

Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec
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Dual acting RAAS blockade and neprilysin inhibition has been
2024-10-17

Dual-acting RAAS blockade and neprilysin inhibition has been evaluated in several clinical HF trials. In PARADIGM-HF [6,7], LCZ696 was superior to enalapril in reducing mortality and HF hospitalizations in symptomatic patients with HF with reduced EF. Augmented benefits on maladaptive cardiac remode
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br Natriuretic peptides and neprilysin
2024-10-17

Natriuretic peptides and neprilysin Left ventricular systolic function, most commonly due to myocardial damage as a consequence of coronary artery disease, hypertension or both, and leading to sustained, pathological activation of the renin angiotensin ITE system (RAAS) and sympathetic nervous s
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br Acknowledgments and Disclosures br Introduction Over the
2024-10-17

Acknowledgments and Disclosures Introduction Over the last decade, the most visible strategy for the treatment of Alzheimer's disease (AD) has been amyloid β peptide (Aβ) immunotherapy (reviewed in [1]). Although the first efforts with Aβ immunotherapy failed to complete clinical trials [1], A
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Sulindac The correlation in the increase of BADH mRNA protei
2024-10-17

The correlation in the increase of BADH mRNA, protein levels, and enzyme activity, demonstrate that oxidation of betaine aldehyde by BADH is primordial to regulate the GB accumulation during physiological cardiac hypertrophy induced by pregnancy, this implies a major role because GB levels enhance c
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An important observation in our
2024-10-16

An important observation in our study is the lack of effect of paroxetine pretreatment alone on β2AR membrane expression, which suggests that paroxetine, and pharmacologic inhibition of GRK2 in general, does not directly induce changes in receptor dynamics. Rather, the decreased ligand-induced β-ar
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Introduction hydroxytryptamine HT is found throughout the
2024-10-16

Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary insulin receptor inhibitor (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The cu
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