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br Results br Discussion Here
2019-12-02
Results Discussion Here we establish a key kinase cascade that acts at PCs to promote homolog pairing and synapsis. CHK-2 phosphorylates the zinc finger proteins that specify PCs, which, in turn, primes their recruitment of PLK-2 (Figure 7D). By recruiting these two kinases, PCs serve as signa
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perhexiline sale br Materials and methods br Results br Disc
2019-12-02
Materials and methods Results Discussion For many years, oral PDE5-Is have been prescribed as an on-demand regimen for treating ED. Several studies have reported on the efficacy and safety of such a regimen, with an overall efficacy rate of 60–70% [21]. However, many patients complain of a
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Currently phosphodiesterase type PDE inhibitors are used wid
2019-12-02
Currently, phosphodiesterase type 5 (PDE-5) inhibitors are used widely as the first- line oral treatment for erectile dysfunction of varying causes. Radical prostatectomy for the treatment of prostate cancer is frequently associated with erectile dysfunction, and this type of erectile dysfunction is
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Given the potency enhancing effect of
2019-12-02
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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We have previously shown that
2019-12-02
We have previously shown that sustained 8-pCPT treatment favored Ca2+-dependent arrhythmogenic activity in rat ventricular cardiomyocytes [8]. Fig. 2 shows line-scan Ca2+ images of myocyte incubated without (Fig. 2A left) and with 8-pCPT (Fig. 2A right) subjected to a train of electrical stimulation
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Introduction Neuropathic pain occurs in approximately one
2019-12-02
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an
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br No Evidence for Further ET Receptor Subtypes Further rece
2019-12-02
No Evidence for Further ET-Receptor Subtypes Further receptor subclassifications have been proposed including suggestions that ETB could be subdivided into ETB1, present on endothelial cells, and ETB2 on smooth muscle cells, but there currently is no evidence that the receptors expressed by these
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For this study we have used
2019-12-02
For this study we have used the intermediate affinity mutant antigen HEL2× for immunization. However, we have observed a similar defect in the plasmablast differentiation of EBI2-deficient SWHEL C598-0466 over a 10,000-fold affinity range by using WT HEL or the low-affinity mutant HEL3× (data not s
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The small GTPase Ran regulates karyopherin cargo interaction
2019-11-30
The small GTPase Ran regulates karyopherin–cargo interactions and the directionality of karyopherin-mediated transport. Like other Ras-family GTPases, Ran cycles between GTP- and GDP-bound states, and the two surface loops in Ran, referred to as the switch I and switch II loops, undergo significant
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Our study demonstrated that the
2019-11-30
Our study demonstrated that the sequential events of PKA and AMPK activation were involved in kinsenoside-mediated lipolysis. Within 1 h, PKA transiently inhibited AMPK activation by mitigating LKB1-mediated AMPK phosphorylation at Thr172, and PKA reduced AMPK-mediated phosphorylation at HSL-Ser565
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The aim of the present study was to
2019-11-30
The aim of the present study was to investigate the acute effects of THC on resting state Nodinitib-1 neurophysiology, and to examine the impact of COMT genotype on these effects. Thirty-nine healthy volunteers participated in a randomised, placebo-controlled, crossover pharmacological MRI study. A
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This structure guided the variation of the
2019-11-30
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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Compounds and possessed relatively low clogP
2019-11-30
Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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Methacholine MCh is a bronchoconstrictive agent that
2019-11-30
Methacholine (MCh) is a bronchoconstrictive agent that has been widely used in the diagnoses of airway narrowing and hyperresponsiveness (Jonasson et al., 2009). MCh induces muscle contractions by stimulating the muscarinic cholinergic receptors that are found in both the airways and the lung parenc
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Tailoring pharmacological treatment to the genetic backgroun
2019-11-30
Tailoring pharmacological treatment to the genetic background of a person can enhance therapeutic response (), increase compliance (), and decrease drug toxicity (, , ). Because cocaine addiction has a strong genetic basis, with the vulnerability to develop an addiction estimated to be as high as 72
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