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A linker length of and atoms was found
2021-09-24

A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and d
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Wasting syndrome is a common complication of HIV infection a
2021-09-24

Wasting syndrome is a common complication of HIV infection and is marked by progressive weight loss and weakness, often associated with fever (Weinroth et al., 1995). Fever is a highly complex process initiated by the action on the pop over to this site thermosensitive cells of a number of endogenou
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Ki8751 Xie et al b reported
2021-09-24

Xie et al. (2009b) reported that the combination of diagnostic ultrasound impulses and cyclic RGD-bearing MBs targeted for GP IIb/IIIa resulted in the successful recovery of epicardial and microvascular blood flow in swine models with acute thrombotic occlusion. It is well known that the stability o
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Much less is known about the and subunits GlyR subunit
2021-09-24

Much less is known about the α3 and α4 subunits. GlyR α3 subunit immunoreactive synapses are concentrated in discrete bands across the IPL; besides, bipolar, amacrine and ganglion cells have been suggested to express it (Haverkamp et al., 2003, Wässle et al., 2009). In fact, All amacrine express α3β
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Glutamate is a ubiquitous principal excitatory neurotransmit
2021-09-24

Glutamate is a ubiquitous principal excitatory neurotransmitter in the 6 mercaptopurine synthesis that plays a central role in a variety of brain functions (Delgado, 2013, Hawkins, 2009). Several studies reported that CSF glutamate was associated with mental illness, including major depressive diso
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The mechanism underlying the anorectic effect of OXM is
2021-09-24

The mechanism underlying the anorectic effect of OXM is well established. It is centrally mediated via GLP-1 receptor activation, confirmed by both pharmacological blockade of the GLP-1 receptor, and using GLP-1 receptor knock-out mice [2], [11], [12]. However, the mechanism by which it increases en
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br Acknowledgements Funding for this study
2021-09-24

Acknowledgements Funding for this study is gratefully acknowledged from the Department of Employment and Learning (QC) and the Northern Ireland Chest Heart and Stroke Association (2008107). Introduction Preeclampsia is a major human pregnancy-specific disorder that occurs in at least 5–10% of
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In the CNS histamine is known to regulate sleep and
2021-09-24

In the CNS, AZD 8055 is known to regulate sleep and wakefulness, learning and memory, feeding, and energy. Here, we address its actions in relation to CNS disorders, and emphasize potential clinical applications of histamine receptor ligands (Table 1). In addition, as the effect of histamine on neu
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The HIF complex was initially identified as an
2021-09-23

The HIF complex was initially identified as an important component of the cell machinery involved in the response and Salicylic acid receptor to hypoxia (Semenza, 2001). Further studies have shown that HIF can also modulate whole-body energy homeostasis by controlling hypothalamic neurons (Varela et
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In conclusion studies of the regulation of
2021-09-23

In conclusion, studies of the regulation of the HO-1/BVR/CO pathway by selective pharmacological approaches may lead to the discovery of novel compounds for the treatment of diverse diseases. Recent results validate the use of advances in targeting HO-1 in various vascular diseases. However, there a
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Recently IL was also identified
2021-09-23

Recently, IL-10 was also identified as an important mediator of collagen deposition in the development of HF [64,65]. It was shown, that this cytokine activates macrophages found in the hearts of mice suffering from diastolic dysfunction in the autocrine manner [64]. In response, specific subset of
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br Substrate Interactions Outside of the Catalytic Cleft
2021-09-23

Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use
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The biological function of NPRA is demonstrated
2021-09-23

The biological function of NPRA is demonstrated primarily through the ANP/BNP-dependent GC catalytic activity of the receptor and the production of cGMP, which is regulated by several factors, including hormones, growth factors, physiological milieu, and the ligand itself [26,34,[36], [37], [38], [3
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Another interesting approach is to use partial agonists as s
2021-09-23

Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain
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Over the last few years experimental
2021-09-23

Over the last few years, experimental evidence for the involvement of Epac1 in cancer progression is beginning to emerge (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). For example in melanoma cells, silencing of Epac1 attenuates
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