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A single ICV injection of
2022-03-29
A single ICV injection of GALP stimulated food intake in goldfish at 1h post-administration. This result is similar to that observed in rats, where ICV injection of GALP exerted an acute orexigenic effect [14], [15], [16]. Simultaneously, our findings counter the results found in mice, where central
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br Acknowledgements This work was supported under the
2022-03-29
Acknowledgements This work was supported under the National Natural Science Foundation of China (Grant numbers 31200576, 21472197, 21675162), Beijing Natural Science Foundation (Grant No. 7182189), and Project supported by the Joint Funds of the National Natural Science Foundation of China (Grant
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tsa trichostatin receptor br Conflicts of interest br Acknow
2022-03-29
Conflicts of interest Acknowledgment Introduction The tsa trichostatin receptor growth factor receptors (FGFRs) are a family members of receptor tyrosine kinase (RTK) that represent attractive therapeutic targets for anti-cancer therapy gaining more and more attention in recent years [1],
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Two classes of histones demethylases
2022-03-28
Two classes of histones demethylases have thus far been identified: the Jumonji C (JmjC) domain-containing proteins and the amine oxidase domain (AOD)-containing proteins. They have distinct enzymatic mechanisms and substrate specificity. The JmjC domain is conserved through evolution and belongs to
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5-ht3 Recent studies have shown that
2022-03-28
Recent studies have shown that epigenetic modification is involved in neuropathic pain. For instance, peripheral noxious stimulation changes DNA methylation and histone modifications, which are related to pain hypersensitivity under chronic pain conditions [8]. Importantly, the epigenetic abnormalit
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Multi targeting agents are of major
2022-03-28
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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Although we showed that RBL
2022-03-28
Although we showed that RBL-2H3 Sc98 Iberiotoxin took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including SER
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However despite medicinal chemistry efforts lead
2022-03-28
However, despite medicinal chemistry efforts lead to considerable improvement in potency and selectivity of new HO-1 inhibitors, still have not identified inhibitors in the low nanomolar range. Therefore, due to the possible in vivo non-specific effects at high dosage, novel strategies should be de
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prostaglandin receptors However despite medicinal chemistry
2022-03-28
However, despite medicinal chemistry efforts lead to considerable improvement in potency and selectivity of new HO-1 inhibitors, still have not identified inhibitors in the low nanomolar range. Therefore, due to the possible in vivo non-specific effects at high dosage, novel strategies should be dev
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Several layers of regulation for this
2022-03-28
Several layers of regulation for this canonical activation of the HH pathway exist. First, the protein kinase A (PKA), the casein kinase 1α (CK1α) and GSK3β can phosphorylate and mark for proteosomal degradation the GLI transcription factors. [36] Second, Suppressor of Fused (SUFU) binds to GLI and
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Glutathione S transferases constitute a family
2022-03-28
Glutathione-S-transferases constitute a family of enzymes involved in the detoxification of xenobiotics, signalling cascades and serving as ligandins or/and catalyzing the conjugation of various chemicals and drugs [53]. The present finding indicates significant increase in GST activity in the brain
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A nitric oxide donor glyceryl trinitrite and the substrate f
2022-03-28
A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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The urinary levels of OHP
2022-03-28
The urinary levels of 1-OHP among the exposed workers were higher than those reported for a Brazilian group of charcoal workers (0.07 μmol mol creatinine) exposed to wood smoke (Kato et al., 2004), and for nonsmoking bus drivers (0.19 μmol mol creatinine) and nonsmoking mail carriers (0.11 μmol mol
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While the specific set of challenges associated with
2022-03-28
While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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metabolic enzymes A similar symbiotic relationship has been
2022-03-28
A similar symbiotic relationship has been reported in the brain, where increased gradients of lactate secreted by astrocytes enables neurons to import and use this nutrient, a process referred to the ‘neuron–astrocyte lactate shuttle’ [16]. Similarly, lactate-based metabolic coupling established by
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