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In this review we will present the traditional
2023-10-11

In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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However most of these SBVS studies
2023-10-11

However, most of these SBVS studies were focused on the target(s) for which crystal structures were available or have a similar template in PDB for comparative modeling. Besides, these were limited to SBVS only which relies on the rigid binding pocket, therefore, it may result in high false positive
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Thymoquinone TQ is the major active compound derived from
2023-10-11

Thymoquinone (TQ) is the major active myc pathway derived from Nigella sativa (Woo et al., 2012). Recent animal studies support the potential of TQ for the treatment of a variety of inflammatory disorders like inflammatory bowel disease (IBD), RA, and osteoarthritis (OA) (Salem, 2005, Badr et al.,
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Cyclophosphamide receptor Gene regulation of MMPs is influen
2023-10-11

Gene regulation of MMPs is influenced by the transcription factor activating factor-1 (AP-1). AP-1 complexes are heterodimers of proteins of the two proto-oncogene families (jun and fos) and have Cyclophosphamide receptor in the promoter region of MMPs, as well as in genes mediating inflammatory re
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Most human diseases e g cancer
2023-10-11

Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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In AD and possibly other forms of dementia it
2023-10-11

In AD, and possibly other forms of dementia, it has been suggested that tau mislocalization to dendritic spines anticipates neurodegeneration [48]. Accumulation of hyperphosphorylated tau in dendritic spies would cause a derangement of synaptic function, thereby impairing excitatory synaptic transmi
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br Conclusion br Introduction The identification of
2023-10-11

Conclusion Introduction The identification of Alzheimer's disease (AD) biomarkers and their ability to measure pathology antemortem has led to a fundamental reconsideration of the pathogenesis of AD. The importance of biomarkers was already reflected in revised diagnostic criteria proposed by
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Cells have developed strategies aiming
2023-10-11

Cells have developed strategies aiming to enhance both the efficiency of proteins with chaperone activity as well as their overall antioxidant capacity to maintain proteostasis under oxidative stress conditions (Miyata et al., 2012). For instance, 2-Cys peroxiredoxin is an abundantly expressed, anti
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Aberrant or a sustained activation
2023-10-11

Aberrant or a sustained activation of AhR signaling pathway, triggered by exogenous toxic ligands such as dioxins, PAHs or polychlorinated biphenyls (PCBs), is a well-described biological process engaged during tumor initiation and/or promotion in various tissues (e.g. liver, lung, skin)(reviewed in
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br Conclusion The HT receptor
2023-10-11

Conclusion The 5-HT receptor family is complex, and one may ask as does Bryan Roth et al. [205] whether this is useless Auranofin (i.e. too much redundancy) or an embarrassment of the riches (i.e. many potential targets to choose from to affect normal or pathological function); molecular biology
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HT modulates cortical and hippocampal
2023-10-11

5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal Bay 65-1942 HCl salt as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser
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Previous work established interactions between CRF and KOR s
2023-10-11

Previous work established interactions between CRF and KOR systems in regulating attention (39). The CRF antagonist ANT attenuated, but did not completely reverse, the effects of PACAP (.5 µg) and did not have any effects on its own (Table 2). There were no significant differences in performance amo
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Mast cells Mast cells are immune cells of
2023-10-11

Mast cells. Mast Capsazepine are immune cells of the myeloid lineage and are ubiquitously present in connective tissues [75]. These cells are involved in the modulation of a number of physiological functions, such as vasodilation, angiogenesis, bacterial, and parasite elimination [75]. Moreover, ma
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The same applies also to intermediate formally obtained
2023-10-11

The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char
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It is worth pointing out that phenotypes of
2023-10-11

It is worth pointing out that phenotypes of in vivo HSP90β inhibition were not identical to those observed in rapsyn mutant mice (Gautam et al., 1995). Postsynaptically, junctional AChR clusters appeared fragmented, in addition to expected reduction in AChR intensity, in muscles injected with 17-AAG
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