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br Mutagenesis and Receptor Modeling Studies
2021-12-22

Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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br Conclusions Beta cell specific
2021-12-22

Conclusions Beta cell-specific expression in human islets of DGCR2, GBF1, GPR44 and SerpinB10 has not previously been described, although the proteins have partly been characterized in other contexts not related to beta the full report or diabetes. DGCR2, GPR44 and SerpinB10 were negative in all
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Acknowledgments Financial support from the National Natural
2021-12-22

Acknowledgments Financial support from the National Natural Science Foundation of China (81730094, 81473262 and 81573299) is gratefully acknowledged. This project was also supported by the “111 Project” from the Ministry of Education of China, the State Administration of Foreign Expert Affairs of C
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The cytoprotective effects of glyRs have
2021-12-22

The cytoprotective effects of glyRs have been reported to associate with the MAPK (JNK, ERK1/2 and p38) signaling pathways [47], [48]. The present study reveals that suppressive phosphorylation of cRaf-MEK1/2-ERK1/2 is initiated by glycine – glyR α2 interactions in cardiomyocytes. As a central regul
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cal a br Materials and Methods br Results br Discussion
2021-12-22

Materials and Methods Results Discussion A model of seizure and excitotoxicity induced by neonatal MSG administration was described recently (19) in which extracellular glutamate increased after the first and second MSG administrations were observed, the greatest increase seen following the
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protein kinase g br Acknowledgements br Introduction Benzodi
2021-12-22

Acknowledgements Introduction Benzodiazepine (BZ) treatment is widely used for quick and efficient anxiolytic and sedative responses. However, when the use is extended to longer periods, adverse effects emerge. These include tolerance to the initial drug effect, dependence as revealed by withd
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The presence of ghrelin s
2021-12-22

The presence of ghrelin's mRNA in the eye and the presence of ghrelin in the aqueous humor, along with a decrease of its levels in glaucoma, suggest a local role for this peptide in the ocular tissue [8], [16], [18]. There is no available data regarding the presence of GHSR-1 in the anterior segment
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So far only few studies report about GAL
2021-12-22

So far only few studies report about GAL in the visual system: GAL has been detected in the cornea of rat (Jones and Marfurt, 1998), mouse (Henken and Martin, 1992) and pig (Stone et al., 1988), and in the uvea of rat (Strömberg et al., 1987), pig (Stone et al., 1988) and cat (Grimes et al., 1994),
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VS strategies have been building momentum in G drug discover
2021-12-22

VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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The typical pharmacophore for GPR agonists
2021-12-22

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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AZD-5438 As a part of our
2021-12-22

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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SETDB is ubiquitously expressed in mouse tissues and more th
2021-12-21

SETDB1 is ubiquitously expressed in mouse tissues, and more than 900,000 ERVs are dispersed through the mouse genome. Nevertheless, the repertoire of ERVs under the control of SETDB1 was limited and highly cell-type specific. Only 17,349 ERVs were associated with H3K9me3 domains in Th2 cells. The va
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The mast cell has long been recognized as central
2021-12-21

The mast cell has long been recognized as central to the mediation of allergic responses not least because it is the principal repository of histamine in the body. Following activation by allergens, the mast cell can release histamine as well as generate a host of additional mediators such as cystei
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The site of metastasis in breast cancer often contributes
2021-12-21

The site of metastasis in breast cancer often contributes to the patient’s OS. Patients with bone metastasis from their breast cancer often have a notably increased survival over patients with visceral or AR-M 1896 sale metastasis. In this analysis, ER+/HER2+ patients were noted to have a higher ra
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In first wave first generation drugs
2021-12-21

In 2013, first-wave, first-generation drugs telaprevir and boceprevir was the first protease inhibitors (PIs) incorporated in Brazilian Clinical Guidelines for the treatment of patients infected with HCV AZD2932 1. Based on this 2013 Clinical Guideline, telaprevir could be used for both naïve and e
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