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Many investigators have noted structural similarities betwee
2021-11-10

Many investigators have noted structural similarities between certain flavonoids and benzodiazepines, such as diazepam, that are the most widely studied positive modulators of GABAA receptors. Benzodiazepines can act on these receptors via ‘two distinct and separable mechanisms’ (Walters, Hadley, Mo
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The PK profile and tissue distribution of
2021-11-10

The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an
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In a recent study Neelaveni
2021-11-10

In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported
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In this study we followed the fate of
2021-11-10

In this study, we followed the fate of Ag-specific CD8+ T L189 by directly visualizing them using MHC class I tetramers coupled with ovoalubumin (OVA)257–264 following EG.7 inoculation. We also examined the mechanism of apoptosis in exhausted Ag-specific CD8+ T cells during tumor immune response usi
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br Conflicts of interest br Funding This work
2021-11-10

Conflicts of interest Funding This work was supported by the Higher Education Commission Pakistan start-up research grant to Anjum Riaz. Introduction Distraction osteogenesis (DO) is an endogenous tissue engineering technology used to repair skeletal including craniofacial deformities, in
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br Acknowledgments I thank Takeshi Sakaba
2021-11-10

Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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Evidence suggests that phosphorylation increases synaptotagm
2021-11-10

Evidence suggests that phosphorylation increases synaptotagmin affinity for the SNARE complex [15], [128]. It is, however, unclear how this might affect release. Synaptotagmin has been identified as part of the minimal vesicle docking machinery in chromaffin c-Myc Peptide receptor [129]. Thus, phosp
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Another property shared between Hat p and Rtt p
2021-11-10

Another property shared between Hat1p and Rtt109p is a transient or substoichiometric interaction with Asf1p. Asf1p is necessary for the acetylation of histone H3 lysine 56 by Rtt109p. However, they do not appear to form a stable complex [22], [24], [27], [84], [90]. Surprisingly, the original type
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br Acknowledgment S A was supported by V Plan Propio
2021-11-10

Acknowledgment S.A was supported by V Plan Propio US-Acceso USE-14793-G. Introduction The Hippo signaling pathway is an evolutionarily conserved pathway that controls organ size and cell differentiation across diverse organisms through the regulation of cell proliferation and apoptosis (Di Ca
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The transcription factor Nrf is a master regulator of cytopr
2021-11-09

The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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Over the last years numerous studies gave insights
2021-11-09

Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137
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While the specific set of challenges
2021-11-09

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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To characterize the basic functions of
2021-11-09

To characterize the basic functions of GPR84 in phagocytes, we have utilized the receptor selective antagonist GLPG1205 (a small selective antagonist of GPR84 developed by Galapagos NV [14]) together with ZQ16 (2-(hexylthio) pyrimidine-4,6-diol), a potent GPR84 selective agonist identified in a high
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The opposite modulation observed for circulating LPI levels
2021-11-09

The opposite modulation observed for circulating LPI levels and WAT GPR55 kainic acid by nutritional status suggests that increased levels of LPI may down-regulate the expression of its receptor in WAT, whereas in conditions of low serum LPI levels, the expression of GPR55 is stimulated. However, d
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IC is a rat mAb
2021-11-09

IC2 is a rat mAb specifically binding to insulin granula [127,128]. Although this mAb was discovered 30 years ago, it has only recently been used for β-cell imaging in vivo. Moore et al. used this mAb for β-cell imaging in 2001 [129]. After DTPA conjugation, IC2 was labeled with 111In. Both in vitro
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