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Pharmacological inhibition of PKR seems
2021-12-21

Pharmacological inhibition of PKR seems to be an interesting strategy for revealing the role of PKR in oxytosis and ferroptosis. The oxindole/imidazole derivative C16 was identified by screening a library of 26 different ATP-binding site-directed inhibitors of varying structure that is more selectiv
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Similar to in vitro data in vivo studies have also
2021-12-21

Similar to in vitro data, in vivo studies have also revealed modulation of TLR4-induced inflammatory responses by AEA. The proposed AEA reuptake inhibitor AM404 has been shown to attenuate TLR4-induced increases in plasma levels of IL-6 and IL-1β, the latter effect mediated by CB1 receptor activatio
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br Results br Discussion In this study six new
2021-12-20

Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of Rofecoxib synthesis unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations i
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The even bigger surprise was the second feature of both
2021-12-20

The even bigger surprise was the second feature of both structures. Interestingly, binding of the MRG domain hardly altered the conformation of the SET domain compared with its apo state (An et al., 2011). What did change, however, is the conformation of the ASH1L auto-inhibitory loop (Figure 1). D
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SCH is a H R receptor antagonist
2021-12-20

SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese
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It has been reported that
2021-12-20

It has been reported that expression of murine haspin is found only in post-meiotic spermatids and that overexpression of murine haspin in HEK-293 cells leads to reduced cell proliferation. Therefore, it was suggested that haspin functions to bring about BCECF-AM arrest in haploid germ cells (Tanaka
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br Introduction Soluble guanylyl cyclase GC maintains vascul
2021-12-20

Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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The ketone body receptor HCA
2021-12-20

The ketone body receptor HCA2 is most likely not active under normal conditions, since local levels and plasma levels of ketone bodies such as β-HB are too low to activate the receptor. However, overnight fasting or prolonged starvation results in plasma levels of the ketone body in the millimolar r
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The results of our study indicate the
2021-12-20

The results of our study indicate the general importance of the gp120 V3 loop 5'-Iodoresiniferatoxin patch in the subunit association of primate immunodeficiency virus Env trimers. Our observation that the stem insertion mutants and hydrophobic patch mutants exhibit similar phenotypes with respect
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Attempting to further elucidate the
2021-12-20

Attempting to further elucidate the role of i thought about this and activation of the Gcgr without the influence of GLP-1, we used DT-Gcg mice with acute knockdown of all proglucagon products. This mouse model has previously been shown previously to have a normal total islet area as well as β cell
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br Fipronil resistance associated with A
2021-12-20

Fipronil resistance associated with A2′S and A2′G mutations Fipronil is a second-generation NCA (Fig. 1), and A2′S and A2′G mutations provide a low level of cross-resistance to fipronil (Cole et al., 1995, Gao et al., 2007). As shown in Table 1, the A2′S Veliparib mg confers high resistance to d
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br Experimental br Acknowledgments br
2021-12-20

Experimental Acknowledgments Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS), and without treatment results in a debilitating disease that cripples the immune system of the patient, increasing susceptibility to opportunistic diseases
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Accumulating evidence suggests an important role for endothe
2021-12-20

Accumulating evidence suggests an important role for endothelin ETB receptors in renal homeostasis. ETB receptors promote vasodilation, natriuresis, and diuresis (Davenport and Maguire, 2011) and maintain renal perfusion via counterbalancing the effects of vasoconstrictors and regulation of water re
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br Retrieval requires histamine H
2021-12-20

Retrieval requires histamine H1 receptors in dorsal hippocampus Retrieval is a dynamic process that requires neurotransmitter regulation (Barros et al., 2000, Barros et al., 2001). Recently, histamine, and histaminergic transmission has entered the list of putative neurotransmitter modulators of
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Here we examine the impact of
2021-12-20

Here we examine the impact of hypoxia on lake whitefish (Coregonus clupeaformis) during embryonic and larval development. Lake whitefish are a cold-water salmonid endemic to North America and are found from western Alaska, USA to eastern Labrador in Canada. Spawning occurs from late autumn to early
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