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Generally glycines and other small residues such
2021-06-25

Generally, glycines (and other small residues such as alanine) present in a helical GxxxG-motif that are facing the same side of the helix form a uniform surface that enables direct contact with a second helix. Crystal structures of multipass membrane proteins have demonstrated that GxxxG-motifs are
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172 5 receptor The field of synthetic cytokine biology conti
2021-06-24

The field of synthetic cytokine biology continues to grow through molecular, physiological and pathophysiological insights, as well as via new methodical advances. The approval of chimeric antigen receptor (CAR) T cell immunotherapy by the US Food and Drug administration (FDA) in August 2017 for rel
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Henderson et al reported that allergen induced airway
2021-06-24

Henderson et al. [20] reported that allergen-induced airway remodeling was blocked by the CysLT1 receptor antagonist montelukast. The development of epithelial thickening and mucus accumulation at relatively small quetiapine mechanism of action receptor was also suppressed by montelukast. The CysLT2
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br Role of CRF receptors in
2021-06-24

Role of CRF1 receptors in the BNST in stress-induced relapse to cocaine seeking The seminal work of Stewart and co-workers [19] showed that rats that have extinguished their auto-administration of different drugs of abuse relapse to drug-seeking behaviour when exposed to footshock, even after a 4
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In the present study we investigated the
2021-06-24

In the present study, we investigated the role played by CRF1 and CRF2 receptors located within the mouse PAG on the anxiogenic and antinociceptive effects produced by local infusion of CRF. To block CRF receptors, we used the selective CRF1 and CRF2 PPADS tetrasodium salt australia antagonists, re
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Dopamine activity in the PFC and striatum may be
2021-06-24

Dopamine activity in the PFC and striatum may be antagonistic, meaning that lower levels of dopamine in the striatum tend to correspond to higher levels of dopamine in the PFC and vice versa (Cools and D'Esposito, 2011; Tunbridge et al., 2006). Human PET studies have reported that dopaminergic PFC f
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It would be very useful if unphosphorylated CK
2021-06-24

It would be very useful if unphosphorylated CK1s could be prepared using an E. coli expression system without the troublesome in vitro phosphatase treatment. So far, it has been shown that coexpressed λPPase, a Mn2+-dependent protein phosphatase that can dephosphorylate phospho-Ser/Thr/Tyr [20,21],
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br Results and discussion br Conclusion In
2021-06-24

Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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The modes of action of
2021-06-24

The modes of action of insecticides are classified by the Insecticide Resistance Action Committee (IRAC) [6]. In this classification, a large proportion of insecticides are categorized as nerve- and muscle-targeting insecticides, which encompass GABACl antagonists (Group 2) and GluCl allosteric modu
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Interestingly selective ETA blockade increased cutaneous blo
2021-06-24

Interestingly, selective ETA blockade increased cutaneous blood flow as measured by laser Doppler fluxmetry. This is a measure of total blood flow in the different vessels in the skin including venules, ephrin receptor as well as arterioles. This finding is in accordance with the previous demonstra
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We hypothesize that both IGF dependent kinase activation and
2021-06-24

We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal G-15 in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for these studies because IGF-1-
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Brg is a core unit of BAF
2021-06-24

Brg1 is a core unit of BAF complex and is required for the self-renewal and pluripotency of ESCs (Ho and Crabtree, 2010). We confirmed the interaction of DPF2 and BRG1 by immunoprecipitation and showed that these proteins extensively co-localize in the genome. Although both Brg1 and Dpf2 positively
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PDK1 inhibitor In this paper we focused
2021-06-24

In this paper, we focused on Ewing sarcoma (ES), a rapidly growing, highly malignant bone tumor developing metastases in the vast majority of patients unless multiagent chemotherapy is applied [16]. ES is the second most frequent bone tumor in childhood and adolescence, and is characterized by the p
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ep4 receptor br Conclusion Our study demonstrates that the e
2021-06-24

Conclusion Our study demonstrates that the effects of Epac activation are strongly conditioned by the steady-state Ca levels at which the myocyte is functioning. As intracellular Ca increases, the activity of CaMKII enhances and the phosphorylation of its SR substrates acquires different relevanc
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The effect of transformation of the linker
2021-06-24

The effect of transformation of the linker Y between the carboxylic ret proto oncogene residue and the phenyl moiety of 2b was also investigated, and is illustrated in Table 5. Analogs 2b, 16, and 17, possessing conformationally restricted carboxylic acid residues, tended to show stronger antagonist
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