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Molecular dynamics studies have proved an effective means of
2021-11-02

Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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In conclusion we demonstrated that the atypical
2021-11-02

In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 how to calculate mmol results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network act
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The dorsal horn of the spinal cord shows a high
2021-11-02

The dorsal horn of the spinal cord shows a high density of Ca2+-permeable AMPA receptors, particularly in the superficial spinal laminae (laminae I and II), where primary afferents carrying nociceptive and thermoreceptive inputs terminate and synapse on spinal second-order neurons (Engelman et al.,
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The main aim of our study was to identify whether
2021-11-02

The main aim of our study was to identify whether glucokinase and Irs2 were required for beta cell replication induced by short-term HF diet feeding. Glucokinase plays a critical role in regulating blood glucose levels by catalysing the rate-limiting biochemical reaction of glycolysis [26,27]. In pa
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The manner in which various residue
2021-11-02

The manner in which various residue side chains are oriented in the active site of HsHxKIV was a driving factor for why glucosamine analogues could not bind, as we previously proposed [16]. These compounds would have difficulty managing access into the active site based on residue P153 in addition t
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Newt GHS R a proteins expressed in a mammalian cell
2021-11-02

Newt GHS-R1a proteins expressed in a mammalian cell were able to bind homologous newt ghrelin, heterologous rat and bullfrog ghrelin, and a peptidyl GHS-R1a agonist, GHSRP-6, with inducing intracellular Ca signaling. This indicates that the identified cDNA encodes the ghrelin receptor from a view of
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br Results and discussion br Conclusion In conclusion twenty
2021-11-02

Results and discussion Conclusion In conclusion, twenty-one 4-monocyclic aryl-5-carbamoyl-3-isoxazolols have been synthesized and evaluated for their antagonistic activities against housefly and common cutworm GABARs expressed in Xenopus oocytes. The TEVC results indicated that Latrunculin B
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Recently the classical view of the compartmentalization of
2021-11-02

Recently, the classical view of the compartmentalization of the plant isoprenoid metabolism has been re-evaluated, following the demonstration of the partial peroxisomal localization of the mevalonic Metabolism Compound Library (MVA) pathway, generally regarded as cytosolic. Using GFP-tagging approa
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LMWHs are currently recommended for the treatment of
2021-11-02

LMWHs are currently recommended for the treatment of VTE in patients with cancer. Compared to vitamin K antagonists, LMWHs are more effective in reducing the risk of recurrent VTE without increasing the risk of bleeding [13]. However, a post hoc analysis of this Bestatin hydrochloride receptor previ
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br Acknowledgment br Introduction Non steroidal
2021-11-01

Acknowledgment Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are widely utilized to treat pain and inflammation [1], but their chronic use is hindered by a variety of potentially serious adverse events that include gastrointestinal (GI) mucosal lesions, bleeding and perforations
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Introduction Histamine Imidazolyl ethylamine is an important
2021-11-01

Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric b12 500 mg secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamine exert
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br STAR Methods br Author Contributions
2021-11-01

STAR★Methods Author Contributions Introduction Hyaluronan, a major constituent of the extracellular matrix (ECM), is produced by hyaluronan synthases (HASs) and degraded by hyaluronidases (HYALs) (Vigetti et al., 2014). Physiologically, hyaluronan exists in a form with a molecular weight of
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The fact that GSK recognition of its substrate involves
2021-11-01

The fact that GSK-3 recognition of its substrate involves pre-phosphorylation supports the rational for using synthetic phosphorylated peptides as substrate competitive inhibitors [57]. Phosphorylated peptides derived from the N-terminal pseudosubstrate sequence of GSK-3β were very weak inhibitors o
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TNF-alpha, recombinant human protein br Conclusion In this r
2021-11-01

Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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Recently we suggested that KYNA an
2021-11-01

Recently, we suggested that KYNA – an endogenous GPR35 agonist could be produced in a human cornea since we showed the presence of the enzymes that catalyze the synthesis of KYNA – kynurenine aminotransferases I-III in corneal epithelium, stroma and endothelium (). Therefore, these findings provided
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