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br Introduction The generic antifibrinolytic drug tranexamic
2022-04-08

Introduction The generic antifibrinolytic drug tranexamic VU590 hydrochloride (TXA) inhibits the protein-protein interaction between plasminogen and fibrin [9]. TXA is frequently used to reduce bleeding in various hemorrhagic conditions, such as during surgical procedures in the heart [19]. Howe
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In this study we find that DH CBD induces analgesic
2022-04-08

In this study, we find that DH-CBD induces analgesic effects on inflammatory but not acute pain and the hqn level of spinal α1 GlyRs increased after CFA paw injection. These results suggest that GlyR α1 is only involved in chronic pain. A possible explanation is that once the expression of α1 GlyRs
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Introduction Human pathogenic Leishmania protozoa comprise d
2022-04-08

Introduction Human pathogenic Leishmania protozoa comprise 20 different species that are distributed throughout the world and cause the disease leishmaniasis [1]. Transmission primarily occurs through the bite of a female sand fly and clinical manifestations of the disease span from cutaneous lesio
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Human GS is a multi
2022-04-07

Human GS is a multi-subunit complex consisting of four components: presenilin 1 (PS1), presenilin enhancer 2 (PEN-2), anterior pharynx-defective 1A (APH-1A) and nicastrin (NCT) (Fig. 1a) [5,6]. PS1 comprise nine transmembrane helices (TM 1–9) and contains the catalytic aspartate residues in its TM6
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Two types of processes intrinsic and
2022-04-07

Two types of processes, intrinsic and extrinsic, contribute synergistically to the age-related change on structural integrity and physiological function of the skin (Farage, Miller, Elsner, & Maibach, 2008). Intrinsic aging arise from genetically programmed cell aging, normal metabolic activities, a
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Conclusions br Author information The obtained models of com
2022-04-07

Conclusions Author information The obtained models of complexes of FPR2 with most of the described compounds are freely available at the author’s web site: http://www.biomodellab.eu/models/. Acknowledgements This work was partly done at the Interdisciplinary Centre for Mathematical and Compu
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So what makes a FFAR agonist different and
2022-04-07

So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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NMR analyses support the above statement Compound
2022-04-07

NMR analyses support the above statement. Compound 32 is an interesting example of an isosteric analog of compounds 12–14. It has been demonstrated that 32 forms a rather stable six-membered ring via a hydrogen bond based on the chemical shift of the phosphorus Pepstatin A at the C-3 position as ill
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The PI K AKT pathway is known
2022-04-07

The PI3K/AKT pathway is known to affect cell cycle, survival, and apoptosis (Yu et al., 2006; Park et al., 2008). After phosphorylation by AKT, the cytoplasmic apoptotic protein bad (bcl-xl/bcl-2) cannot be transferred to the mitochondria and dissociates from the inhibition protein bcl-2 and bcl-xl,
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Recent studies in our laboratory demonstrated that
2022-04-07

Recent studies in our laboratory demonstrated that several histamine H1 receptor antagonists induce apo A-I gene expression while histamine itself represses it [20]. In humans, there are three histamine receptor genes (H1, H2, and H3) that code for G-protein-coupled receptors (GPCR's) which bind his
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H R antagonism can prevent seizure development and improve
2022-04-07

H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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br Epigenetic regulation of OA
2022-04-07

Epigenetic regulation of OA pathogenesis Although epigenome of each cell is unique but can undergo temporal and spatial changes in response to environmental stimuli such as diet, exercise, smoking and disease status. Aberrant epigenetic modifications due to environmental factors are associated wi
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In this study we explore
2022-04-06

In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixed
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GPR co localizes with ghrelin in the duodenum
2022-04-06

GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1
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Dendritic damage and loss of synaptic connections correlate
2022-04-06

Dendritic damage and loss of synaptic connections correlate with cognitive decline in HAND patients. Synapse loss induced by HIV proteins occurs early and via a different signaling pathway from that leading to neuronal death (Kim et al., 2008), suggesting that synapse loss might be a mechanism to re
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