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Various compounds have been designed to inhibit
2024-05-18

Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic Stiripentol moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a p
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br Regulation of AHR Activity AHR activity is
2024-05-18

Regulation of AHR Activity AHR activity is regulated in various ways. First, AHR protein levels are controlled via ubiquitin-mediated proteosomal degradation: Ligand binding induces AHR ubiquitination and subsequent degradation by the proteasome [5]. AIP, a component of the AHR chaperone complex,
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br Impact of global AHR deficiency on diet induced obesity
2024-05-18

Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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RGFP966 Since non lipoprotein derived free
2024-05-18

Since non-lipoprotein-derived free cholesterol is recycled from the plasma membrane through the endosomal system through receptor-independent mechanisms, we wanted to determine whether ABCA2 could alter the trafficking of this source of free cholesterol. Our approach was to measure the effect of mob
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Circulating adrenal derived stress hormones epinephrine
2024-05-18

Circulating adrenal-derived stress hormones, epinephrine and corticosterone mediate their tissue effects through adrenergic (AR; α and β) and glucocorticoid (GR) receptors. AR are widely distributed throughout the body and although epinephrine is a prototypical agonist for all types of AR, the selec
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These results from the present study are summarized in
2024-05-18

These results from the present study are summarized in Table 1. Eight drugs (doxorubicin, epirubicin, daunorubicin, idarubicin, irinotecan, imatinib, sunitinib and gefitinib) inhibited 5-HT-induced 5-HT3A and 5-HT3AB currents; three (irinotecan, topotecan and mitoxantrone) showed different responses
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AP26113 mg Application of the broad acting HTR antagonist
2024-05-18

Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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histone methyltransferase inhibitor Adenosine receptors are
2024-05-18

Adenosine receptors are proposed to play proangiogenic role in vascular and immune histone methyltransferase inhibitor within microenvironment of hypoxic tissues to maintain tissue oxygenation in chronic ischemic condition [9]. Adenosine also stimulates the production of angiopoetin-1, VEGF and Int
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Introduction Pyometra is relatively common
2024-05-18

Introduction Pyometra is relatively common in intact bitches and its diagnosis is aided by ultrasonography (Bigliardi et al., 2004), along with measurement of acute phase proteins and leucocyte (white blood cell, WBC) counts; assessment of these parameters during recovery may be helpful for monito
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br Materials and methods br
2024-05-18

Materials and methods Results Discussion The data presented here demonstrate the important role of B lymphocyte-expressed α7 nAChRs in regulating the antibody immune response. It is shown that, in addition to ACh produced by activated T lymphocytes (Fujii et al., 2012), activated B lymphocy
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The next level of possible correlation
2024-05-18

The next level of possible correlation and comparison between the α7 and 5HT3 receptors is at the subunit arrangement and protein folding. Crystal structures of the nicotinic and serotoninergic Pasireotide receptors [45], [46] reinforced the concept of similarities between these families of receptor
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akt pathway Bioactive peptides contain amino acids
2024-05-18

Bioactive peptides contain 2–20 amino acids with possible bioactivities including antihypertensive, antioxidant, antimicrobial, anticancer, and opioid activity [9], [10], [11]. There has been a great interest in antihypertensive peptides for their efficiency in lowering blood pressure. The antihyper
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br Author contributions br Conflict of interest br Acknowled
2024-05-18

Author contributions Conflict of interest Acknowledgements This work was supported by the National Natural Science Foundation of China (81502276), Major Projects of Science and Technology of Health and Family Planning Commission of Hunan Province (A2017013), the Natural Science Foundation o
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Ryoichi et al modified potent clinical candidate
2024-05-18

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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br Acknowledgements M M M is the William Dow
2024-05-18

Acknowledgements M.M.M. is the William Dow Lovett Professor of Neurology and is supported by grants from the Michael J. Fox Foundation for Parkinson's Research, the American Parkinson Disease Association, the New Jersey Health Foundation/Nicholson Foundation, and by the National Institutes of Hea
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