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Using embelin and its analogs as surrogate GPR agonists
2021-09-15

Using embelin and its analogs as surrogate GPR84 agonists we discovered that GPR84 couples to G12 and G13 signaling pathways in addition to Gi, linking receptor function to Rho/Rac signaling and modulation of the cytoskeleton. In primary human macrophages, GPR84 activation leads to Gβγ signaling, Er
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The first described synthetic FFA active
2021-09-15

The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was
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Because of the commercial availability of some acetamide phe
2021-09-14

Because of the commercial availability of some acetamide phenol starting materials, a few acetamide final products (such as and , ) were directly synthesized via a Mitsunobu reaction with chloropyrimidine piperidinyl cyclopropyl alcohol . The 3-pyridinyl analogue was synthesized by a nucleophilic
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FPG had no consistent activity in reducing
2021-09-14

FPG-2 had no consistent activity in reducing G→T transversions. Gao and Murphy [2] earlier reported that FPG-2 had a limited amount of activity in vitro on depurinated, UV-treated, and methylene-blue-treated DNA (but not on 8-oxo-G-containing oligonucleotides). FPG-2 contains the N-terminal domain a
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In general fish has a limited ability for
2021-09-14

In general, fish has a limited ability for digestion and metabolism of carbohydrate though carbohydrate is the cheapest dietary energy and carbon source to animals and the best candidate for replacing dietary protein (Enes et al., 2009, Kamalam et al., 2017, Wilson, 1994). Furthermore, the analysis
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A number of models have been proposed in order to
2021-09-14

A number of models have been proposed in order to explain the mechanisms of protein transport through nuclear pore complexes. One theory is that the transport is mediated by specific peptide signals known as NLSs. The classical NLSs are short sequences containing a high proportion of the positively
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br Glucocorticosteroid receptor structure and function The g
2021-09-14

Glucocorticosteroid receptor structure and function The gene encoding for the human GR is composed of 9 exons (Oakley and Cidlowski, 2011) and the translated protein is described as having 4 functional regions. The protein contains a highly conserved central DNA-binding domain (DBD) or C-domain,
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Galanin was shown to play
2021-09-14

Galanin was shown to play an important role in pain and pain processing [14] and the involvement of neuropeptides in the development of migraine is well established [[24], [25], [26]], however, so far it has not been examined whether systemic galanin levels correlate with migraine. Therefore, we use
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MTEP hydrochloride receptor br The potential of EPA Ffar
2021-09-14

The potential of EPA-Ffar4 signaling as a novel intervention for HFpEF Conclusions and future directions Optimization of ω3-PUFA/EPA-therapy based upon titration to achieve therapeutic levels: A pressing clinical challenge is to continue to define the benefit of ω3-PUFA/EPA-therapy. Recent ana
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Corresponding to the different insulinotropic signaling the
2021-09-14

Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct 543 mg on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full agonists
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Introduction Vesicular exocytosis an intracellular membrane
2021-09-14

Introduction Vesicular exocytosis, an intracellular membrane trafficking pathway, is a ubiquitous process for intercellular communication. It occurs when an intracellular vesicle fuses with the cell membrane and subsequently releases an infinitely minute number of chemical or biochemical messengers
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Sometime ago we have described diamino triazines as histamin
2021-09-14

Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by CBiPES hydrochloride receptor and zymosan. In this work w
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A complimentary approach with Per
2021-09-14

A complimentary approach with Per2:Luc BIO-acetoxime exposed to hypoxia as well as with mBmal1:Luc circadian reporter cells in which we overexpressed variants of HIF-1α and HIF-2α revealed that hypoxia and HIFs can not only shorten the period but also decrease the amplitude of the clock (Figures 2
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A complimentary approach with Per
2021-09-14

A complimentary approach with Per2:Luc BIO-acetoxime exposed to hypoxia as well as with mBmal1:Luc circadian reporter cells in which we overexpressed variants of HIF-1α and HIF-2α revealed that hypoxia and HIFs can not only shorten the period but also decrease the amplitude of the clock (Figures 2
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Introduction As a compound class histone deacetylase inhibit
2021-09-14

Introduction As a compound class, histone deacetylase inhibitors (HDIs) have been remarkably successful in the treatment of T-cell lymphoma [1]. Vorinostat (suberanilohydroxamic UK-5099 or SAHA) was approved by the FDA in 2006 for the treatment of cutaneous T-cell lymphoma [2], [3]; romidepsin (RD
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