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While published data around the functional significance
2021-11-18

While published data around the functional significance of GPR84 are quite sparse, details of signaling pathways initiated by the receptor are even more limited, including in recombinant systems. In recombinant cells, GPR84 activation reportedly leads to Gi pathway activation, resulting in pertussis
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Several studies have sought a cross
2021-11-18

Several studies have sought a cross-relationship between commensal bacteria-derived metabolites and the Gprs (Blad et al., 2012). Gpr81 is expressed primarily in adipocytes, and hence, lactate-Gpr81 interaction inhibits lipolysis (Cai et al., 2008, Liu et al., 2009). Lactate reduced inflammation by
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There is abundant literature about
2021-11-18

There is abundant literature about different functional aspects of the cannabinoid system (Badal et al., 2017, Balenga et al., 2011, Henderson-Redmond et al., 2016, Nair et al., 2015); however, not a great deal is known about the mechanism by which ethanol impacts its function in connection to the i
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A motivation for this study is the ability
2021-11-18

A motivation for this study is the ability of PGD2 to inhibit hair lengthening (). Here we demonstrate that PGD2 also inhibits hair regeneration after wounding. Thus, PGD2 and Gpr44 inhibition of the hair follicle occurs in multiple contexts and may be exploited in future therapies. Pharmaceutical c
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As part of our discovery efforts
2021-11-17

As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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We first investigated the influence of the acyl
2021-11-17

We first investigated the influence of the -acyl group of the glycine amide side chain and found that shorter linkers lead to better activities (–); simple -benzoyl substituents were always superior to the 3-arylpropanoyl group present in the high-throughput hit (). Electron withdrawing substituents
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br Material and methods br Results br Discussion Accumulatin
2021-11-17

Material and methods Results Discussion Accumulating evidence suggests that the hippocampus is sensitive to noise-induced hearing loss and other forms of sensory deprivation, which deprives the hippocampus of sensory information required for its normal operations such as spatial navigation
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As early as glucagon was shown
2021-11-17

As early as 1957, glucagon was shown to increase Ouabain expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [27]. This con
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In the present study five Glu substituted analogues of
2021-11-17

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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br Galanin in depression A major impediment in depression
2021-11-17

Galanin in depression A major impediment in depression research is the lack of validated animals´ models. Animals not only lack consciousness of self, self-reflection and consideration of others but also hallmarks of the disorder such as depressed mood, low self-esteem or suicidal intent are hard
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EPZ031686 In skeletal as well as in the heart muscle
2021-11-17

In skeletal as well as in the EPZ031686 muscle, the same FBPase isozyme is present (Gizak and Dzugaj, 2003). On the other hand, different isoforms of 6-fructo-2 kinase/fructose-2,6-bisphosphatase (FBPase-2/PFK-2) have been discovered in muscle fibres and cardiomyocytes (Okar et al., 2001, Marsin et
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A second H R antagonist
2021-11-17

A second H3R antagonist with benzamide-based structure from Johnson & Johnson is JNJ-31001074, known as Bavisant and under chemical IUPAC name of (4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone. It is a compound with molecular weight 329.44, HBA four, and MLogP 1.52 encompass
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br Conflict of interest br Funding This work
2021-11-17

Conflict of interest Funding This work was supported by the National Institutes of Health MSK Cancer Center Support Grant/Core Grant [P30 CA008748]. The funding source had no involvement in the study design; in the collection, analysis and interpretation of data; in the writing of the report;
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While a role for YAP TAZ signaling in oligodendrocytes
2021-11-16

While a role for YAP/TAZ signaling in oligodendrocytes has not been described, these iso 1 receptor are also responsive to mechanical stimuli. OPC proliferation and migration can be altered by plating on substrates of varying stiffness [20], resulting in differentiation in a density-dependent manne
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Introduction Cancer is known as a renegade system of expansi
2021-11-16

Introduction Cancer is known as a renegade system of expansion that initiate in human body. It is distinguished, in spite of its category, by one universal characteristic, which is uncontrolled cell division. Cancerous DBIBB have the ability to bypass the normal apoptosis mechanism (National Cance
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