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Having identified initial leads and further
2021-10-13

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic hiv protease inhibitor derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, meth
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Recent evidence suggests that HCA can also mediate antineuro
2021-10-13

Recent evidence suggests that HCA2 can also mediate antineuroinflammatory effects [63]. Studies in this field were initiated when monomethyl fumarate, the metabolite of DMF, was shown to be an agonist of HCA2[5]. DMF at the same time was shown to not only have beneficial effects in the treatment of
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The pharmacokinetics of was obtained in mouse rat and
2021-10-13

The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi
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br Conclusion br Introduction The intracellularly generated
2021-10-13

Conclusion Introduction The intracellularly generated metabolite methylglyoxal (MG, 2-oxopropanal) acts as a potent electrophile causing irreparable cellular damage if allowed to build to cytotoxic concentrations [1], [2], [3], [4], [5], [6]. The glyoxalase (Glx) system is an enzyme couple cri
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About epilepsy no specific seizure type
2021-10-13

About epilepsy, no specific seizure type has been identified because GLUT1-DS is associated with a wide range of epilepsies: patients develop seizures in infancy and early childhood, which are, frequently, do not respond to anticonvulsant medication. In infants, seizures are described as brief, subt
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There are two ways to transport FFAs
2021-10-13

There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty ochratoxin a transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is responsib
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GCK MODY is the most common form of
2021-10-13

GCK-MODY is the most common form of MODY diabetes in many populations (Chevre et al., 1998; Massa et al., 2001; Barrio et al., 2002; Estalella et al., 2007; Pruhova et al., 2010; Capuano et al., 2012; Giuffrida et al., 2017). However, data about GCK-MODY among North African populations are very rare
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Despite the potential promise of
2021-10-13

Despite the potential promise of both of these peptides, such compounds are still susceptible to efficient renal filtration (Emmanouel et al., 1978, Holst, 1991, Deacon et al., 1996). However, numerous studies have demonstrated that fatty SKF 83566 hydrobromide mg dervatisation of related regulatory
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br In vivo actions of GLP
2021-10-13

In vivo actions of GLP-1/GLP-1R agonists on the vascular endothelium Using contrast-enhanced ultrasound, male Sprague Dawley rats receiving an intravenous infusion of native GLP-1 (30 pmol/kg/min) for 2 h demonstrated significant improvements in both microvascular blood volume and microvascular b
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Given the estimated number of NSVDC channels in a red
2021-10-13

Given the estimated number of 150–300 NSVDC channels in a red cell [7] and a single channel conductance of 30 pS at physiological salt concentrations [6], the maximum conductance observed in intact red RGDfK indicate either a very low open state probability, in the order of 10−3 or a far lower unit
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Gap junction channels exhibit different
2021-10-13

Gap junction channels exhibit different types of gating properties. One alternative mechanism that should be mentioned is loop gating in which the extracellular loop of connexin assumes a configuration to form a narrow pathway for closure of unopposed hemichannels [53] and docked junction channels [
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This study introduces a mouse model carrying
2021-10-12

This study introduces a mouse model carrying the point mutation R258W in Ffar1, which abolishes the stimulation of insulin secretion in response to long chain fatty acids. The minimal genetic alteration mirrors the human situation and has the advantage over conventional knockout/congenic mouse model
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br Acknowledgements We thank Dr Bhushan Nagar and
2021-10-12

Acknowledgements We thank Dr. Bhushan Nagar and Dr. Albert Berghuis for access to the X-ray diffraction machine at McGill University. We also thank Dr. Manon Couture and Dr. Steve Charette at Université Laval for access to scientific equipment. Funding for this research was provided by Discovery
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br Materials and methods br Results br Discussion
2021-10-12

Materials and methods Results Discussion Cell migration not only plays major roles in physiological events, such as embryo implantation, embryogenesis, morphogenesis, neurogenesis, angiogenesis, wound healing and inflammation [[29], [30], [31]], but it is also implicated in the pathophysiol
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According to the World Health Organization
2021-10-12

According to the World Health Organization (WHO) classification, oligodendrogliomas or anaplastic oligodendrogliomas are primary neoplasms of the central nervous system, which are predominantly composed of cells morphologically resembling oligodendrocytes [23]. These tumors are often estimated to re
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