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A linker length of and atoms was found to be
2021-10-14

A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and d
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br Introduction The third variable
2021-10-14

Introduction The third variable (V3) loop of the gp120 envelope glycoprotein (Env) on the surface of human immunodeficiency virus type 1 (HIV-1) becomes exposed after the virus binds CD4, the initial receptor; the V3 loop plays an important role in contacting the coreceptor CCR5 or CXCR4 to media
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br Acknowledgements We thank the following individuals for n
2021-10-14

Acknowledgements We thank the following individuals for notable contributions to this work: Dr. Ruth Wood, Dr. Alan Watts, Dr. Casey Donovan, Andrea Suarez, Emily Nakamoto, Allison Apfel, April Banayan, and Jonathan Cheung. This study was supported by the National Institute of Health grants, DK10
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br Conflict of interest statement br Introduction br
2021-10-14

Conflict of interest statement Introduction Gap junction assembly Induced disassembly of gap junctions The regulation of connexin and gap junction turnover are still not well understood. This is, in part, due to the fact that while the overall turnover of connexin molecules is fairly con
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Dysregulation of the HPA axis resulting in alteration to
2021-10-13

Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba
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There were hub genes identified
2021-10-13

There were 11 hub genes identified by WGCNA among which KIBRA was the hub gene of the black module. The bioinformatics method is an effective and powerful tool to analyze mRNA pkc pathway profiles and the related pathways. For instance, the lung cancer risk modules that were closely related to lung
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Under most circumstances NO is a potent endogenous vasodilat
2021-10-13

Under most circumstances, NO is a potent endogenous vasodilator. Therefore, its involvement in an endothelium-dependent contraction seems paradoxical, to say the least. Soluble guanylyl cyclase (sGC) is the major downstream target of NO; its inhibition results in the lack of vasoconstrictor response
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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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